Regulation of stress-induced cytokine production by pyridinylimidazoles; Inhibition of CSBP kinase

被引：210

作者：

Gallagher, TF

Seibel, GL

Kassis, S

Laydon, JT

Blumenthal, MJ

Lee, JC

Lee, D

Boehm, JC

FierThompson, SM

Abt, JW

Soreson, ME

Smietana, JM

Hall, RF

Garigipati, RS

Bender, PE

Erhard, KF

Krog, AJ

Hofmann, GA

Sheldrake, PL

McDonnell, PC

Kumar, S

Young, PR

Adams, JL

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT, DEPT MED CHEM, KING OF PRUSSIA, PA 19406 USA

[2] SMITHKLINE BEECHAM PHARMACEUT, DEPT PHYS & STRUCT CHEM, KING OF PRUSSIA, PA 19406 USA

[3] SMITHKLINE BEECHAM PHARMACEUT, DEPT CELLULAR BIOCHEM, KING OF PRUSSIA, PA 19406 USA

[4] SMITHKLINE BEECHAM PHARMACEUT, DEPT BIOMOL DISCOVERY, KING OF PRUSSIA, PA 19406 USA

[5] SMITHKLINE BEECHAM PHARMACEUT, DEPT CHEM DEV, KING OF PRUSSIA, PA 19406 USA

[6] SMITHKLINE BEECHAM PHARMACEUT, DEPT MOL IMMUNOL, KING OF PRUSSIA, PA 19406 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 01期

关键词：

D O I：

10.1016/S0968-0896(96)00212-X

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：

Members of three classes of pyridinylimidazoles bind with varying affinities to CSBP (p38) kinase which is a member of a stress-induced signal transduction pathway. Based upon SAR and protein homology modeling, the pharmacophore and three potential modes of binding to the enzyme are presented. For a subset of pyridinylimidazoles, binding is shown to correlate with inhibition of CSBP kinase activity, whereas no significant inhibition of PKA, PKC alpha and ERK kinase activity is observed. Copyright (C) 1997 Elsevier Science Ltd.

引用

页码：49 / 64

页数：16

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[21] SYNTHETIC AND MECHANISTIC STUDIES ON THE PREPARATION OF PYRIDYL-SUBSTITUTED IMIDAZOTHIAZOLES [J].