CELLULAR-METABOLISM OF (-) ENANTIOMERIC 2'-DEOXY-3'-THIACYTIDINE

被引：110

作者：

CAMMACK, N ^{[1
]}

ROUSE, P ^{[1
]}

MARR, CLP ^{[1
]}

REID, PJ ^{[1
]}

BOEHME, RE ^{[1
]}

COATES, JAV ^{[1
]}

PENN, CR ^{[1
]}

CAMERON, JM ^{[1
]}

机构：

[1] GLAXO GRP RES LTD,DEPT VIROL,GREENFORD RD,GREENFORD UB6 0HE,MIDDX,ENGLAND

来源：

BIOCHEMICAL PHARMACOLOGY | 1992年 / 43卷 / 10期

关键词：

D O I：

10.1016/0006-2952(92)90162-C

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

页码：2059 / 2064

页数：6

共 11 条

[1] THE SEPARATED ENANTIOMERS OF 2'-DEOXY-3'-THIACYTIDINE (BCH-189) BOTH INHIBIT HUMAN-IMMUNODEFICIENCY-VIRUS REPLICATION INVITRO
COATES, JAV
CAMMACK, N
JENKINSON, HJ
MUTTON, IM
PEARSON, BA
STORER, R
CAMERON, JM
PENN, CR
[J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1992, 36 (01) : 202 - 205
[2] PHOSPHOROLYSIS OF (E)-5-(2-BROMOVINYL)-2'-DEOXYURIDINE (BVDU) AND OTHER 5-SUBSTITUTED-2'-DEOXYURIDINES BY PURIFIED HUMAN THYMIDINE PHOSPHORYLASE AND INTACT BLOOD-PLATELETS
DESGRANGES, C
RAZAKA, G
RABAUD, M
BRICAUD, H
BALZARINI, J
DECLERCQ, E
[J]. BIOCHEMICAL PHARMACOLOGY, 1983, 32 (23) : 3583 - 3590
[3] EFFECTS OF 3'-AZIDO-3'-DEOXYTHYMIDINE ON THE DEOXYNUCLEOTIDE TRIPHOSPHATE POOLS OF CULTURED HUMAN-CELLS
FRICK, LW
NELSON, DJ
STCLAIR, MH
FURMAN, PA
KRENITSKY, TA
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1988, 154 (01) : 124 - 129
[4] FRICK LW, 1989, PURINE PYRIMIDINE B, V6, P389
[5] PHOSPHORYLATION OF 3'-AZIDO-3'-DEOXYTHYMIDINE AND SELECTIVE INTERACTION OF THE 5'-TRIPHOSPHATE WITH HUMAN-IMMUNODEFICIENCY-VIRUS REVERSE-TRANSCRIPTASE
FURMAN, PA
FYFE, JA
STCLAIR, MH
WEINHOLD, K
RIDEOUT, JL
FREEMAN, GA
LEHRMAN, SN
BOLOGNESI, DP
BRODER, S
MITSUYA, H
BARRY, DW
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1986, 83 (21) : 8333 - 8337
[6] HAO Z, 1988, MOL PHARMACOL, V34, P431
[7] INHIBITION OF THE INVITRO INFECTIVITY AND CYTOPATHIC EFFECT OF HUMAN LYMPHOTROPHIC-T VIRUS "TYPE-III/LYMPHADENOPATHY-ASSOCIATED VIRUS (HTLV-III/LAV) BY 2',3'-DIDEOXYNUCLEOSIDES
MITSUYA, H
BRODER, S
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1986, 83 (06) : 1911 - 1915
[8] ORR DC, IN PRESS J BIOL CHEM
[9] STARNES MC, 1987, J BIOL CHEM, V262, P988
[10] ESTABLISHMENT AND CHARACTERIZATION OF A HUMAN HISTIOCYTIC LYMPHOMA CELL LINE (U-937)
SUNDSTROM, C
NILSSON, K
[J]. INTERNATIONAL JOURNAL OF CANCER, 1976, 17 (05) : 565 - 577

← 1 2 →