Identification of ligands for the orphan nuclear receptor GCNF

被引：0

作者：

Buijsman, R

Garritsen, A

Gossen, J

Klomp, J

Kuil, C

van Noort, P

van Rijn, R

Rovers, G

Schoonen, W

Sterrenburg, JG

Stock, T

Verdonk, G

Visser, A

van Boeckel, S

Dijkema, R

Hermkens, P

机构：

[1] NV Organon, Lead Discovery, NL-5340 BH Oss, Netherlands

[2] NV Organon, Target Discovery, NL-5340 BH Oss, Netherlands

[3] NV Organon, Mol Design & Informat, NL-5340 BH Oss, Netherlands

[4] NV Organon, Pharmacol, NL-5340 BH Oss, Netherlands

来源：

MEDICINAL CHEMISTRY RESEARCH | 2004年 / 13卷 / 3-4期

关键词：

Nuclear Receptor; Orphan Nuclear Receptor; Orphan Nuclear;

D O I：

10.1007/s00044-004-0027-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

HTS has been executed with a luciferase reporter assay in CHO cells stably expressing an ERa/GCNF chimer. Confirmed hits could be optimized some 10 to 100 fold. Partial agonists identified during the hit optimization process behaved as antagonists in a competition based variant of the reporter assay. The latter assay format was also used to identify some full antagonists by HTS. GCNF binding of agonists and antagonists was confirmed by GCNF/cofactor interactions studies in solution.

引用

页码：210 / 215

页数：6

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