Structural features of subtype-selective EP receptor modulators

被引：130

作者：

Markovic, Tijana ^{[1
]}

Jakopin, Ziga ^{[1
]}

Dolenc, Marija Sollner ^{[1
]}

Mlinaric-Rascan, Irena ^{[1
]}

机构：

[1] Univ Ljubljana, Fac Pharm, Askerceva Cesta 7, Ljubljana 1000, Slovenia

来源：

DRUG DISCOVERY TODAY | 2017年 / 22卷 / 01期

关键词：

PROSTANOID RECEPTORS; PROSTAGLANDIN E-2; ACYLSULFONAMIDE ANALOGS; EP4-RECEPTOR AGONIST; INTERNATIONAL UNION; HIGHLY POTENT; ACID ANALOGS; PART; DISCOVERY; ANTAGONIST;

D O I：

10.1016/j.drudis.2016.08.003

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Prostaglandin E2 is a potent endogenous molecule that binds to four different G-protein-coupled receptors: EP1-4. Each of these receptors is a valuable drug target, with distinct tissue localisation and signalling pathways. We review the structural features of EP modulators required for subtype-selective activity, as well as the structural requirements for improved pharmacokinetic parameters. Novel EP receptor subtype selective agonists and antagonists appear to be valuable drug candidates in the therapy of many pathophysiological states, including ulcerative colitis, glaucoma, bone healing, B cell lymphoma, neurological diseases, among others, which have been studied in vitro, in vivo and in early phase clinical trials.

引用

页码：57 / 71

页数：15

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