Structure-activity relationship of cantharidin derivatives to protein phosphatases 1, 2A1, and 2B

DOI: 10.1016/S0960-894X(97)00316-8

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1833 - 1836 (1997)

Update date:2022-07-29

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Authors:

Sodeoka, Mikiko

Baba, Yoshiyasu

Kobayashi, Satoko

Hirukawa, Nozomu

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Article abstract of DOI:10.1016/S0960-894X(97)00316-8

The effects of structural modification of cantharidin on the inhibition of protein Ser/Thr phosphatases are described. Removal of the methyl substituents at C2 and C3 in cantharidin improved the inhibition of PP2B. In contrast, introduction of a substituent to C1/C4-position drastically decreased inhibition of PP1 and PP2A₁. PP2B was found to be quite tolerant to modifications at the C5 position.

Full text of DOI:10.1016/S0960-894X(97)00316-8

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