4.5 Article

The selective inhibition of phosphatases by natural toxins: The anhydride domain of tautomycin is not a primary factor in controlling PP1/PP2A selectivity

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 13, Issue 9, Pages 1597-1600

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(03)00105-7

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Funding

  1. NIGMS NIH HHS [R01 GM057550] Funding Source: Medline
  2. NINDS NIH HHS [NS 57550] Funding Source: Medline

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Analogues of the potent and moderately selective PP1/PP2A inhibitor tautomycin (TM) were prepared with modifications in the C1'-C7' anhydride moiety. While all retain varying degrees of activity within a 3000-fold range of potencies, they also show remarkable constancy in their IC50 ratios, suggesting that the anhydride moiety is not critical in controlling the selectivity of inhibition. (C) 2003 Elsevier Science Ltd. All rights reserved.

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