A NOVEL INOSITOL MONO-PHOSPHATASE INHIBITOR FROM Memnoniella echinata

Autor:	Maria S. Meinz, Richard W. Burg, Gerald F. Bills, G G Reid, L. Guariglia, C I Ragan, Robert A. Giacobbe, Yiu-Kuen T. Lam, Susan S. Honeycutt, R G Jackson, Sagrario Mochales, Richard L. Monaghan, J. J. Maguire, D. L. Zink, L. Huang, Li Kong, A. T. Mcknight, Carol F. Wichmann
Rok vydání:	1992
Předmět:	Pharmacology chemistry.chemical_classification Agonist biology medicine.drug_class Biological activity In vitro Guinea pig chemistry.chemical_compound Enzyme chemistry Biochemistry Enzyme inhibitor Drug Discovery biology.protein medicine Inositol IC50
Zdroj:	The Journal of Antibiotics. 45:1397-1402
ISSN:	1881-1469 0021-8820
DOI:	10.7164/antibiotics.45.1397
Popis:	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 450μM. 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 μM.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::cfd8d3e396f266f7677f61e6631dd314 https://doi.org/10.7164/antibiotics.45.1397 Zobrazit plný text záznamu