Histidine and homohistidine derivatives as inhibitors of protein
申请人:Warner-Lambert Company
公开号:US05571792A1
公开(公告)日:1996-11-05
Novel inhibitors of protein farnesyltransferase enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer and restenosis.
A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice
作者:Joseph Pontillo、Joseph A. Tran、Stacy Markison、Margaret Joppa、Beth A. Fleck、Dragan Marinkovic、Melissa Arellano、Fabio C. Tucci、Marion Lanier、Jodie Nelson、John Saunders、Sam R.J. Hoare、Alan C. Foster、Chen Chen
DOI:10.1016/j.bmcl.2005.03.053
日期:2005.5
Optimization on a series of piperazinebenzylamines resulted in analogues with low nanomolar binding at the human MC4 receptor but weak affinity (K-i > 500 nM) at the MC3 receptor. Compound 14c was identified to be a potent MC4R antagonist (K-i = 3.2 nM) with a selectivity of 240-fold over MC3R. It proved to be an insurmountable antagonist in a cAMP assay. Compound 14c potently stimulated food intake in satiated mice when given by intracerebroventricular administration. (c) 2005 Elsevier Ltd. All rights reserved.
[EN] HISTIDINE-SELECTIVE POLYMER REAGENTS<br/>[FR] RÉACTIFS POLYMÈRES SÉLECTIFS À L'HISTIDINE
申请人:[en]NEKTAR THERAPEUTICS
公开号:WO2022266498A1
公开(公告)日:2022-12-22
The instant disclosure provides (among other things) novel water-soluble polymer reagents capable of selective conjugation to histidine residues, e.g., in peptides and proteins, as well the resulting conjugates and related compositions. In addition, provided are methods of preparing the polymer reagents, as well as methods for conjugating the polymer reagents to active agents and other substances, pharmaceutical compositions, and methods for administering the conjugates.
Nishiyama, Yasuhiro; Shintomi, Noriyuki; Kondo, Yukihiro, Journal of the Chemical Society. Perkin transactions I, 1995, # 18, p. 2309 - 2314