Lysophosphatidic acid receptor agonists and antagonists (WO2010051053)

被引：4

作者：

Parrill, Abby L. ^{[1
]}

机构：

[1] Univ Memphis, Dept Chem, Memphis, TN 38152 USA

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2011年 / 21卷 / 02期

关键词：

cancer; chemoprotection; LPA(2) receptor; lysophosphatidic acid; radioprotection; FATTY ALCOHOL PHOSPHATES; DNA POLYMERASE-ALPHA; BIOLOGICAL EVALUATION; PHOSPHONATE ANALOGS; CELL-PROLIFERATION; SIGNALING PATHWAYS; LPA RECEPTORS; CANCER; PROGRESSION; INHIBITION;

D O I：

10.1517/13543776.2011.539206

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Lysophosphatidic acid (LPA) is a bioactive lipid involved in signaling pathways that result in cell survival, proliferation, migration and invasion. These cellular responses are a critical element of both normal development as well as pathophysiology. In particular, dysregulated LPA production and function have been linked with cancer and cardiovascular disease. RxBio, Inc. has generated several series of LPA analogs with varied agonist/antagonist function at the LPA(1-3) GPCR targets of LPA signaling. These analogs are simplified relative to LPA through deletion of the glycerol moiety linking the LPA phosphate and fatty acid groups. One of the example compounds was shown to protect intestinal crypt cells from radiation-induced apoptosis in mice when whole body irradiation occurred 2 h after oral dosing.

引用

页码：281 / 286

页数：6

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