Literature DB >> 15816047

Structure-activity relationships of inverse agonists for G-protein-coupled receptors.

Willem Soudijn1, Ineke van Wijngaarden, Adriaan P Ijzerman.   

Abstract

It has been recently established that G-protein-coupled receptors (GPCRs) can be constitutively active, i.e., they can be active in the absence of an agonist. This activity can be inhibited by so-called inverse agonists. For a number of GPCRs, such inverse agonists have been developed and studied, now enabling for the first time a study into their structure-activity relationships. Copyright 2005 Wiley Periodicals, Inc.

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Year:  2005        PMID: 15816047     DOI: 10.1002/med.20031

Source DB:  PubMed          Journal:  Med Res Rev        ISSN: 0198-6325            Impact factor:   12.944


  9 in total

1.  Ligands raise the constraint that limits constitutive activation in G protein-coupled opioid receptors.

Authors:  Vanessa Vezzi; H Ongun Onaran; Paola Molinari; Remo Guerrini; Gianfranco Balboni; Girolamo Calò; Tommaso Costa
Journal:  J Biol Chem       Date:  2013-07-08       Impact factor: 5.157

2.  Abilities of candesartan and other AT(1) receptor blockers to impair angiotensin II-induced AT(1) receptor activation after wash-out.

Authors:  Yoshihiro Kiya; Shin-ichiro Miura; Yoshino Matsuo; Sadashiva S Karnik; Keijiro Saku
Journal:  J Renin Angiotensin Aldosterone Syst       Date:  2011-08-08       Impact factor: 1.636

3.  A small difference in the molecular structure of angiotensin II receptor blockers induces AT₁ receptor-dependent and -independent beneficial effects.

Authors:  Masahiro Fujino; Shin-ichiro Miura; Yoshihiro Kiya; Yukio Tominaga; Yoshino Matsuo; Sadashiva S Karnik; Keijiro Saku
Journal:  Hypertens Res       Date:  2010-07-29       Impact factor: 3.872

4.  Unique binding behavior of the recently approved angiotensin II receptor blocker azilsartan compared with that of candesartan.

Authors:  Shin-ichiro Miura; Atsutoshi Okabe; Yoshino Matsuo; Sadashiva S Karnik; Keijiro Saku
Journal:  Hypertens Res       Date:  2012-10-04       Impact factor: 3.872

5.  Small molecules with similar structures exhibit agonist, neutral antagonist or inverse agonist activity toward angiotensin II type 1 receptor.

Authors:  Shin-ichiro Miura; Yoshihiro Kiya; Hiroyuki Hanzawa; Naoki Nakao; Masahiro Fujino; Satoshi Imaizumi; Yoshino Matsuo; Hiroaki Yanagisawa; Hiroyuki Koike; Issei Komuro; Sadashiva S Karnik; Keijiro Saku
Journal:  PLoS One       Date:  2012-06-14       Impact factor: 3.240

6.  A novel chemokine receptor for SDF-1 and I-TAC involved in cell survival, cell adhesion, and tumor development.

Authors:  Jennifer M Burns; Bretton C Summers; Yu Wang; Anita Melikian; Rob Berahovich; Zhenhua Miao; Mark E T Penfold; Mary Jean Sunshine; Dan R Littman; Calvin J Kuo; Kevin Wei; Brian E McMaster; Kim Wright; Maureen C Howard; Thomas J Schall
Journal:  J Exp Med       Date:  2006-08-28       Impact factor: 14.307

7.  Crystal structure of human endothelin ETB receptor in complex with peptide inverse agonist IRL2500.

Authors:  Chisae Nagiri; Wataru Shihoya; Asuka Inoue; Francois Marie Ngako Kadji; Junken Aoki; Osamu Nureki
Journal:  Commun Biol       Date:  2019-06-21

8.  Molecular mechanism of agonism and inverse agonism in ghrelin receptor.

Authors:  Jiao Qin; Ye Cai; Zheng Xu; Qianqian Ming; Su-Yu Ji; Chao Wu; Huibing Zhang; Chunyou Mao; Dan-Dan Shen; Kunio Hirata; Yanbin Ma; Wei Yan; Yan Zhang; Zhenhua Shao
Journal:  Nat Commun       Date:  2022-01-13       Impact factor: 17.694

9.  Suppression of osteoclastogenesis via α2-adrenergic receptors.

Authors:  Kosuke Hamajima; Kazunori Hamamura; Andy Chen; Hiroki Yokota; Hironori Mori; Shoyoku Yo; Hisataka Kondo; Kenjiro Tanaka; Kyoko Ishizuka; Daisuke Kodama; Takao Hirai; Ken Miyazawa; Shigemi Goto; Akifumi Togari
Journal:  Biomed Rep       Date:  2018-03-09
  9 in total

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