Molecular mechanism of anti-SARS-CoV-2 activity of Ephedra Herb macromolecule condensed-tannin contained in Ephedrine alkaloids-free Ephedra Herb extract
M. Hyuga,* N. Uchiyama, M. Yoshimura, Y. Amakura, S. Hyuga, M. Uema, G. Tsuji, A. Nishi, H. Odaguchi, Y. Demizu, Y. Goda* Chem. Pharm. Bull., accepted.
Screening and evaluation of hydrophobic cell-penetrating peptides for antisense oligonucleotide delivery
S. Tamura, G. Tsuji,* Y. Demizu* Bioorg. Med. Chem., 126, 118223 (2025). doi:10.1016/j.bmc.2025.118223
Palindromic Peptide Foldamers : A Strategy for Structural Stability and Cellular Uptake
M. Fujita,# T. Ito,# A. Inokuma, K. Saito, M. Hirano, H. Yokoo,* Y. Demizu* Org. Biomol. Chem., accepted. #These authors equally contributed to this work.
High-resolution HPLC for separating peptide-oligonucleotide conjugates
M. Naganuma, G. Tsuji,* M. Amiya, R. Hirai, Y. Higuchi, N. Hata, S. Nozawa, D. Watanabe, T. Nakajima,* Y. Demizu* ACS Omega, accepted.
Mechanistic study of plasmid DNA delivery by Magainin 2-derived stapled peptides
M. Hirano, Y. Takechi-Haraya, Y. Abe, T. Misawa, N. Shibata, Y. Sato, Y. Demizu* Bioorg. Med. Chem., 123, 118176 (2025). doi:10.1016/j.bmc.2025.118176
Enzymatic hydrolysis of ∆8-THC-O, ∆9-THC-O, 11-α-HHC-O, and 11-β-HHC-O by pooled human liver microsomes to generate ∆8-THC, ∆9-THC, 11-α-HHC, and 11-β-HHC
S. Zhao, J. C. P. García, R. Li, R. Kikura-Hanajiri, Y. Demizu, Y. Tanaka, Y. Ishii* Forensic Toxicol., in press. doi:10.1007/s11419-025-00719-2
Comprehensive in-vitro evaluation of the inhibitory effects of relatively high molecular weight peptides on drug-drug interaction-associated four liver transporters and its association with physicochemical properties
R. Ishikawa, T. Misawa, Y. Demizu, Y. Saito, R. Kikura-Hanajiri, K. Saito* Drug Metab. 61, 101055 (2025). doi:10.1016/j.dmpk.2025.101055
Clozapine as an E3 ligand for PROTAC technology
R. Takano, N. Ohoka,* T. Kurohara, N. Arakawa, K. Ohgane, T. Inoue, H. Yokoo,* Y. Demizu* ACS Med. Chem. Lett., 16, 258-262 (2025). <Selected as Supplementary Cover> doi:10.1021/acsmedchemlett.4c00500
Advances in the development of Wnt/β-catenin signaling inhibitors
M. Fujita, Y. Demizu* RSC Med. Chem., 16, 984-999 (2025). <Selected as Front Cover> doi:10.1039/D4MD00749B
2024
Strategic design of GalNAc-helical peptide ligands for efficient liver targeting
T. Ito, N. Ohoka, M. Aoyama, T. Nishikaze, T. Misawa, T. Inoue, A. Ishii-Watabe, Y. Demizu* Chem. Sci., 15, 18789-18795 (2024). <Selected as Outside Front Cover> doi:10.1039/D4SC05606J
Correlation Between Membrane Permeability and the Intracellular Degradation Activity of Proteolysis-Targeting Chimeras
H. Yokoo, H. Osawa, K. Saito,* Y. Demizu* Chem. Pharm. Bull., 72, 961-965 (2024). <Selected as Featured Article> doi:10.1248/cpb.c24-00615
Linker and Conjugation Site Synergy in Antibody‒Drug Conjugates: Impacts on Biological Activity
M. Aoyama,* M. Tada, H. Yokoo, T. Ito, T. Misawa, Y. Demizu, A. Ishii-Watabe Bioconjug. Chem., 35, 1568-1576 (2024). <Selected as Supplementary Cover> doi:10.1021/acs.bioconjchem.4c00348
Hydrophobic CPP/HDO Conjugates: A New Frontier in Oligonucleotide-Warheaded PROTAC Delivery
M. Naganuma, N. Ohoka,* M. Hirano, D. Watanabe, G. Tsuji, T. Inoue, Y. Demizu* RSC Med. Chem., 15, 3695-3703 (2024). <Selected as Inside Front Cover> doi:10.1039/D4MD00546E
Dual-modified penetratin peptides: Enhancing nucleic acid delivery through stapling and endosomal escape domain
K. Horikoshi, M. Miyamoto, K. Tsuchiya, H. Yokoo,* Y. Demizu* Bioorg. Med. Chem., 111, 117871 (2024). doi:10.1016/j.bmc.2024.117871
Nitrosamine contamination of pharmaceuticals: Cases in Japan, formation mechanisms, detection methods, regulatory perspectives, and insights
G. Tsuji, H. Yokoo, Y. Demizu, Y. Abe, S. Masada, N. Uchiyama, T. Tsutsumi, E. Yamamoto* JPBA Open, 4, 100034 (2024). doi:10.1016/j.jpbao.2024.100034
One-pot C(sp3)-H difluoroalkylation of tetrahydroisoquinolines and isochromans via electrochemical oxidation and
organozinc alkylation
K. Kamata, M. Kuriyama,* H. Tahara, A. Nishikawa, K. Yamamoto, Y. Demizu, O. Onomura* Chem. Commun., 60, 6395-6398 (2024). doi:10.1039/D4CC02033B
The application of microsampling disks in circular dichroism spectroscopy for peptide and nucleic acid drugs
G. Tsuji,# T. Misawa,# Y. Demizu* Chem. Pharm. Bull., 72, 658-663 (2024). #These authors equally contributed to this work. <Selected as Featured Article> doi:10.1248/cpb.c24-00244
In silico design, synthesis and evaluation of PROTAC against hematopoietic prostaglandin D synthase
H. Yokoo, N. Shibata,* Y. Demizu* Methods Mol. Biol., 2780, 345-359 (2024). doi:10.1007/978-1-0716-3985-6_18
Photo-regulated PROTACs: A novel tool for temporal control of targeted protein degradation
H. Xu, N. Ohoka,* T. Inoue, H. Yokoo,* Y. Demizu* Bioorg. Med. Chem. Lett., 107, 129778 (2024). doi:10.1016/j.bmcl.2024.129778
Innovative Peptide Architectures: Advancements in Foldamers and Stapled Peptides for Drug Discovery
Z. Dongrui, M. Miyamoto, H. Yokoo,* Y. Demizu* Expert Opin. Drug Discov., 19, 699-723 (2024). doi:10.1080/17460441.2024.2350568
Structural analysis of an lysergic acid diethylamide (LSD) analogue N-methyl-N-isopropyllysergamide (MiPLA): Insights from Rotamers in NMR spectra
T. Shoda,#,* G. Tsuji,# Y. Kawamura, T. Kurohara, T. Misawa, R. Hanajiri-Kikura, Y. Demizu Drug Test. Anal., 16, 588-594 (2024). #These authors equally contributed to this work. doi:10.1002/dta.3586
Rapid structure determination of ranitidine hydrochloride API in two crystal forms using microcrystal electron diffraction
H. Yokoo,* Y. Aoyama, T. Matsumoto, E. Yamamoto, N. Uchiyama, Y. Demizu* Chem. Pharm. Bull., 72, 471-474 (2024). <Selected as Featured Article> doi:10.1248/cpb.c23-00745
Development of STING degrader with double covalent ligands
M. Nakamura, N. Ohoka,* N. Shibata, T. Inoue, G. Tsuji,* Y. Demizu* Bioorg. Med. Chem. Lett.,102, 129677 (2024).. doi:10.1016/j.bmcl.2024.129677
[3+2] Cycloaddition of Heteroaromatic N-Ylides with Sulfenes
K. Yamamoto,* K. Torigoe, M. Kuriyama, Y. Demizu, O. Onomura* Org. Lett., 26, 798-803 (2024). doi:10.1021/acs.orglett.3c03878
Expansion of targeted degradation by gilteritinib-warheaded PROTACs to ALK fusion proteins
H. Yokoo,# G. Tsuji,# T. Inoue, M. Naito, Y. Demizu,* N. Ohoka* Bioorg. Chem., 145, 107204 (2024). #These authors equally contributed to this work. doi:10.1016/j.bioorg.2024.107204
In silico prediction of N-nitrosamine formation pathways in pharmaceutical products
G. Tsuji,* T. Kurohara, T. Shoda, H. Yokoo, T. Ito, S. Masada, N. Uchiyama, E. Yamamoto, Y. Demizu* Chem. Pharm. Bull., 72, 166-172 (2024). doi:10.1248/cpb.c23-00550
Rational design of amphipathic antimicrobial peptides with alteration of L-/D-amino acids that form helical structures
M. Hirano, H. Yokoo,* N. Ohoka, T. Ito, T. Misawa, M. Oba, T. Inoue, Y. Demizu* Chem. Pharm. Bull., 72, 149-155 (2024). doi:10.1248/cpb.c23-00465
Visualization of the Plasmid DNA Delivery System by Complementary Fluorescence Labeling of Arginine-rich Peptides
A. Imayoshi,* H. Yokoo, M. Kawaguchi, K. Tsubaki, M. Oba* Chem. Pharm. Bull., 72, 856-861 (2024). doi:10.1248/cpb.c24-00479
Poly(ethylene Glycol) (PEG)-OligoRNA Hybridization to mRNA Enables Fine-Tuned Polyplex PEGylation for Spleen-Targeted mRNA Delivery
M. Suzuki,# Y. Mochida,# M. Hori, A. Hayashi, K. Toh, T. A. Tockary, X. Liu, V. Marx, H. Yokoo, Miyata, M. Oba, S. Uchida* Small Science, 4, 2300258 (2024). doi:10.1002/smsc.202300258
2023
Sculpting secondary structure of a cyclic peptide: Conformational analysis of a cyclic hexapeptide containing a combination of L-Leu, D-Leu and Aib residues
T. Ito, H. Yokoo, T. Kato,* M. Doi, Y. Demizu* ACS Omega, 8, 44106-44111 (2023). <Selected as Supplementary Cover> doi:10.1021/acsomega.3c06397
Development of decoy oligonucleotide-warheaded chimeric molecules targeting STAT3
Po-C. Shih, M. Naganuma, G. Tsuji, Y. Demizu, M. Naito* Bioorg. Med. Chem., 95, 117507 (2023). doi:10.1016/j.bmc.2023.117507
Structural optimization of decoy oligonucleotide-based PROTAC that degrades the estrogen receptor
M. Naganuma, N. Ohoka,* G. Tsuji, T. Inoue, M. Naito, Y. Demizu* Bioconjug. Chem., 34, 1780-1788 (2023).. <Selected as Supplementary Cover> doi:10.1021/acs.bioconjchem.3c00332
Magainin 2-derived stapled peptides derived with the ability to deliver pDNA, mRNA, and siRNA into cells
M. Hirano, H. Yokoo, C. Goto, M. Oba, T. Misawa,* Y. Demizu* Chem. Sci., 14, 10403-10410 (2023). <Selected as Front Cover> doi:10.1039/D3SC04124G
Enhancing chemical stability through structural modification of antimicrobial peptides with non-proteinogenic amino acids
T. Ito.,# N. Matsunaga,# M. Kurashima, Y. Demizu,* T. Misawa* Antibiotics, 12, 1326 (2023). #These authors equally contributed to this work. doi:10.3390/antibiotics12081326
Development of hydrophobic cell-penetrating stapled peptides as drug carriers
K. Tsuchiya, K. Horikoshi, M. Fujita, M. Hirano, M. Miyamoto, H. Yokoo,* Y. Demizu* Int. J. Mol. Sci., 24, 11768 (2023). doi:10.3390/ijms241411768
Structure-activity relationship study of helix-stabilized antimicrobial peptides containing non-proteinogenic amino acids
T. Ito, W. Hashimoto, N. Ohoka, T. Misawa, T. Inoue, R. Kawano, Y. Demizu* ACS Biomater. Sci. Eng., 9, 4654-4661 (2023). <Selected as Supplementary Cover> doi:10.1021/acsbiomaterials.3c00759
Identification of the Stapled α-Helical Peptide ATSP-7041 as a Substrate and Strong Inhibitor of OATP1B1 In Vitro
R. Ishikawa, K. Saito,* T. Misawa, Y. Demizu, Y. Saito Biomolecules, 13(6), 1002 (2023). doi:10.3390/biom13061002
Development of DNA aptamer-based PROTACs that degrade the estrogen receptor
H. Tsujimura,# M. Naganuma,# N. Ohoka,* T. Inoue, M. Naito, G. Tsuji,* Y. Demizu* ACS Med. Chem. Lett., 14, 827-832 (2023). #These authors equally contributed to this work. doi:10.1021/acsmedchemlett.3c00126
Development of a versatile solid-phase synthesis of PROTAC with diverse E3 ligands
H. Xu#, T. Kurohara#, N. Ohoka, G. Tsuji, Inoue, M. Naito, Y. Demizu* Bioorg. Med. Chem., 86, 117293 (2023). #These authors equally contributed to this work. doi:10.1016/j.bmc.2023.117293
Design and properties of PNA containing a dicationic nucleobase based on N4-benzoylated cytosine
S. Moriya, K. Funaki, Y. Demizu, M. Kurihara, A. Kittaka, T. Sugiyama* Bioorg. Med. Chem. Lett., 88, 129287 (2023). doi:10.1016/j.bmcl.2023.129287
Design of antimicrobial peptides containing non-proteinogenic amino acids using multi-objective Bayesian optimization
Y. Murakami, S. Ishida, Y. Demizu, K. Terayama* Digital Discovery, 2, 1347-1353 (2023).. ChemRxiv, doi:10.26434/chemrxiv-2023-cbrjc
In silico optimization of peptides that inhibit Wnt/β-catenin signaling
M. Fujita, K. Tsuchiya,* T. Kurohara, K. Fukuhara, T. Misawa, Y. Demizu* Bioorg. Med. Chem., 84, 117264 (2023). doi:10.1016/j.bmc.2023.117264
CRBN ligand expansion for Hematopoietic Prostaglandin D2 Synthase (H-PGDS) targeting PROTAC design and their ADME profiles
H. Osawa,# T. Kurohara,# T. Ito, N. Shibata, Y. Demizu* Bioorg. Med. Chem., 84, 117259 (2023). doi:10.1016/j.bmc.2023.117259
Investigating the cell permeability of PROTACs
H. Yokoo, M. Naito,* Y. Demizu* Expert Opin. Drug Discov., 18, 357-361 (2023). doi:10.1080/17460441.2023.2187047
Current status of oligonucleotide-warheaded protein degraders
Po-C. Shih, M. Naganuma, Y. Demizu, M. Naito* Pharmaceutics, 15(3), 765 (2023). doi:10.3390/pharmaceutics15030765
Developmental trends of peptide drugs and their quality assessment using secondary structure analysis
T. Misawa,* Y. Demizu ChemistrySelect, 8, e202300408 (2023). doi:10.1002/slct.202300408
Structure-activity relationship studies of substitutions of cationic amino acid residues on antimicrobial peptides
M. Takada, T. Ito, M. Kurashima, N. Matsunaga, Y. Demizu,* T. Misawa* Antibiotics, 12(1), 19 (2023). doi:10.3390/antibiotics12010019
Comprehensive synthesis of 20 fentanyl derivatives for use as reference materials
T. Kurohara,# T. Ito,# G. Tsuji,* T. Misawa,* H. Yokoo, M. Kawamura, T. Shoda, R. Hanajiri-Kikura, Y. Demizu Heterocycles, 106, 82-93 (2023). #These authors equally contributed to this work. doi:10.3987/COM-22-14760
Advanced solid-state NMR analysis of two crystal forms of ranitidine hydrochloride: Detection of 1H-14N intra-/intermolecular correlations
H. Yokoo,# S. Tanaka,# E. Yamamoto, G. Tsuji, Y. Demizu,* N. Uchiyama* Chem. Pharm. Bull., 71, 58-63 (2023). #These authors equally contributed to this work. <Highlighted Paper selected by Editor-in-Chief> <Selected as Featured Article> doi:10.1248/cpb.c22-00628
Effect of helicity and hydrophobicity on cell-penetrating ability of arginine-rich peptides
M. Oba,* S. Nakajima, K. Misao, H. Yokoo, M. Tanaka Bioorg. Med. Chem., 91, 117409 (2023). doi:10.1016/j.bmc.2023.117409
An amphipathic structure of a dipropylglycine-containing helical peptide with sufficient length enables safe and effective intracellular siRNA delivery
M. Oba,* M. Shibuya, Y. Yamaberi, H. Yokoo, S. Uchida, A. Ueda, M. Tanaka Chem. Pharm. Bull., 71, 250-256 (2023). doi:10.1248/cpb.c22-00852
2022
Oligoarginine-conjugated peptide foldamers inhibiting vitamin D receptor-mediated transcription
M. Takyo, Y. Sato, N. Hirata, K. Tsuchiya, H. Ishida, T. Kurohara, Y. Yanase, T. Ito, N. Ito, Y. Kanda, K. Yamamoto, T. Misawa,* Y. Demizu* ACS Omega, 7, 46573-46582 (2022). doi:10.1021/acsomega.2c05409
Development of Gilteritinib-based chimeric small molecules that potently induce degradation of FLT3-ITD protein
N. Ohoka,* M. Suzuki, T. Uchida, G. Tsuji, Y. Tsukumo, M. Yoshida, T. Inoue, Y. Demizu, H. Ohki, M. Naito* ACS Med. Chem. Lett., 13, 1885-1891 (2022). doi:10.1021/acsmedchemlett.2c00402
Derivatives of methoxetamine and major methoxetamine metabolites potently block NMDA receptors
T. Irie,* Y. Yanase, Y. Demizu, M. Usami, R. Kikura-Hanajiri J. Pharmacol. Sci., 150, 233-243 (2022). doi:10.1016/j.jphs.2022.09.005
Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase
Y. Murakami,# H. Osawa,# T. Kurohara,# Y. Yanase, T. Ito, H. Yokoo, N. Shibata, M. Naito, K. Aritake, Y. Demizu* RSC Med. Chem., 13, 1495-1503 (2022). #These authors equally contributed to this work. <Selected as Front Cover> doi:10.1039/D2MD00284A
Recent advances in PROTAC technology toward new therapeutic modalities
H. Yokoo,* M. Naganuma, M. Oba, Y. Demizu* Chem. Biodivers., 19, e202200828 (2022). <Selected as Front Cover> doi:10.1002/cbdv.202200828
Development of a penetratin-conjugated stapled peptide that inhibits Wnt/β-catenin signaling
K. Tsuchiya, M. Kiyoshi, N. Hashii, M. Fujita, T. Kurohara, A. Ishii-Watabe, K. Fukuhara, T. Misawa,* Y. Demizu* Bioorg. Med. Chem., 73, 117021 (2022). doi:10.1016/j.bmc.2022.117021
Development of delivery carriers for plasmid DNA by conjugation of a helical template to oligoarginine
H. Yokoo,# T. Misawa,# T. Kato, M. Tanaka, Y. Demizu,* M. Oba* Bioorg. Med. Chem., 72, 116997 (2022). #These authors equally contributed to this work. doi:10.1016/j.bmc.2022.116997
Organocatalytic synthesis of phenols from diaryliodonium salts with water under metal-free conditions
K. Katagiri, M. Kuriyama,* K. Yamamoto, Y. Demizu, O. Onomura* Org. Lett., 24, 5149-5154 (2022). doi:10.1021/acs.orglett.2c01989
Control of STING Agonistic/Antagonistic Activity Using Amine-Skeleton-Based c-di-GMP Analogues
Y. Yanase, G. Tsuji,* M. Nakamura, N. Shibata, Y. Demizu* Int. J. Mol. Sci., 23(12), 6847 (2022). doi:10.3390/ijms23126847
Development of rapid and facile solid-phase synthesis of PROTACs via a variety of binding styles
H. Xu#, T. Kurohara#, R. Takano, H. Yokoo, N. Shibata, N. Ohoka, T. Inoue, M. Naito, Y. Demizu* ChemistryOpen, 11, e303300131 (2022). #These authors equally contributed to this work. doi:10.1002/open.202200131
Helix-Stabilized Cell-Penetrating Peptides for Delivery of Antisense Morpholino Oligomers: Relationships among Helicity, Cellular Uptake, and Antisense Activity
H. Takada, K. Tsuchiya, Y. Demizu* Bioconjug. Chem., 38, 1311-1318 (2022).
<Selected as Front Cover> doi:10.1021/acs.bioconjchem.2c00199
Analysis of the interaction of cyclosporine congeners with cell membrane models
M. Nakao, Y. Takeuchi-Haraya, T. Ohgita, H. Saito, Y. Demizu, K. Izutsu, K. Sakai-Kato* J. Pharm. Biomed. Anal., 218, 114874 (2022). doi:10.1016/j.jpba.2022.114874
Current Status and Challenges of Analytical Methods for Evaluation of Size and Surface Modification of Nanoparticle-Based Drug Formulations
Y. Takeuchi-Haraya,* T. Ohgita, Y. Demizu, H. Saito, T. Nakanishi, K. Izutsu K. Sakai-Kato* AAPS PharmSciTech, 23, 150 (2022). doi:10.1208/s12249-022-02303-y
Helical Foldamers and Stapled Peptides as New Modalities in Drug Discovery: Modulators of Protein-Protein Interactions
K. Tsuchiya, T. Kurohara, K. Fukuhara, T. Misawa,* Y. Demizu* Processes, 10, 924 (2022)． doi:10.3390/pr10050924
Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication
G. Tsuji,#,* S. Nakajima,# K. Watashi, S. Torii, R. Suzuki, T. Fukuhara, N. Ohoka, T. Inoue, Y. Demizu* J. Pharmacol. Sci., 149, 81-84 (2022). #These authors equally contributed to this work. doi:10.1016/j.jphs.2022.04.001
Copper-Catalyzed Asymmetric Oxidative Desymmetrization of 2-Substituted 1,2,3-Triols
K. Yamamoto, Y. Suganomata, T. Inoue, M. Kuriyama, Y. Demizu, O. Onomura* J. Org. Chem., 87, 6479-6491 (2022). doi:10.1021/acs.joc.2c00398
Molecular Design, Synthesis, and Evaluation of SNIPER (ER) that Induces Targeted Protein Degradation of ERα
N. Ohoka,# H. Yokoo,# K. Okuhira, Y. Demizu, M. Naito* Methods Mol. Biol., 2418, 363-382 (2022). #These authors equally contributed to this work. doi:10.1007/978-1-0716-1920-9_20
Development of Chimeric Molecules That Degrade the Estrogen Receptor Using Decoy Oligonucleotide Ligands
M. Naganuma, N. Ohoka,* G. Tsuji, H. Tsujimura, K. Matsuno, T. Inoue, M. Naito, Y. Demizu* ACS Med. Chem. Lett., 13, 134-139 (2022).
<Selected as Supplementary Cover> doi:10.1021/acsmedchemlett.1c00629
The effects of magainin 2-derived and rationally designed antimicrobial peptides on Mycoplasma pneumoniae
K. Hayashi,* T. Misawa, C. Goto, Y. Demizu, Y. Hara-Kudo, Y. Kikuchi PLOS ONE, 17, e0261893 (2022). doi:10.1371/journal.pone.0261893
Nanoparticle tracking analysis for characterization of extracellular vesicles including exosomes
K. Sakai-Kato,* S. Yahata, Y. Takeuchi-Haraya, T. Ohgita, Y. Demizu, H. Saito, K. Izutsu Pharm. Tech. Japan, 38, 213-218 (2022).
Fcγ Receptor-Dependent Internalization and Off-Target Cytotoxicity of Antibody-Drug Conjugate Aggregates
M. Aoyama,* M. Tada, H. Yokoo, Y. Demizu, Ishii-Watabe Pharm. Res., 39, 89-103 (2022). doi:10.1007/s11095-021-03158-x
2021
Synthesis of Norgestomet and its 17β-isomer and evaluation of their agonistic activities against progesterone receptor
T. Kurohara, T. Ito, G. Tsuji,* T. Misawa,* H. Yokoo, Y. Yanase, T. Shoda, T. Sakai, J. Hosoe, N. Uchiyama, H. Akiyama, Y. Demizu Bioorg. Med. Chem., 49, 116425 (2021). doi:10.1016/j.bmc.2021.116425
Peptide Stapling Improves the Sustainability of a Peptide-Based Chimeric Molecule That Induces Targeted Protein Degradation
H. Yokoo,# N. Ohoka,# M. Takyo, T. Ito, K. Tsuchiya, T. Kurohara, K. Fukuhara, T. Inoue, M. Naito, Y. Demizu* Int. J. Mol. Sci., 22, 8772 (2021). #These authors equally contributed to this work. doi:10.3390/ijms22168772
Nickel-Catalyzed Hydrodeoxygenation of Aryl Sulfamates with Alcohols as Mild Reducing Agents
K. Matsuo, M. Kuriyama,* K. Yamamoto, Y. Demizu, K. Nishida, O. Onomura* Synthesis, 53, 4449-4460 (2021). doi:10.1055/a-1548-8362
Discovery of non-proteinogenic amino acids inhibiting biofilm formation by S. aureus and methicillin-resistant S. aureus
K. Ikeda, T. Shoda, Y. Demizu,* G. Tsuji* Bioorg. Med. Chem. Lett., 48, 128259 (2021). doi:10.1016/j.bmcl.2021.128259
Structure–activity relationship study of amphipathic antimicrobial peptides using helix-destabilizing sarcosine
H. Yokoo,* M. Hirano, N. Ohoka, T. Misawa, Y. Demizu* J. Pept. Sci., e3360, 1-6 (2021). doi:10.1002/psc.3360
Discovery of a Highly Potent and Selective Degrader Targeting Hematopoietic Prostaglandin D Synthase via In Silico Design
H. Yokoo, N. Shibata,* A. Endo, T. Ito, Y. Yanase, Y. Murakami, K. Hamamura, Y. Saeki, M. Naito,* K. Aritake,* Y. Demizu* J. Med. Chem., 64, 15868-15882 (2021).
<Selected as Supplementary Cover> doi:10.1021/acs.jmedchem.1c01206
N-Nitrosodimethylamine (NDMA) Formation from Ranitidine Impurities: Possible Root Causes of the Presence of NDMA in Ranitidine Hydrochloride
H. Yokoo,# E. Yamamoto,#,* S. Masada, N. Uchiyama, G. Tsuji, T. Hakamatsuka, Y. Demizu, K. Izutsu, Y. Goda Chem. Pharm. Bull., 69, 872-876 (2021). #These authors equally contributed to this work. doi:10.1248/cpb.c21-00289
Development of Agonist-Based PROTACs Targeting Liver X Receptor
H. Xu,# N. Ohoka,# H. Yokoo, K. Nemoto, T. Ohtsuki, H. Matsufuji, M. Naito, T. Inoue, G. Tsuji,* Y. Demizu* Frontiers in Chemistry, 9, 674967 (2021). #These authors equally contributed to this work. doi:10.3389/fchem.2021.674967
Development of ciclesonide analogues that block SARS-CoV-2 RNA replication
G. Tsuji,# K. Yonemitsu,# T. Ito, Y. Yanase, M. Uema, N. Ohoka, T. Inoue, H. Asakura, Y. Demizu* Bioorg. Med. Chem. Lett.,43, 128052 (2021). #These authors equally contributed to this work. doi:10.1016/j.bmcl.2021.128052
Miroestrol Quantification in Pueraria mirifica Crude Drugs and Products by Single-Reference UPLC/PDA/MS Using Relative Molar Sensitivities to Kwakhurin
S. Masada, J. Hosoe, R. Arai, Y. Demizu, T. Hakamatsuka, Y. Goda, N. Uchiyama* Chem. Pharm. Bull., 69, 573-580 (2021). doi:10.1248/cpb.c21-00160
Protocols for synthesis of SNIPERs and the methods to evaluate the anticancer effects
Y. Tsukumo,# G. Tsuji,# H. Yokoo, N. Shibata, N. Ohoka, Y. Demizu, M. Naito* Methods Mol. Biol., 2365, 331-347 (2021). #These authors equally contributed to this work. doi:10.1007/978-1-0716-1665-9_18
Design and synthesis of novel estrogen receptor antagonists with acetal containing biphenylmethane skeleton
M. Yuyama, T. Misawa, Y. Demizu, T. Kanaya, M. Kurihara* Results in Chemistry, 3, 100124 (2021). doi:10.1016/j.rechem.2021.100124
Synthesis and characterization of PNA oligomers containing preQ1 as a positively charged guanine analogue
S. Moriya, H. Shibasaki, M. Kohara, K. Kuwata, Y. Imamura, Y. Demizu, M. Kurihara, A. Kittaka, T. Sugiyama* Bioorg. Med. Chem. Lett., 39, 127850 (2021). doi:10.1016/j.bmcl.2021.127850
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer
H. Yokoo,# N. Shibata,# M. Naganuma, Y. Murakami, T. Ito, K. Aritake,* M. Naito,* Y. Demizu* ACS Med. Chem. Lett., 12, 236-241 (2021).
<Selected as Supplementary Cover>
Development of Antimicrobial Stapled Peptides Based on Magainin 2 Sequence
M. Hirano, C. Saito, H. Yokoo, C. Goto, R. Kawano, T. Misawa,* Y. Demizu* Molecules, 26, 444 (2021). Special Issue Novel Antibacterials: Antimicrobial Peptides, Peptidomimetics and Conjugates doi:10.3390/molecules26020444
TRIP12 promotes small-molecule-induced degradation through K29/K48-branched ubiquitin chains
A. Soma-Kaiho, Y. Akizuki, K. Igarashi, A. Endo, Y. Kawase, T. Shoda, Y. Demizu, M. Naito, Y. Saeki, K. Tanaka, F. Ohtake* Mol. Cell, 81, 1411-1424 (2021). doi:10.1016/j.molcel.2021.01.023
Helical Antimicrobial Peptide Foldamers Containing Non-proteinogenic Amino Acids
H. Yokoo, M. Hirano, T. Misawa, Y. Demizu* ChemMedChem, 16, 1226-1233 (2021). doi:10.1002/cmdc.202000940
Approach to Establishment of Control Strategy for Oral Solid Dosage Forms Using Continuous Manufacturing
H. Ishimoto,* M. Kano, H. Sugiyama, H. Takeuchi, K. Terada, A. Aoyama, T. Shoda, Y. Demizu, J. Shimamura, R. Yokoyama, Y. Miyamoto, K. Hasegawa, M. Serizawa, K. Unosawa, K. Osaki, N. Asai, Y. Matsuda Chem. Pharm. Bull., 69, 211-217 (2021). doi:10.1248/cpb.c20-00824
Transition Metal-Free O-Arylation of Quinoxalin-2-ones with Diaryliodonium Salts
M. Kuriyama,* Y. Mochizuki, T. Miyagi, K. Yamamoto, Y. Demizu, O. Onomura* Heterocycles, 103, doi:10.3987/COM-20-S(K)26 (2021). doi:10.3987/COM-20-S(K)26
Development of Selective TGR5 Ligands Based on the 5,6,7,8-Tetrahydro-5,5,8,8-tetramethylnaphthalene Skeleton
R. Terui, Y. Yanase, H. Yokoo, Y. Suhara, M. Makishima, Y. Demizu,* T. Misawa* ChemMedChem, 16, 458-462 (2021).
<Selected as Front Cover> doi:10.1002/cmdc.202000567
Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors
K. Ikeda,# Y. Yanase,# H. Hayashi, Y. Hara-Kudo, G. Tsuji,* Y. Demizu* Bioorg. Med. Chem. Lett., 32, 127713 (2021). #These authors equally contributed to this work. doi:10.1016/j.bmcl.2020.127713
2020
Rational Design of Helix-Stabilized Antimicrobial Peptide Foldamers Containing α,α-Disubstituted Amino Acids or Side-Chain Stapling
M. Hirano, C. Saito, C. Goto, H. Yokoo, R. Kawano, T. Misawa,* Y. Demizu* ChemPlusChem, 85, 2731-2736 (2020). doi:10.1002/cplu.202000749
Synthesis of Chiral α-Trifluoromethyl α,α-Disubstituted α-Amino Acids and Conformational Analysis of L-Leu-Based Peptides with (R)- or (S)-α-Trifluoromethylalanine
A. Ueda, M. Ikeda, T. Kasae, M. Doi, M. Oba, Y. Demizu, M. Tanaka* ChemistrySelect, 5, 10882-10886 (2020). doi:10.1002/slct.202002888
De Novo Design of Cell-Penetrating Foldamers
H. Yokoo, T. Misawa,* Y. Demizu* Chem. Rec., 20, 912-921 (2020).
<Selected as Cover Picture> doi:10.1002/tcr.202000047
Design and synthesis of peptide-based chimeric molecules to induce degradation of the estrogen and androgen receptors
H. Yokoo,# N. Ohoka,# M. Naito, Y. Demizu* Bioorg. Med. Chem., 28, 115595 (2020). #These authors equally contributed to this work. doi:10.1016/j.bmc.2020.115595
Temperature-Dependent Formation of N-Nitrosodimethylamine during the Storage of Ranitidine Reagent Powders and Tablets
Y. Abe,# E. Yamamoto,# H. Yoshida, A. Usui, N. Tomita, H. Kanno, S. Masada, H. Yokoo, G. Tsuji, N. Uchiyama, T. Hakamatsuka, Y. Demizu, K. Izutsu,* Y. Goda, H. Okuda Chem. Pharm. Bull., 68, 1008-1012 (2020). #These authors equally contributed to this work. doi:10.1248/cpb.c20-00431
Design, Synthesis, and Biological Activity of Conformationally Restricted Analogues of Silibinin
M. Mizuno, K. Mori, K. Tsuchiya, T. Misawa, Y. Demizu, M. Shibanuma, K. Fukuhara* ACS Omega, 5,23164-23174 (2020). doi:10.1021/acsomega.0c02936
Facile Synthesis of Kwakhurin, a Marker Compound of Pueraria mirifica and Its Quantitative NMR Analysis for Standardization as a Reagent
G. Tsuji,# M. Yusa,# S. Masada, H. Yokoo, J. Hosoe, T. Hakamatsuka, Y. Demizu,* N. Uchiyama* Chem. Pharm. Bull., 68, 797-801 (2020). #These authors equally contributed to this work. doi:10.1248/cpb.c20-00346
Targeted Protein Degradation by Chimeric Compounds using Hydrophobic E3 Ligands and Adamantane Moiety
T. Shoda,* N. Ohoka, G. Tsuji, T. Fujisato, H. Inoue, Y. Demizu, M. Naito, M. Kurihara Pharmaceuticals, 13, 34 (2020). doi:10.3390/ph13030034
Selective Degradation of Target Proteins by Chimeric Small-Molecular Drugs, PROTACs and SNIPERs
M. Ishikawa,* S. Tomoshige, Y. Demizu, M. Naito Pharmaceuticals, 13, 74 (2020). doi:10.3390/ph13040074
Critical role of mitochondrial ubiquitination and the OPTN–ATG9A axis in mitophagy
K. Yamano,* R. Kikuchi, W. Kojima, R. Hayashida, F. Koyano, J. Kawawaki, T. Shoda, Y. Demizu, M. Naito, K. Tanaka, N. Matsuda* J. Cell. Biol., 219, e201912144 (2020). doi:10.1083/jcb.201912144
Deubiquitylase USP25 prevents degradation of BCR-ABL protein and ensures proliferation of Ph-positive leukemia cells
N. Shibata, N. Ohoka, G. Tsuji, Y. Demizu, T. Akiyama, M. Naito* Oncogene, 39, 3867-3878 (2020). doi:10.1038/s41388-020-1253-0
Development of Photoswitchable Estrogen Receptor Ligands
K. Tsuchiya, T. Umeno, G. Tsuji, H. Yokoo, M. Tanaka, K. Fukuhara, Y. Demizu,* T. Misawa* Chem. Pharm. Bull., 68, 398-402 (2020). doi:10.1248/cpb.c19-01108
Copper-Catalyzed Enantioselective Synthesis of Oxazolines from Aminotriols via Asymmetric Desymmetrization
K. Yamamoto, Y. Tsuda, M. Kuriyama Y. Demizu, O. Onomura* Chem. Asian J., 15, 840-844 (2020). doi:10.1002/asia.201901742
Design and Synthesis of 4-(2-Pyrrolyl)-4-phenylheptane Derivatives as Estrogen Receptor Antagonists
M. Naganuma, H. Yokoo, T. Misawa, K. Matsuno, G. Tsuji,* Y. Demizu* Heterocycles, 101, 429-434 (2020). doi:10.3987/COM-19-14121
2019
Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins
N. Ohoka, G. Tsuji, T. Shoda, T. Fujisato, M. Kurihara, Y. Demizu, M. Naito* ACS Chem. Biol., 14, 2822-2832 (2019). doi:10.1021/acschembio.9b00704
Development of Amphipathic Antimicrobial Peptide Foldamers Based on Magainin 2 Sequence
C. Goto, M. Hirano, K. Hayashi, Y. Kikuchi, Y. Hara-Kudo, T. Misawa,* Y. Demizu* ChemMedChem, 14, 1911-1916 (2019). doi:10.1002/cmdc.201900460
Rapid and efficient high-performance liquid chromatography analysis of N-nitrosodimethylamine impurity in valsartan drug substance and its products
S. Masada,# G. Tsuji,# R. Arai, N. Uchiyama,* Y. Demizu,* T. Tsutsumi, Y. Abe, H. Akiyama, T. Hakamatsuka, K. Izutsu, Y. Goda, H. Okuda #These authors equally contributed to this work. Sci. Rep., 9, 11852 (2019). doi:10.1038/s41598-019-48344-5
Inhibition of β-amyloid–induced neurotoxicity by planar analogues of procyanidin B3
M. Mizuno, K. Mori, T. Misawa, Y. Demizu, M. Shibanuma, K. Fukuhara* Bioorg. Med. Chem. Lett., 29, 2659-2663 (2019). doi:10.1016/j.bmcl.2019.07.038
Refining Calibration Procedures of Circular Dichroism Spectrometer to Improve Usability
K. Sakai-Kato,* K. Yoshida, T. Ohgita, Y. Takechi-Haraya, Y. Demizu, H. Saito Anal. Sci., 35, 1275-1278 (2019). doi:10.2116/analsci.19N022
Palladium-Catalyzed Synthesis of Deuterated Alkenes through Deuterodechlorination of Alkenyl Chlorides
M. Kuriyama,* G. Yano, H. Kiba, T. Morimoto, K. Yamamoto, Y. Demizu, O. Onomura* Org. Process Res. Dev., 23, 1152-1557 (2019). doi:10.1021/acs.oprd.9b00193
Development of 2-aminoisobutyric acid (Aib)-rich cell-penetrating foldamers for efficient siRNA delivery
T. Misawa,* N. Ohoka,* M. Oba, H. Yamashita, M. Tanaka, M. Naito, Y. Demizu* Chem. Commun., 55, 7792-7795 (2019). doi:10.1039/C9CC02203A
Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues
T. Misawa, C. Goto, N. Shibata, M. Hirano, Y. Kikuchi,* M. Naito,* Y. Demizu* MedChemComm, 10, 896-900 (2019).
<Selected as Cover Picture> doi:10.1039/C9MD00166B
Facile synthesis of a-exo-methylene ketones from a,a-disubstituted allyl alcohols by electrochemical oxidative migration
Facile Synthesis of α-exo-Methylene Ketones from α,α-Disubstituted Allyl Alcohols by Electrochemical Oxidative Migration
K. Yamamoto, N. Kikuchi, T. Hamamizu, H. Yoshimatsu, M. Kuriyama, Y. Demizu, O. Onomura* ChemElectroChem, 16, 4169-4172 (2019). doi:10.1002/celc.201900172
Analysis of an Impurity, N-Nitrosodimethylamine, in Valsartan Drug Substances and Associated Products Using GC-MS
T. Tsutsumi, H. Akiyama,* Y. Demizu, N. Uchiyama, S. Masada, G. Tsuji, R. Arai, Y. Abe, Y. Haraya, T. Hakamatsuka, K. Izutsu, Y. Goda, H. Okuda Biol. Pharm. Bull., 42, 547-551 (2019). doi:10.1248/bpb.b19-00006
2018
Left-Handed Helix of Three-Membered Ring Amino Acid Homopeptide Interrupted by an N–H···Ethereal O-Type Hydrogen Bond
Y. Koba, A. Ueda, M. Oba, M. Doi, T. Kato, Y. Demizu, M. Tanaka* Org. Lett., 20, 7830-7834 (2018). doi:10.1021/acs.orglett.8b03331
Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon
T. Misawa,* G. Tsuji, T. Takahashi, E. Ochiai, K. Takagi, K. Horie, S. Kakuda, M. Takimoto-Kamimura, M. Kurihara,* Y. Demizu* Bioorg. Med. Chem.，26, 6146-6152 (2018). doi:10.1016/j.bmc.2018.11.008
Design and synthesis of cell-permeable fluorescent nitrilotriacetic acid derivatives
G. Tsuji,* T. Hattori, M. Kato, W. Hakamata, H. Inoue, M. Naito, M. Kurihara, Y. Demizu, T. Shoda* Bioorg. Med. Chem., 46, 5494-5498 (2018). doi:10.1016/j.bmc.2018.09.028
Extent of Helical Induction Caused by Introducing α-Aminoisobutyric Acid into an Oligovaline Sequence
G. Tsuji, T. Misawa, M. Doi, Y. Demizu* ACS Omega, 3,6395-6399 (2018). doi:10.1021/acsomega.8b01030
Structural Development of Cell-Penetrating Peptides Containing Cationic Proline Derivatives
H. Kobayashi, T. Misawa,* M. Oba, N. Hirata, Y. Kanda, M. Tanaka, K. Matsuno, Y. Demizu* Chem. Pharm. Bull., 66,575-580 (2018).
<Highlighted Paper selected by Editor-in-Chief> doi:10.1248/cpb.c18-00079
Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton
R. Eto, T. Misawa,* N. Ohoka, M. Kurihara, M. Naito, M. Tanaka, Y. Demizu* Bioorg. Med. Chem., 26,1638-1642 (2018). doi:10.1016/j.bmc.2018.02.010
Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins
K. Okitsu, T. Hattori, T. Misawa, T. Shoda, M. Kurihara, M. Naito,* Y. Demizu* J. Med. Chem., 61,576-582 (2018). doi:10.1021/acs.jmedchem.7b00413
2017
Rational Design and Synthesis of Post-Functionalizable Peptide Foldamers as Helical Templates
T. Misawa,* Y. Kanda, Y. Demizu* Bioconj. Chem., 28, 3029-3035 (2017). doi:10.1021/acs.bioconjchem.7b00621
Diastereomeric Right- and Left-Handed Helical Structures with Fourteen (R)-Chiral Centers
R. Eto, M. Oba, A. Ueda, T. Uku, M. Doi, Y. Demizu, M. Kurihara, M. Tanaka* Chem. Eur. J., 23, 18120-18124 (2017). doi:10.1002/chem.201705306
Preorganized Cyclic α,α-Disubstituted α-Amino Acids Bearing Functionalized Side Chains That Act as Peptide-Helix Inducers
H. Kobayashi, T. Misawa, K. Matsuno, Y. Demizu* J. Org. Chem., 82, 10722-10726 (2017). doi:10.1021/acs.joc.7b01946
Development of a peptide-based inducer of protein degradation targeting NOTCH1
N. Ohoka,# T. Misawa,# M. Kurihara, Y. Demizu,* M. Naito* #These authors equally contributed to this work. Bioorg. Med. Chem. Lett., 27, 4985-4988 (2017). doi:10.1016/j.bmcl.2017.10.011
Simple and efficient knockdown of His-tagged proteins by ternary molecules consisting of a His-tag ligand, a ubiquitin ligase ligand, and a cell-penetrating peptide
T. Hattori, K. Okitsu, N. Yamazaki, N. Ohoka, N. Shibata, T. Misawa, M. Kurihara, Y. Demizu,* M. Naito* Bioorg. Med. Chem. Lett., 27, 4478-4481 (2017). doi:10.1016/j.bmcl.2017.08.001
Development of helix-stabilized antimicrobial peptides composed of lysine and hydrophobic α,α-disubstituted α-amino acid residues
T. Misawa, M. Imamura, Y. Ozawa, K. Haishima, M. Kurihara, Y. Kikuchi,* Y. Demizu* Bioorg. Med. Chem. Lett., 27, 3950-3953 (2017). doi:10.1016/j.bmcl.2017.07.074
Development of an ON/OFF switchable fluorescent probe targeting His tag fused proteins in living cells
K. Okitsu, T. Misawa,* T. Shoda, M. Kurihara, Y. Demizu* Bioorg. Med. Chem. Lett., 27, 3417-3422 (2017). doi:10.1016/j.bmcl.2017.05.087
PNA monomers fully compatible with standard Fmoc-based solid-phase synthesis of pseudocomplementary PNA
T. Sugiyama,* G. Hasegawa, C. Niikura, K. Kuwata, Y. Imamura, Y. Demizu, M. Kurihara, M. Takano, A. Kittaka* Bioorg. Med. Chem. Lett., 27, 3337-3341 (2017). doi:10.1016/j.bmcl.2017.06.015
Efficient synthesis of a multi-substituted diphenylmethane skeleton as a steroid mimetic
T. Misawa,* K. Tanaka, Y. Demizu, M. Kurihara* Bioorg. Med. Chem. Lett., 27, 2590-2593 (2017). doi:10.1016/j.bmcl.2017.03.066
Low pH-triggering changes in peptide secondary structures
K. Furukawa, M. Oba,* K. Toyama, G. O. Opiyo, Y. Demizu, M. Kurihara, M. Doi, M. Tanaka* Org. Biomol. Chem., 15, 6302-6305 (2017). <Selected as Cover Picture> doi:10.1039/C7OB01374D
Helical L–Leu-Based Peptides Having Chiral Five-Membered Carbocyclic Ring Amino Acids with an Ethylene Acetal Moiety
Y. Koba, A. Ueda, M. Oba, M. Doi, Y. Demizu, M. Kurihara, M. Tanaka* ChemistrySelect, 2,8108-8114 (2017). doi:10.1002/slct.201700832
Tamoxifen and Fulvestrant Hybrids Showed Potency as Selective Estrogen Receptor Down-Regulators
T. Shoda,* M. Kato, T. Fujisato, Y. Demizu, H. Inoue, M. Naito, M. Kurihara* Med. Chem. (Bentham), 13, 206-213 (2017). doi:10.2174/1573406412666160805101408
Targeted Degradation of Proteins Localized in Subcellular Compartments by Hybrid Small Molecules
K. Okuhira, T. Shoda, R. Omura, N. Ohoka, T. Hattori, N. Shibata, Y. Demizu, R. Sugihara, A. Ichino, H. Kawahara, Y. Ito, M. Ishikawa, Y. Hashimoto, M. Kurihara, H. Saito, M. Naito* Mol. Pharmacol., 91, 159-166 (2017). doi:10.1124/mol.116.105569
Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton
T. Misawa,* T. Fujisato, Y. Kanda, N. Ohoka, T. Shoda, M. Yorioka, M. Makishima, Y. Sekino, M. Naito, Y. Demizu, M. Kurihara* MedChemComm, 8, 239-246 (2017). doi:10.1039/C6MD00553E
Development of non-secosteroidal vitamin D receptor (VDR) ligands bearing a long alkyl chain
T. Misawa,* Y. Demizu, T. Yachide, N. Ohoka, H. Nojiri, A. Kittaka, M. Makishima, M. Naito, M. Kurihara* Bitamin, 91, 113-120 (2017). doi:10.20632/vso.91.2_113
Development of helix-stabilized cell-penetrating peptides containing cationic α,α-disubstituted amino acids as helical promoters
H. Yamashita, T. Misawa, M. Oba, M. Tanaka, M. Naito, M. Kurihara,* Y. Demizu* Bioorg. Med. Chem., 25, 1846-1851 (2017). doi:10.1016/j.bmc.2017.01.044
Murakami, Y., Ishida, S., Ohta, M., Honma, T., Demizu, Y., Terayama, K., Machine learning-based PROTAC linker design method to enhance cell membrane permeability, PACIFICHEM 2025, Hawaii (2025.12/15-20).
Yokoo, H., Dongrui, Z., Demizu, Y., Design of cell-Permeable peptide-based E3 ligase ligands for development of protein degrader, PACIFICHEM 2025, Hawaii (2025.12/15-20).
Shoda, T., Hashii, N., Harazono, A., Ishii-Watabe, A., Demizu, Y., Development of a fluorescent glycan labeling reagent using excimer fluorescence, PACIFICHEM 2025, Hawaii (2025.12/15-20).
Demizu, Y., Approaches to Protein Lifetime Control via Chemical Degraders, International Symposium on Protein and Organelle Lifetime Regulation Nara (2025.10/30-11/2).
Tsuji, K., Huang, X., Miyamoto, M., Yokoo, H., Kobayakawa, T., Demizu, Y., Tamamura, H., Utilization of HIV-1 Viral Protein R-derived Peptides as Novel E3 Ligase Ligands for Development of BRD4 Degraders, Chemical Biology Symposium 2025, India (2025.2/25).
Fujii, S., Mudiyanselage, H.N.T.N., Misawa, T., Demizu, Y., Hanazono, Y., Ito, N., Kagechika, H., Structural development and crystallographic analysis of diphenylcarborane-based novel vitamin D receptor ligands, The 9th International Symposium on Biomedical Engineering (ISBE2024), Hamamatsu, Japan (2024.12/3-4).
Kikura-Hanajiri, R., Kawamura, M., Mizutani, S., Tanaka, R., Tsuji, G., Misawa, T., Yokoo, H., Demizu, Y., Isomeric analysis of hexahydrocannabinol (HHC), hexahydrocannabihexol (HHCH), and hexahydrocannabiphorol (HHCP) in products using LC-MS and supercritical fluid chromatograph (SFC)-QTOF-MS, The 61st Annual Meeting of TIAFT, Switzerland (2024.9/2-6).
Takada, H., Tsuchiya, K., Demizu, Y., Study on the role of helix-stabilized peptides in transporting antisense morpholino oligomers into cells: relationships among helicity, cellular uptake, and antisense activity, 37th European Peptide Symposium & 14th International Peptide Symposium, Italy (2024.8/25-30).
Hirano, M., Yokoo, H., Oba, M., Misawa, T., Demizu, Y., Development of novel amphipathic stapled peptides as DDS carriers for intracellular delivery of nucleic acids, 37th European Peptide Symposium & 14th International Peptide Symposium, Italy (2024.8/25-30).
Yokoo, H., Dongrui, Z., Demizu, Y., Development of nanoparticle-based protein degradation inducers based on nucleic acid delivery, 37th European Peptide Symposium & 14th International Peptide Symposium, Italy (2024.8/25-30).
Fujita, M., Kikuchi, A., Arita, K., Misawa, T., Demizu, Y., Development of peptide-based inhibitors against β-catenin using in silico approach, 37th European Peptide Symposium & 14th International Peptide Symposium, Italy (2024.8/25-30).
Ito, T., Misawa T., Ohoka N., Aoyama M., Inoue T., Ishii A., Demizu, Y., Strategies for designing hepatocyte-selective carriers using helical peptides as stable scaffolds, 37th European Peptide Symposium & 14th International Peptide Symposium, Italy (2024.8/25-30).
Thilakarathne, N. M. H. N., Misawa, T., Demizu, Y., Hanazono, Y., Ito, N., Kagechika, H., Fujii , S., Structure-activity relationship (SAR) study of hydrophobic moiety of nonsecosteroidal VDR ligands using diphenylsilane scaffold, 21st IUPAB Congress 2024 & 62nd BSJ Joint Congress 2024, Kyoto (2024.6/24-28).
Moriya, S., Demizu, Y., Kurihara, M., Kittaka, A., Sugiyama, T., Strand invasion by PNA containing preQ1, The 50th International Symposium on Nucleic Acids Chemistry, Miyazaki (2023.11).
Ito, T., Misawa, T., Demizu, Y., Development of helical peptide foldamers for tissue-selective carriers, Munich 2023 Symposium on Foldamers, Germany (2023.9/4-6).
Misawa, T., Ito, T., Kato, T., Ohoka, N., Inoue, T., Doi, M., Demizu, Y., Development of helical template peptides for efficient DDS carriers, The 6th Asian Chemical Biology Conference, Korea (2023.8.20-23).
Kikura-Hanajiri, R., Mizutani, S., Kawamura, M., Tanaka, R., Misawa, T., Tsuji, G., Kurohara, T., Ito, M., Demizu, Y., Investigation on the semi-synthetic cannabinoids distributed on the internet in Japan: Reduced forms or acetyl derivatives of tetrahydrocannabinol (THC), X International Conference on Novel Psychoactive Substances, AbuDhabi (2023.11).
Shih, Po-C., Naganuma, M., Tsuji, G., Demizu, Y., Naito, M., Towards development of protein degraders for targeting signal transducer and activator of transcription 3 (STAT3), Ubiquitin New Frontier “from Neo-Biology to Targeted Protein Degradation” Tokyo (2022.12).
Ohoka, N., Suzuki, M., Uchida, T., Tsuji, G., Tsukumo, Y., Yoshida, M., Inoue, T., Demizu, Y., Ohki, H., Naito, M., Development of Gilteritinib-based chimeric small molecules that potently induce degradation of FLT3-ITD protein, Twelfth AACR-JCA Joint Conference on Breakthroughs in Cancer Research: Translating Knowledge into Practice, Hawaii (2022.12).
Demizu, Y., Development of potent PROTACs targeting hematopoietic prostaglandin D synthase via in silico design, The International Symposium in Tokyo, Ubiquitin New Frontier “from Neo-Biology to Targeted Protein Degradation” Tokyo (2022.12).
Osawa, H., Kurohara, T., Murakami, Y., Shibata, N., Naito, M., Demizu, Y., Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase, Ubiquitin New Frontier “from Neo-Biology to Targeted Protein Degradation” Tokyo (2022.12).
Kuriyama, M., Katagiri, K., Yamamoto, K., Demizu, Y., Onomura, O., Metal-free synthesis of phenols from diaryliodonium salts with water catalyzed by N-benzylpyridin-2-one, The 15th International Symposium on Organic Reactions, Taiwan (2022.11).
Nagamuma. M., Ohoka, N., Tsuji, G., Matsuno, K., Naito, M., Inoue, T., Demizu, Y., Development of chimeric molecules that degrade the estrogen receptor using decoy oligonucleotide ligands, The 49th International Symposium on Nucleic Acids Chemistry, Tokyo (2022.11).
Moriya, S., Yonezu, M., Kondo, Y., Demizu, Y., Kurihara, M., Kittaka, A., Sugiyama, T., Synthesis of peptide nucleic acid possessing dicationic cytosine derivative, The 49th International Symposium on Nucleic Acids Chemistry, Tokyo (2022.11).
Kikura-Hanajiri, R., Mizutani, S., Kawamura, M., Tanaka, R., Shoda, T., Demizu, Y., The differentiation of LSD and its 17 related compounds by GC-EI-MS and GC-CI-QTOF-MS, The 30th Meetings of SFTA, the 59th Annual Meeting of TIAFT, France (2022.9).
Fukuhara, K., Mori, K., Okiyama, Y., Misawa, T., Mizuno, M., Demizu, Y., Shibanuma, M., Ohno, A., Rationally designed peptide modulators of amyloid-β toxicity in Alzheimer’s disease, AIMECS2021, Tokyo (Web) (2021.11).
Tsuji, G., Yonemitsu, K., Ito, T., Uema, M., Asakura, H., Demizu, Y., Development of ciclesonide analogues that block SARS-CoV-2 RNA replication, AIMECS2021, Tokyo (Web) (2021.11).
Misawa, T., Ohoka, N., Hirano, M., Oba, M., Inoue, T., Demizu, Y., Development of helix-stabilized hydrophobic/cationic-block peptides for intracellular delivery of biomacromolecules, AIMECS2021, Tokyo (Web) (2021.11).
Yokoo, H., Shibata, N., Endo, A., Ito, T., Yanase, Y., Murakami, Y., Fujii, K., Saeki, Y., Naito, M., Aritake, K., Demizu, Y., Discovery of a highly potent and selective PROTAC targeting hematopoietic prostaglandin D synthase via in silico design, AIMECS2021, Tokyo (Web) (2021.11).
Yamamoto, E., Yokoo, H., Kan-no, H., Tomita, N., Masada, S., Uchiyama, N., Tsuji, G., Hakamatsuka, T., Demizu, Y., Izutsu, K., Goda, Y., Control of N-nitrosodimethylamine (NDMA) in drug substances, The 31st International Symposium on Pharmaceutical and Biomedical Analysis (PBA2021), Kyoto (2021.8).
Abe Y., Yamamoto, E., Yoshida, Masada, S., Yokoo, H., Tsuji, G., Uchiyama, N., Hakamatsuka, T., Demizu, Y., Izutsu, K., Goda, Y., Okuda, H., Temperature-dependent formation of N-nitrosodimethylamine (NDMA) during the storage of ranitidine reagent powders and tablets, AAPS 2020 PHARMSCI 360 , Web (2020.10).
Ohoka, N., Tsuji, G., Shoda, T., Fujisato, T., Kurihara, M., Demizu, Y., Naito, M., Development of small molecule chimeras that recruit aryl-hydrocarbon receptor (AhR) E3 ligase to induce degradation of target proteins, AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, Boston, USA (2019.10).
Tsuji, G., Naganuma, M., Yokoo, H., Misawa, T., Matsuno, K., Demizu, Y., Design and synthesis of 4-(2-pyrrolyl)-4-phenylheptane derivatives as estrogen receptor ligands, 17th Annual Discovery on TARGET, Boston, USA (2019.9).
Misawa, T., Ohoka, N., Goto, C., Oba, M., Tanaka, M., Naito, M., Demizu, Y., Development of amphipathic cell-penetrating foldamers for delivery of biomacromolecules, European Symposium on Organic Chemistry, Austria (2019.7).
Oba, M., Furukawa, K., Nonaka, H., Demizu, Y., Tanaka, M., Development of peptide foldamers changing their secondary structures in response to the environmental milieu, 26th American Peptide Symposium, Monterey, USA (2019.6).
Tsuji, G., Misawa, T., Demizu, Y., Peptide foldamers in drug discovery, 27th French-Japanese Symposium on Medicinal and Fine Chemistry, Fukuoka (2019.5).
Demizu, Y., Goto, C., Misawa, T., Tsuji, G., Peptide foldamers in drug discovery, 26th American Peptide Symposium, Monterey, USA (2019.6).
Eto, R., Oba, M., Ueda, A., Doi, M., Demizu, Y., Kurihara, M., Tanaka, M., Helical secondary structures of peptides composed of cyclic amino acids with a chiral acetal moiety, 10th International Peptide Symposium, Kyoto (2018.12).
Misawa, T., Ohoka, N., Oba, M., Tanaka, M., Naito, M., Demizu, Y., Development of cell-penetrating peptide foldamers for siRNA delivery, 10th International Peptide Symposium, Kyoto (2018.12).
Sugiyama, T., Shibasaki, H., Moriya, S., Kuwata, K., Imamura, Y., Demizu, T., Kurihara, M., Kittaka, T., PNA oligomers possessing PreQ1 as a cationic analogue of guanine, 10th International Peptide Symposium, Kyoto (2018.12).
Demizu, Y., Misawa, T., Tsuji, G., Peptide foldamers in drug discovery, Bordeaux 2018 Symposium on Foldamers, France (2018.9).
Oba, M., Furukawa, K., Toyama, K., Opiyo, G. O., Demizu, T., Kurihara, M., Doi, M., Tanaka, M., Low pH-responsive cyclic α,α-disubstituted α-amino acids for controlling secondary structures of peptide foldamers, Bordeaux 2018 Symposium on Foldamers, France (2018.9).
Misawa, T., Ohoka, N., Oba, M., Tanaka, M., Naito, M., Demizu, Y., Development of helix-stabilized amphipathic cell-penetrating peptides for siRNA delivery, 35th European Peptide Symposium, Ireland (2018.9).
Yamashita, H., Misawa, M., Kurihara, M., Demizu, Y., Development of helical cell penetrating peptides using non-proteinogenic amino acids, Lindau Nobel Laureate Meetings 2017, Germany (2017.6).
足達晴香，上田篤志，井吉彬太，出水庸介，田中正一，Development of α-helical peptides using five-membered α-carbocyclic α,α-disubstituted α-amino acids for side chain cross-linking，第61回ペプチド討論会，名古屋（2024．10/29-31）．
Shun-suke Moriya，Saki Matsumoto，Yosuke Demizu，Masaaki Kurihara，Atsushi Kurihara，Toru Sugiyama，Design and synthesis of a new cytosine derivative for PNA monomer with improved stability and affinity，第61回ペプチド討論会，名古屋（2024．10/29-31）．
宮本真歩，横尾英知，出水庸介，Efficient intracellular delivery of PROTAC using cell-penetrating peptides，第61回ペプチド討論会，名古屋（2024．10/29-31）．（ポスター賞）
武田紗和，横尾英知，出水庸介，Development of peptoid nucleic acids and their structural properties，第61回ペプチド討論会，名古屋（2024．10/29-31）．
横尾英知，周東睿，出水庸介，Development of peptide-based ubiquitin ligase ligands with cell permeability，第61回ペプチド討論会，名古屋（2024．10/29-31）．
村上優貴，石田祥一，出水庸介，寺山慧，De novo PROTAC linker design to enhance cell membrane permeability based on a data-driven method，CBI学会2024年大会，東京（2024．10/28-31）．
N. M. Hansaka N. Thilakarathne，Takashi Misawa，Yosuke Demizu，Nobutoshi Ito，Hiroyuki Kagechika，Shinya Fujii，Structure-activity relationship (SAR) study of hydrophobic moiety of nonsecosteroidal VDR ligands using diphenylsilane scaffold，日本薬学会第144年会，横浜（2024.3/29-31）．
森谷俊介，Mai Kiyosue，出水庸介，栗原正明，橘高敦史，杉山亨，Properties of peptide nucleic acid containing N4-bis(aminomethyl)benzoylated cytosine for enhanced DNA binding，第60回ペプチド討論会，滋賀（2023．11/8-10）．
三澤隆史，伊藤貴仁，加藤巧馬，大岡伸通，井上貴雄，土井光暢，出水庸介，Development of helical template peptides for efficient DDS carrier，第60回ペプチド討論会，滋賀（2023．11/8-10）．
Δ9-THC-O-acetateおよびΔ8-THC-O-acetateのヒト肝臓ミクロゾームによる酵素化学的加水分解とΔ9-THCおよびΔ8-THC生成，Jorge Carlos Pineda Garcia1，趙爽利，李任時，花尻瑠理，出水庸介，田中嘉孝，石井祐次，日本薬学会第143回年会，北海道（2023．3）．
Maeyama, Y., Hosokawa, Y., Hamamura, K., Yokoo, H., Shibata, N., Naito, M., Demizu, Y., Aritake, K.，Specific degrader of hematopoietic prostaglandin D synthase prevented the progression of dilated cardiomyopathy in Duchenne muscular dystrophy，第95回日本薬理学会年会，福岡（2022．3）．
2021
森谷俊介，桑田啓子，Yuki Yoneta, 今村保忠，出水庸介，栗原正明，橘高敦史，杉山亨，PreQ1 facilitates DNA strand invasion by PNA，第58回ペプチド討論会，Web（2021．10）．
横尾英知，大岡伸通，大庭誠，伊藤貴仁，井上貴雄，内藤幹彦，出水庸介，Peptide stapling improves the sustainability of peptide-based degraders against estrogen receptors，第58回ペプチド討論会，Web（2021．10）．
三澤隆史，大岡伸通，大庭誠，田中正一，内藤幹彦，出水庸介，Development of cell-penetrating foldamers for delivery of biomacromolecules，第56回ペプチド討論会，東京（2019．10）．
後藤千尋，平野元春，林克彦，三澤隆史，菊池裕，出水庸介，Development of antimicrobial peptide foldamers based on Magainin 2 sequence，第56回ペプチド討論会，東京（2019．10）．
森谷俊介，Yuko Sasa，桑田啓子，今村保忠，出水庸介，栗原正明，橘高敦史，杉山亨，An approach toward visual detection of single nucleotide polymorphism using pseudocomplementary peptide nucleic acid，第56回ペプチド討論会，東京（2019．10）．
小林寛幸，三澤隆史，大庭誠，田中正一，内藤幹彦，松野研司，出水庸介，Development of cationic cell-penetrating peptides focused on their secondary structures，第54回ペプチド討論会，大阪（2017．11）．
三澤隆史，出水庸介，Development of post functionalizable oligopeptides as helical templates，第54回ペプチド討論会，大阪（2017．11）．
古川かほり，大庭誠，遠山琴美，George Ouma Opiyo，出水庸介，栗原正明，土井光暢，田中正一，Peptide foldamers changing their conformations in response to low pH trigger，第54回ペプチド討論会，大阪（2017．11）．
古場百合恵，池田光生，上田篤志，大庭誠，出水庸介，土井光暢，田中正一，Synthesis of chiral three-membered ring α,α-disubstituted α-amino acid and conformational analysis of its peptides，第54回ペプチド討論会，大阪（2017．11）．
杉山亨，小原美咲，桑田啓子，今村保忠，出水庸介，栗原正明，高野真史，橘高敦史，Peptide nucleic acid possessing PreQ1 as a cationic analogue of guanine，第54回ペプチド討論会，大阪（2017．11）．
