Molecular pharmacology of histamine H4 receptors

被引：11

作者：

Nijmeijer, Saskia ^{[1
]}

de Graaf, Chris ^{[1
]}

Leurs, Rob ^{[1
]}

Vischer, Henry F. ^{[1
]}

机构：

[1] Vrije Univ Amsterdam, Amsterdam Ctr Drug Res, NL-1081 HV Amsterdam, Netherlands

来源：

FRONTIERS IN BIOSCIENCE-LANDMARK | 2012年 / 17卷

关键词：

Histamine H4 receptor; Histamine; GPCR; Inflammation; Dimerization; Review; PROTEIN-COUPLED RECEPTORS; 2ND EXTRACELLULAR LOOP; H-4; RECEPTOR; CONSTITUTIVE ACTIVITY; HUMAN EOSINOPHILS; INVERSE AGONISM; BINDING-SITE; FUNCTIONAL EXPRESSION; MEDIATES CHEMOTAXIS; LIGAND-BINDING;

D O I：

10.2741/4039

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：

The histamine H-4 receptor (H4R) is the youngest member of the histamine receptor family. Based on its predominant expression pattern in hematopoietic cells, the H4R is considered to be an interesting drug target for inflammatory disorders such as allergy and asthma. Since the identification and cloning of the H4R in 2000, drug discovery programs boosted the development of various H4R (specific) ligands. Differences between H4R orthologs in combination with available three-dimensional G protein-coupled receptor (GPCR) models have guided site-directed mutagenesis studies to gain insight in ligand binding and receptor activation. In addition, ongoing characterization of H4R-mediated signaling in transfected and native cells contributes to further unravel the (patho-) physiological functions of H(4)Rs.

引用

页码：2089 / 2106

页数：18

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