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Discovery of protein phosphatase inhibitor classes by biology-oriented synthesis.


ABSTRACT: Protein phosphatases have very recently emerged as important targets for chemical biology and medicinal chemistry research, and new phosphatase inhibitor classes are in high demand. The underlying frameworks of natural products represent the evolutionarily selected fractions of chemical space explored by nature so far and meet the criteria of relevance to nature and biological prevalidation most crucial to inhibitor development. We refer to synthesis efforts and compound collection development based on these criteria as biology-oriented synthesis. For the discovery of phosphatase inhibitor classes by means of this approach, four natural product-derived or -inspired medium-sized compound collections were synthesized and investigated for inhibition of the tyrosine phosphatases VE-PTP, Shp-2,

SUBMITTER: Noren-Muller A 

PROVIDER: S-EPMC1502279 | biostudies-literature | 2006 Jul

REPOSITORIES: biostudies-literature