Ligand identification for G-protein-coupled receptors: a lead generation perspective

被引：36

作者：

Bleicher, KH ^{[1
]}

Green, LG ^{[1
]}

Martin, RE ^{[1
]}

Rogers-Evans, M ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, Switzerland

来源：

CURRENT OPINION IN CHEMICAL BIOLOGY | 2004年 / 8卷 / 03期

关键词：

D O I：

10.1016/j.cbpa.2004.04.008

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

This review addresses strategies for the generation of ligands for G-protein-coupled receptors outside classical high-throughput screening and literature based approaches. These range from the chemical intuition-based strategies of endogenous ligand elaboration and privileged structure decoration to the in silico approaches of virtual screening and de novo design. Examples are cited where supporting pharmacological data has been presented.

引用

页码：287 / 296

页数：10

共 50 条

[1] Design of Multivalent Ligand Targeting G-Protein-Coupled Receptors
Liu, Zhili
Zhang, Jing
Zhang, Ao
CURRENT PHARMACEUTICAL DESIGN, 2009, 15 (06) : 682 - 718
[2] Orphan G-protein-coupled receptors and natural ligand discovery
Howard, AD
McAllister, G
Feighner, SD
Liu, QY
Nargund, RP
Van der Ploeg, LHT
Patchett, AA
TRENDS IN PHARMACOLOGICAL SCIENCES, 2001, 22 (03) : 132 - 140
[3] G-protein-coupled receptors
Bergsma, DJ
Wilson, S
BIOFUTUR, 1999, (191) : 26 - 27
[4] Strategies for the identification of allosteric modulators of G-protein-coupled receptors
Burford, Neil T.
Watson, John
Bertekap, Robert
Alt, Andrew
BIOCHEMICAL PHARMACOLOGY, 2011, 81 (06) : 691 - 702
[5] Untangling ligand induced activation and desensitization of G-protein-coupled receptors
Woolf, PJ
Linderman, JJ
BIOPHYSICAL JOURNAL, 2003, 84 (01) : 3 - 13
[6] Dissecting G-protein-coupled receptors: Structure, function, and ligand interaction
Schwalbe, H
Wess, G
CHEMBIOCHEM, 2002, 3 (10) : 915 - 919
[7] Genetic variation in G-protein-coupled receptors - consequences for G-protein-coupled receptors as drug targets
Tang, CM
Insel, PA
EXPERT OPINION ON THERAPEUTIC TARGETS, 2005, 9 (06) : 1247 - 1265
[8] Fragment-based lead discovery on G-protein-coupled receptors
Visegrady, Andras
Keseru, Gyorgy M.
EXPERT OPINION ON DRUG DISCOVERY, 2013, 8 (07) : 811 - 820
[9] Efficacy at g-protein-coupled receptors
Terry Kenakin
Nature Reviews Drug Discovery, 2002, 1 : 103 - 110
[10] G-protein-coupled receptors at a glance
Kroeze, WK
Sheffler, DJ
Roth, BL
JOURNAL OF CELL SCIENCE, 2003, 116 (24) : 4867 - 4869

← 1 2 3 4 5 →