FCCC LOGO Faculty Publications
Chernoff Jonathan , Peterson Jeffrey R
Methods for screening for inhibitors of autoinhibited proteins
. 2006 09/05/2006 :48 pp
PMID: AN 2006:236813   
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Abstract
Methods for obtaining highly target-specific inhibitory compds. are disclosed. These inhibitory compds. provide for the preservation of a native, non-activated form of an autoinhibited mol., such as a protein or enzyme. The inhibitory compds. are further described as essentially free of inhibitory activity for non-native forms of an autoinhibited mol. of interest. By way of example, such autoinhibited mols. of interest include proteins and enzymes, such as the p-21-activated kinases (Paks) and the Rho-activated proteins. The inhibitory compds. act by binding to a distinct, autoinhibitory domain of an autoinhibited mol. (protein), and thereby stabilize an autoinhibited conformation of the mol. (protein). Prepns., including pharmaceutical prepns., compromising a compn. enriched for the inhibitory compds. are also disclosed. [on SciFinder (R)]
Notes
CAN 144:286146 1-1 Pharmacology Patent written in English. 20060316 153190-46-6 (MLK3 kinase); 161384-20-9 (Protein kinase D); 177893-51-5; 192140-83-3 (Pak2 kinase); 372092-80-3 (Protein kinase) Role: BSU (Biological study, unclassified), BIOL (Biological study) (methods for screening for inhibitors of autoinhibited proteins) A2 US 2004-608105 20040909