FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2017011289> ?p ?o ?g. }

• W2017011289 endingPage "12676" @default.
• W2017011289 startingPage "12671" @default.
• W2017011289 abstract "Indinavir is a viral protease inhibitor used for the treatment of HIV infection. Unconjugated hyperbilirubinemia develops in up to 25% of patients receiving indinavir, prompting drug discontinuation and further clinical evaluation in some instances. We postulated that this side-effect is due to indinavir-mediated impairment of bilirubin UDP-glucuronosyltransferase (UGT) activity and would be most pronounced in individuals with reduced hepatic enzyme levels, as occurs in approximately 10% of the population manifesting Gilbert's syndrome. This hypothesis was tested in vitro, in the Gunn rat model of UGT deficiency, and in HIV-infected patients with and without the Gilbert's polymorphism. Indinavir was found to competitively inhibit UGT enzymatic activity (K(I) = 183 microM) while concomitantly inducing hepatic bilirubin UGT mRNA and protein expression. Although oral indinavir increased plasma bilirubin levels in wild-type and heterozygous Gunn rats, the mean rise was significantly greater in the latter group of animals. Similarly, serum bilirubin increased by a mean of 0.34 mg/dl in indinavir-treated HIV patients lacking the Gilbert's polymorphism versus 1.45 mg/dl in those who were either heterozygous or homozygous for the mutant allele. Whereas saquinavir also competitively inhibits UGT activity, this drug has not been associated with hyperbilirubinemia, most likely because of the higher K(I) (360 microM) and substantially lower therapeutic levels as compared with indinavir. Taken together, these findings indicate that elevations in serum-unconjugated bilirubin associated with indinavir treatment result from direct inhibition of bilirubin-conjugating activity." @default.
• W2017011289 created "2016-06-24" @default.
• W2017011289 creator A5002199816 @default.
• W2017011289 creator A5023499969 @default.
• W2017011289 creator A5036658494 @default.
• W2017011289 creator A5045657344 @default.
• W2017011289 creator A5052947786 @default.
• W2017011289 creator A5055495178 @default.
• W2017011289 creator A5081134645 @default.
• W2017011289 creator A5084104464 @default.
• W2017011289 date "2001-10-16" @default.
• W2017011289 modified "2023-10-16" @default.
• W2017011289 title "Mechanism of indinavir-induced hyperbilirubinemia" @default.
• W2017011289 cites W101745106 @default.
• W2017011289 cites W1480849379 @default.
• W2017011289 cites W1522241387 @default.
• W2017011289 cites W1532495168 @default.
• W2017011289 cites W1559057202 @default.
• W2017011289 cites W1594166164 @default.
• W2017011289 cites W1601463908 @default.
• W2017011289 cites W1774961775 @default.
• W2017011289 cites W1775799483 @default.
• W2017011289 cites W1899310373 @default.
• W2017011289 cites W1974224443 @default.
• W2017011289 cites W1991736137 @default.
• W2017011289 cites W2022190511 @default.
• W2017011289 cites W2042231584 @default.
• W2017011289 cites W2055681603 @default.
• W2017011289 cites W2057581357 @default.
• W2017011289 cites W2077039378 @default.
• W2017011289 cites W2078326422 @default.
• W2017011289 cites W2088643442 @default.
• W2017011289 cites W2089720722 @default.
• W2017011289 cites W2093977227 @default.
• W2017011289 cites W2107262592 @default.
• W2017011289 cites W2109899602 @default.
• W2017011289 cites W2120129846 @default.
• W2017011289 cites W2132804094 @default.
• W2017011289 cites W2165781594 @default.
• W2017011289 cites W2322536880 @default.
• W2017011289 cites W2329393410 @default.
• W2017011289 cites W2339219218 @default.
• W2017011289 cites W2401391346 @default.
• W2017011289 cites W2412604103 @default.
• W2017011289 cites W4235712548 @default.
• W2017011289 cites W4294293047 @default.
• W2017011289 doi "https://doi.org/10.1073/pnas.231140698" @default.
• W2017011289 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/60112" @default.
• W2017011289 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11606755" @default.
• W2017011289 hasPublicationYear "2001" @default.
• W2017011289 type Work @default.
• W2017011289 sameAs 2017011289 @default.
• W2017011289 citedByCount "228" @default.
• W2017011289 countsByYear W20170112892012 @default.
• W2017011289 countsByYear W20170112892013 @default.
• W2017011289 countsByYear W20170112892014 @default.
• W2017011289 countsByYear W20170112892015 @default.
• W2017011289 countsByYear W20170112892016 @default.
• W2017011289 countsByYear W20170112892017 @default.
• W2017011289 countsByYear W20170112892018 @default.
• W2017011289 countsByYear W20170112892019 @default.
• W2017011289 countsByYear W20170112892020 @default.
• W2017011289 countsByYear W20170112892021 @default.
• W2017011289 countsByYear W20170112892022 @default.
• W2017011289 countsByYear W20170112892023 @default.
• W2017011289 crossrefType "journal-article" @default.
• W2017011289 hasAuthorship W2017011289A5002199816 @default.
• W2017011289 hasAuthorship W2017011289A5023499969 @default.
• W2017011289 hasAuthorship W2017011289A5036658494 @default.
• W2017011289 hasAuthorship W2017011289A5045657344 @default.
• W2017011289 hasAuthorship W2017011289A5052947786 @default.
• W2017011289 hasAuthorship W2017011289A5055495178 @default.
• W2017011289 hasAuthorship W2017011289A5081134645 @default.
• W2017011289 hasAuthorship W2017011289A5084104464 @default.
• W2017011289 hasBestOaLocation W20170112892 @default.
• W2017011289 hasConcept C126322002 @default.
• W2017011289 hasConcept C134018914 @default.
• W2017011289 hasConcept C181199279 @default.
• W2017011289 hasConcept C185592680 @default.
• W2017011289 hasConcept C203014093 @default.
• W2017011289 hasConcept C2776365762 @default.
• W2017011289 hasConcept C2776452011 @default.
• W2017011289 hasConcept C2777210460 @default.
• W2017011289 hasConcept C2777513400 @default.
• W2017011289 hasConcept C2780727368 @default.
• W2017011289 hasConcept C2781278898 @default.
• W2017011289 hasConcept C2911188197 @default.
• W2017011289 hasConcept C3013748606 @default.
• W2017011289 hasConcept C55493867 @default.
• W2017011289 hasConcept C71924100 @default.
• W2017011289 hasConcept C86803240 @default.
• W2017011289 hasConcept C87644729 @default.
• W2017011289 hasConceptScore W2017011289C126322002 @default.
• W2017011289 hasConceptScore W2017011289C134018914 @default.
• W2017011289 hasConceptScore W2017011289C181199279 @default.
• W2017011289 hasConceptScore W2017011289C185592680 @default.
• W2017011289 hasConceptScore W2017011289C203014093 @default.
• W2017011289 hasConceptScore W2017011289C2776365762 @default.

• next