Literature DB >> 12375882

The inhibition of protein phosphatases 1 and 2A: a new target for rational anti-cancer drug design?

A McCluskey1, S P Ackland, E Gardiner, C C Walkom, J A Sakoff.   

Abstract

Recent investigations in our laboratories have highlighted that the inhibition of the serine/threonine protein phosphatases 1 and 2A (PP1 and PP2A) is an excellent target for the development of novel anti-cancer agents. Using a combination of the known crystal structure of PP1 and the modelled structure of PP2A, we have rationally designed a new class of protein phosphatase inhibitors, cantharimides, which exhibit broad-spectrum anti-cancer activity. Synthetic modifications of the simplest known PP1 and PP2A inhibitor, norcantharidin, has led to the development of potent PP1 and PP2A inhibitors.

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Year:  2001        PMID: 12375882

Source DB:  PubMed          Journal:  Anticancer Drug Des        ISSN: 0266-9536


  5 in total

Review 1.  Antitumor potential of the protein phosphatase inhibitor, cantharidin, and selected derivatives.

Authors:  Yulin Ren; A Douglas Kinghorn
Journal:  Bioorg Med Chem       Date:  2021-01-09       Impact factor: 3.641

2.  Antimetastatic effects of norcantharidin on hepatocellular carcinoma by transcriptional inhibition of MMP-9 through modulation of NF-kB activity.

Authors:  Chao-Bin Yeh; Ming-Ju Hsieh; Yi-Hsien Hsieh; Ming-Hsien Chien; Hui-Ling Chiou; Shun-Fa Yang
Journal:  PLoS One       Date:  2012-02-07       Impact factor: 3.240

3.  Precise cloning and tandem integration of large polyketide biosynthetic gene cluster using Streptomyces artificial chromosome system.

Authors:  Hee-Ju Nah; Min-Woo Woo; Si-Sun Choi; Eung-Soo Kim
Journal:  Microb Cell Fact       Date:  2015-09-16       Impact factor: 5.328

4.  Molecular biology of cantharidin in cancer cells.

Authors:  Rolf Rauh; Stefan Kahl; Herbert Boechzelt; Rudolf Bauer; Bernd Kaina; Thomas Efferth
Journal:  Chin Med       Date:  2007-07-04       Impact factor: 5.455

5.  Integrative genomic and transcriptomic analysis identified candidate genes implicated in the pathogenesis of hepatosplenic T-cell lymphoma.

Authors:  Julio Finalet Ferreiro; Leila Rouhigharabaei; Helena Urbankova; Jo-Anne van der Krogt; Lucienne Michaux; Shashirekha Shetty; Laszlo Krenacs; Thomas Tousseyn; Pascale De Paepe; Anne Uyttebroeck; Gregor Verhoef; Tom Taghon; Peter Vandenberghe; Jan Cools; Iwona Wlodarska
Journal:  PLoS One       Date:  2014-07-24       Impact factor: 3.240

  5 in total

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