The first structure-activity relationship study of oxytocin as a positive allosteric modulator for the µ opioid receptor
T Mizuguchi, K Miyano, R Yamauchi, Y Yoshida… - Peptides, 2023 - Elsevier
Positive allosteric modulators (PAMs) of G protein-coupled receptors (GPCRs) have drawn
attention as novel drug candidates. PAMs can enhance the activities of endogenous …
attention as novel drug candidates. PAMs can enhance the activities of endogenous …
Advancements in stapled peptide drug discovery & development
V Guerlavais, TK Sawyer - Annual Reports in Medicinal Chemistry, 2014 - Elsevier
Stapled peptides are an emerging class of drugs with a unique set of properties that fully
capitalize on 25 years of genetic research to attack drivers of complex diseases, including …
capitalize on 25 years of genetic research to attack drivers of complex diseases, including …
Liquid-phase synthesis of bridged peptides using olefin metathesis of a protected peptide with a long aliphatic chain anchor
K Aihara, C Komiya, A Shigenaga, T Inokuma… - Organic …, 2015 - ACS Publications
Bridged peptides including stapled peptides are attractive tools for regulating protein–
protein interactions (PPIs). An effective synthetic methodology in a heterogeneous system …
protein interactions (PPIs). An effective synthetic methodology in a heterogeneous system …
Peptide-derived mid-sized anti-HIV agents
N Ohashi, H Tamamura - 2016 - books.rsc.org
To date, several anti-human immunodeficiency virus (HIV) drugs such as reverse
transcriptase inhibitors, protease inhibitors and integrase inhibitors have been developed …
transcriptase inhibitors, protease inhibitors and integrase inhibitors have been developed …
Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription
Y Demizu, T Misawa, T Nagakubo, Y Kanda… - Bioorganic & Medicinal …, 2015 - Elsevier
Three types of stabilized helical peptides containing disulfide bonds, C–C cross-linked side
chains, or α, α-disubstituted amino acids (2-aminoisobutyric acid (Aib)) were designed and …
chains, or α, α-disubstituted amino acids (2-aminoisobutyric acid (Aib)) were designed and …
D evelopment of anti‐HIV peptides based on a viral capsid protein
T Mizuguchi, N Ohashi, D Matsumoto… - Peptide …, 2017 - Wiley Online Library
Peptide inhibitors with cell permeability targeting an HIV‐1 capsid (CA) protein might make
therapeutic by regulating HIV‐1 replication. Overlapping fragment peptide libraries covering …
therapeutic by regulating HIV‐1 replication. Overlapping fragment peptide libraries covering …
The hydrocarbon staple & beyond: Recent advances towards stapled peptide therapeutics that target protein-protein interactions
RA Hillman, JW Nadraws… - Current Topics in …, 2018 - ingentaconnect.com
Anomalous protein-protein interactions (PPIs) have been correlated to a variety of disease
states, such as cancer, infectious disease, neurological disorders, diabetes, endocrine …
states, such as cancer, infectious disease, neurological disorders, diabetes, endocrine …
Topological Study of the Structures of Heterochiral Peptides Containing Equal Amounts of l-Leu and d-Leu
Y Demizu, H Yamashita, M Doi, T Misawa… - The Journal of …, 2015 - ACS Publications
We designed and synthesized two dodecapeptides, Boc-(l-Leu-l-Leu-Aib-d-Leu-d-Leu-Aib)
2-OMe (5) and Boc-l-Leu-l-Leu-Aib-(d-Leu-d-Leu-Aib) 2-l-Leu-l-Leu-Aib-OMe (6), that …
2-OMe (5) and Boc-l-Leu-l-Leu-Aib-(d-Leu-d-Leu-Aib) 2-l-Leu-l-Leu-Aib-OMe (6), that …
Stapling monomeric GCN4 peptides allows for DNA binding and enhanced cellular uptake
A Iyer, D Van Lysebetten, YR García… - Organic & …, 2015 - pubs.rsc.org
The basic DNA recognition region of the GCN4 protein comprising 23 amino acids has been
modified to contain two optimally positioned cysteines which have been linked and stapled …
modified to contain two optimally positioned cysteines which have been linked and stapled …
Glycosyl‐templated chiral helix stapling of ethynylpyridine oligomers by alkene metathesis between inter‐pitch side chains
H Abe, F Kayamori, M Inouye - Chemistry–A European Journal, 2015 - Wiley Online Library
Ethynylpyridine polymers and oligomers consisting of 4‐substituted pyridine rings linked by
acetylene bonds at the 2‐and 6‐positions have been investigated. Ethynylpyridine …
acetylene bonds at the 2‐and 6‐positions have been investigated. Ethynylpyridine …