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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Recent Advances in the Discovery of Protein Kinase C Modulators Based on the Structures of Natural Protein Kinase C Activators

Author(s): Dawei Ma

Volume 8, Issue 2, 2001

Page: [191 - 202] Pages: 12

DOI: 10.2174/0929867013373868

Price: $65

Abstract

The natural products teleocidins, phorbol esters, asplysiatoxin, ingenol esters, and bryostatins are all potent protein kinase C (PKC) activators. The fact that they act at the same site of PKC implied that these structurally diverse molecules might contain the common structural elements. Several pharmacophores for these compounds have been proposed based on the molecular modeling studied and experimental results. In order to prove these hypotheses various simplified analogues of these compounds are designed, synthesized, and evaluated as new PKC activators. Some of the simplified analogues demonstrated much high potency to activate PKC, which not only gives some insights how these PKC activators bind with PKC, but also provides the new leads to develop the therapeutic tools to treat the diseases related by PKC.


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