title: Cellular metabolism of (-) enantiomeric 2'-deoxy-3'-thiacytidine.
abstract: The metabolism of (-) enantiomeric 2'-deoxy-3'-thiacytidine (3TC) was examined in human immunodeficiency virus type 1 (HIV-1)-infected and mock-infected human cells. 3TC 5'-triphosphate levels accumulated comparably in HIV-1-infected and mock-infected phytohaemagglutinin-stimulated peripheral blood lymphocytes (PBL) and reached 40% or more of total intracellular 3TC metabolites after 4 hr. The rate of decay of 3TC triphosphate in HIV-1-infected and mock-infected PBL measured as a half-life (T1/2) ranged from 10.5 to 15.5 hr. 3TC did not significantly affect metabolism of deoxynucleotides in the U937 cell line, and was shown to be resistant to the action of human platelet pyrimidine nucleoside phosphorylase.
authors.affiliation: Virology Department, Glaxo Group Research Ltd, Greenford, U.K.
authors.forename: N
authors.initials: N
authors.lastname: Cammack
authors.forename: P
authors.initials: P
authors.lastname: Rouse
authors.forename: C L
authors.initials: CL
authors.lastname: Marr
authors.forename: P J
authors.initials: PJ
authors.lastname: Reid
authors.forename: R E
authors.initials: RE
authors.lastname: Boehme
authors.forename: J A
authors.initials: JA
authors.lastname: Coates
authors.forename: C R
authors.initials: CR
authors.lastname: Penn
authors.forename: J M
authors.initials: JM
authors.lastname: Cameron
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000378:metabolism; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D002478:Cells, Cultured / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D019259:Lamivudine; D008214:Lymphocytes / Q000187:drug effects / Q000378:metabolism; D010430:Pentosyltransferases / Q000378:metabolism; D010766:Phosphorylation; D057845:Pyrimidine Phosphorylases; D013237:Stereoisomerism; D013939:Thymidine Phosphorylase / Q000378:metabolism*; D016047:Zalcitabine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D015215:Zidovudine / Q000494:pharmacology
chemical_list: D019259:Lamivudine; D015215:Zidovudine; D016047:Zalcitabine; D010430:Pentosyltransferases; D057845:Pyrimidine Phosphorylases; D013939:Thymidine Phosphorylase