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A novel inositol mono-phosphatase inhibitor from Memnoniella echinata. Producing organism, fermentation, isolation, physicochemical and in vitro biological properties.

作者信息

Lam Y K, Wichmann C F, Meinz M S, Guariglia L, Giacobbe R A, Mochales S, Kong L, Honeycutt S S, Zink D, Bills G F

机构信息

Merck Research Laboratories, Rahway, New Jersey 07065.

出版信息

J Antibiot (Tokyo). 1992 Sep;45(9):1397-403. doi: 10.7164/antibiotics.45.1397.

Abstract

A novel inositol mono-phosphatase inhibitor, L-671,776 (1), was discovered from a culture of the hyphomycete, Memnoniella echinata (ATCC 20928). 1 has a molecular weight of 388 and a molecular formula of C23H32O5. The mode of inhibition is non-competitive, with a Ki of 450 microM. It shows no inhibition of myo-inositol 1,4-bisphosphate 1-phosphatase or myo-inositol 1,4,5-triphosphate 5-phosphatase, although it weakly inhibits myo-inositol 1,4,5-triphosphate 3-kinase (IC50 = 3 mM). It elevates inositol monophosphates in rat parotid slices (EC50 approximately 3 mM), but abolishes agonist effects. It also produces short-lived contraction of guinea pig trachea at 300 microM.

摘要

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