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Literature summary for 2.4.1.17 extracted from

  • Tripathi, S.P.; Bhadauriya, A.; Patil, A.; Sangamwar, A.T.
    Substrate selectivity of human intestinal UDP-glucuronosyltransferases (UGTs): in silico and in vitro insights (2013), Drug Metab. Rev., 45, 231-252.
    View publication on PubMed

Application

Application Comment Organism
drug development drug development process aims to produce safe, effective drugs within a reasonable time and at a reasonable cost. Phase II metabolism (glucuronidation) can affect drug action and pharmacokinetics to a considerable extent. Extensive glucuronidation is an obstacle to oral bioavailability because the first-pass glucuronidation or premature clearance by UDP-glucuronosyltransferases of orally administered agents frequently results in poor oral bioavailability and lack of efficacy. Modeling of chemical entities/drugs for UGTs and their kinetic data can be useful in understanding the binding patterns to be used in the design of better molecules, analysis of first-pass glucuronidation by intestinal UGTs, including their topology, expression profile, and pharmacogenomics, and substrate selectivity at the binding pocket, structural requirements, and mechanism of enzyme actions, detailed overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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-
-

Source Tissue

Source Tissue Comment Organism Textmining
intestine
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Homo sapiens
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Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
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Homo sapiens
UGT
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Homo sapiens