Format

Send to

Choose Destination
Drug Discov Today. 2007 Oct;12(19-20):860-9. Epub 2007 Sep 19.

Panning for SNuRMs: using cofactor profiling for the rational discovery of selective nuclear receptor modulators.

Author information

1
Phenex Pharmaceuticals AG, Gebaeude J542N, Werksgelaende BASF, D-67056 Ludwigshafen, Germany. claus.kremoser@phenex-pharma.com

Abstract

Drugs that target nuclear receptors are clinically, as well as commercially, successful. Their widespread use, however, is limited by an inherent propensity of nuclear receptors to trigger beneficial, as well as adverse, pharmacological effects upon drug activation. Hence, selective drugs that display reduced adverse effects, such as the selective estrogen receptor modulator (SERM) Raloxifene, have been developed by guidance through classical cell culture assays and animal trials. Full agonist and selective modulator nuclear receptor drugs, in general, differ by their ability to recruit certain cofactors to the receptor protein. Hence, systematic cofactor profiling is advancing into an approach for the rationally guided identification of selective NR modulators (SNuRMs) with improved therapeutic ratio.

PMID:
17933688
DOI:
10.1016/j.drudis.2007.07.025
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center