Literature DB >> 16787376

Pharmacophore identification: the case of the ser/thr protein phosphatase inhibitors.

David A Colby1, A Richard Chamberlin.   

Abstract

This review provides a chronological account of the identification and refinement of the pharmacophore for inhibition of two key serine/threonine protein phosphatases, PP1 and PP2A. The dramatic impact of natural product isolation, molecular modeling, analogue design, biochemical studies, and crystallography on the evolution of the pharmacophore will be described.

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Year:  2006        PMID： 16787376     DOI： 10.2174/138955706777435715

Source DB:  PubMed          Journal:  Mini Rev Med Chem        ISSN： 1389-5575            Impact factor:   3.862


  3 in total

1.  Total synthesis and evaluation of cytostatin, its C10-C11 diastereomers, and additional key analogues: impact on PP2A inhibition.

Authors:  Brian G Lawhorn; Sobhana B Boga; Scott E Wolkenberg; David A Colby; Carla-Maria Gauss; Mark R Swingle; Lauren Amable; Richard E Honkanen; Dale L Boger
Journal:  J Am Chem Soc       Date:  2006-12-27       Impact factor: 15.419

2.  Structure-activity relationship studies of fostriecin, cytostatin, and key analogs, with PP1, PP2A, PP5, and( beta12-beta13)-chimeras (PP1/PP2A and PP5/PP2A), provide further insight into the inhibitory actions of fostriecin family inhibitors.

Authors:  Mark R Swingle; Lauren Amable; Brian G Lawhorn; Suzanne B Buck; Christopher P Burke; Pukar Ratti; Kimberly L Fischer; Dale L Boger; Richard E Honkanen
Journal:  J Pharmacol Exp Ther       Date:  2009-07-10       Impact factor: 4.030

3.  Selectivity and potency of microcystin congeners against OATP1B1 and OATP1B3 expressing cancer cells.

Authors:  Timo H J Niedermeyer; Abigail Daily; Monika Swiatecka-Hagenbruch; Jeffrey A Moscow
Journal:  PLoS One       Date:  2014-03-10       Impact factor: 3.240
  3 in total

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