'Irreversible' slow-onset inhibition of orotate phosphoribosyltransferase by an amidrazone phosphate transition-state mimic

Autor:	Chelsea K. Thornburg, Ronald W. McClard, John F. Witte, Kathryn E. Bray
Rok vydání:	2006
Předmět:	Orotate Phosphoribosyltransferase Clinical Biochemistry Pharmaceutical Science Saccharomyces cerevisiae Biochemistry Chemical synthesis chemistry.chemical_compound Drug Discovery Glycosyltransferase Enzyme Inhibitors Molecular Biology chemistry.chemical_classification biology Transition (genetics) Molecular Structure Organic Chemistry Molecular Mimicry Phosphate Yeast Enzyme Activation Enzyme chemistry biology.protein Molecular Medicine Phosphoribosyltransferase Orotate phosphoribosyltransferase Pyrimidine Nucleotides
Zdroj:	Bioorganicmedicinal chemistry letters. 16(23)
ISSN:	0960-894X
Popis:	A mimic of the putative transition-state intermediate has been synthesized and found to be a very slow-onset inhibitor of yeast orotate phosphoribosyltransferase. The mechanism of inhibition may involve a rate-determining isomerization of the enzyme to a form receptive to the inhibitor, which then remains tightly bound.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6216e72da59a8cc9eac6a9c44050976 https://pubmed.ncbi.nlm.nih.gov/16979338 Zobrazit plný text záznamu Full Text from ScienceDirect