Activation of G Protein Coupled Receptors

被引：68

作者：

Deupi, Xavier ^{[1
]}

Kobilka, Brian ^{[1
]}

机构：

[1] Stanford Univ, Sch Med, Dept Cellular & Mol Physiol, Stanford, CA 94305 USA

来源：

MECHANISMS AND PATHWAYS OF HETEROTRIMERIC G PROTEIN SIGNALING | 2007年 / 74卷

关键词：

D O I：

10.1016/S0065-3231(07)74004-4

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：

G protein-coupled receptors (GPCRs) mediate responses to hormones and neurotransmitters, as well as the senses of sight, smell, and taste. These remarkably versatile signaling molecules respond to structurally diverse ligands. Many GPCRs couple to multiple G protein subtypes, and several have been shown to activate G protein-independent signaling pathways. Drugs acting on GPCRs exhibit efficacy profiles that may differ for different signaling cascades. The functional plasticity exhibited by GPCRs can be attributed to structural flexibility and the existence of multiple ligand-specific conformational states. This chapter will review our current understanding of the mechanism by which agonists bind and activate GPCRs.

引用

页码：137 / 166

页数：30

共 104 条

[1]

Alewijnse AE, 2000, MOL PHARMACOL, V57, P890

[2] Structural features and light-dependent changes in the sequence 306-322 extending from helix VII to the palmitoylation sites in rhodopsin: A site-directed spin-labeling study [J].

Altenbach, C ;

Cai, KW ;

Khorana, HG ;

Hubbell, WL .

BIOCHEMISTRY, 1999, 38 (25) :7931-7937

[3] Structural features and light-dependent changes in the sequence 59-75 connecting helices I and II in rhodopsin: A site-directed spin-labeling study [J].

Altenbach, C ;

Klein-Seetharaman, J ;

Hwa, J ;

Khorana, HG ;

Hubbell, WL .

BIOCHEMISTRY, 1999, 38 (25) :7945-7949

[4] Structure and function in rhodopsin: Mapping light-dependent changes in distance between residue 316 in helix 8 and residues in the sequence 60-75, covering the cytoplasmic end of helices TM1 and TM2 and their connection loop CL1 [J].

Altenbach, C ;

Klein-Seetharaman, J ;

Cai, KW ;

Khorana, HG ;

Hubbell, WL .

BIOCHEMISTRY, 2001, 40 (51) :15493-15500

[5]

ALTENBACH C, 2001, BIOCHEMISTRY-US, V38, P7945

[6] Dimerization: An emerging concept for G protein-coupled receptor ontogeny and function [J].

Angers, S ;

Salahpour, A ;

Bouvier, M .

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, 2002, 42 :409-435

[7] Rhodopsin crystal: new template yielding realistic models of G-protein-coupled receptors? [J].

Archer, E ;

Maigret, B ;

Escrieut, C ;

Pradayrol, L ;

Fourmy, D .

TRENDS IN PHARMACOLOGICAL SCIENCES, 2003, 24 (01) :36-40

[8]

ARNIS S, 1994, J BIOL CHEM, V269, P23879

[9] FINGERPRINTING G-PROTEIN-COUPLED RECEPTORS [J].

ATTWOOD, TK ;

FINDLAY, JBC .

PROTEIN ENGINEERING, 1994, 7 (02) :195-203

[10] β-Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors [J].

Azzi, M ;

Charest, PG ;

Angers, S ;

Rousseau, G ;

Kohout, T ;

Bouvier, M ;

Piñeyro, G .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2003, 100 (20) :11406-11411

← 1 2 3 4 5 6 7 8 9 10 →