The synthesis and evaluation of indolylureas as PKCα inhibitors.

Autor: Djung JF; Procter & Gamble Pharmaceuticals Inc., Health Care Research Center, Mason, OH 45040-9462, USA., Mears RJ, Montalbetti CA, Coulter TS, Golebiowski A, Carr AN, Barker O, Greis KD, Zhou S, Dolan E, Davis GF
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2011 Apr 15; Vol. 19 (8), pp. 2742-50. Date of Electronic Publication: 2011 Feb 26.
DOI: 10.1016/j.bmc.2011.02.036
Abstrakt: PKCα and PKA have crucial but opposing roles in the regulation of calcium handling within myocytes. Identification of compounds that inhibit PKCα, but not PKA, are potential therapeutic targets for the treatment of heart disease. The synthesis of indolylureas are described, and a compound displaying nanomolar inhibition towards PKCα with significant selectivity over PKA has been identified.
(Copyright © 2011 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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