Scanning mutagenesis of transmembrane domain 3 of the M1 muscarinic acetylcholine receptor

被引：11

作者：

Hulme, EC ^{[1
]}

Lu, ZL ^{[1
]}

机构：

[1] Natl Inst Med Res, Div Phys Biochem, London NW7 1AA, England

来源：

JOURNAL OF PHYSIOLOGY-PARIS | 1998年 / 92卷 / 3-4期

基金：

英国惠康基金;

关键词：

muscarinic; acetylcholine; G protein; mutagenesis; transmembrane;

D O I：

10.1016/S0928-4257(98)80031-4

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Scanning mutagenesis of transmembrane domain 3 of the M1 muscarinic acetylcholine receptor has revealed a highly-differentiated a-helical structure. Lipid-facing residues are distinguished from a patch of residues which selectively stabilise the ground state of the receptor, and from a band of amino acids extending the full length of the helix, which contribute to the active agonist-receptor-aa protein complex. The most important residues are strongly conserved in the GPCR superfamily. ((C)Elsevier, Paris).

引用

页码：269 / 274

页数：6

共 15 条

[1] An alpha-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors [J].

Baldwin, JM ;

Schertler, GFX ;

Unger, VM .

JOURNAL OF MOLECULAR BIOLOGY, 1997, 272 (01) :144-164

[2] THE PROBABLE ARRANGEMENT OF THE HELICES IN G-PROTEIN-COUPLED RECEPTORS [J].

BALDWIN, JM .

EMBO JOURNAL, 1993, 12 (04) :1693-1703

[3] SOLUBILIZATION AND CHARACTERIZATION OF GUANINE NUCLEOTIDE-SENSITIVE MUSCARINIC AGONIST BINDING-SITES FROM RAT MYOCARDIUM [J].

BERRIE, CP ;

BIRDSALL, NJM ;

HULME, EC ;

KEEN, M ;

STOCKTON, JM .

BRITISH JOURNAL OF PHARMACOLOGY, 1984, 82 (04) :853-861

[4] OPERATIONAL MODELS OF PHARMACOLOGICAL AGONISM [J].

BLACK, JW ;

LEFF, P .

PROCEEDINGS OF THE ROYAL SOCIETY SERIES B-BIOLOGICAL SCIENCES, 1983, 220 (1219) :141-162

[5] A HOT-SPOT OF BINDING-ENERGY IN A HORMONE-RECEPTOR INTERFACE [J].

CLACKSON, T ;

WELLS, JA .

SCIENCE, 1995, 267 (5196) :383-386

[6] Requirement of rigid-body motion of transmembrane helices for light activation of rhodopsin [J].

Farrens, DL ;

Altenbach, C ;

Yang, K ;

Hubbell, WL ;

Khorana, HG .

SCIENCE, 1996, 274 (5288) :768-770

[7] MAPPING THE BINDING-SITE CREVICE OF THE DOPAMINE D2 RECEPTOR BY THE SUBSTITUTED-CYSTEINE ACCESSIBILITY METHOD [J].

JAVITCH, JA ;

FU, DY ;

CHEN, JY ;

KARLIN, A .

NEURON, 1995, 14 (04) :825-831

[8] THE FUNCTION OF A HIGHLY-CONSERVED ARGININE RESIDUE IN ACTIVATION OF THE MUSCARINIC M(1) RECEPTOR [J].

JONES, PG ;

CURTIS, CAM ;

HULME, EC .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1995, 288 (03) :251-257

[9]

KURTENBACH E, 1990, J BIOL CHEM, V265, P13702

[10] The role of the aspartate-arginine-tyrosine triad in the m1 muscarinic receptor: Mutations of aspartate 122 and tyrosine 124 decrease receptor expression but do not abolish signaling [J].

Lu, ZL ;

Curtis, CA ;

Jones, PG ;

Pavia, J ;

Hulme, EC .

MOLECULAR PHARMACOLOGY, 1997, 51 (02) :234-241

← 1 2 →