TSAO DERIVATIVES - HIGHLY SPECIFIC INHIBITORS OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 (HIV-1) REPLICATION

被引:22
作者
CAMARASA, MJ
PEREZPEREZ, MJ
VELAZQUEZ, S
SANFELIX, A
ALVAREZ, R
INGATE, S
JIMENO, ML
KARLSSON, A
DECLERCQ, E
BALZARINI, J
机构
[1] CATHOLIC UNIV LEUVEN,REGA INST MED RES,B-3000 LOUVAIN,BELGIUM
[2] KAROLINSKA INST,BIOCHEM LAB 1,S-10401 STOCKHOLM,SWEDEN
来源
NUCLEOSIDES & NUCLEOTIDES | 1995年 / 14卷 / 3-5期
关键词
D O I
10.1080/15257779508012432
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
TSAO derivatives represent a unique class of nucleosides that are specifically targeted at HIV-1 RT. This overview is focussed on the chemical synthesis, the conformational studies, the antiviral and metabolic properties of TSAO derivatives, as well as their mechanism of antiviral action and the molecular basis of the vapid selection of resistant HIV-1 strains that emerge in cell culture in the presence of TSAO derivatives.
引用
收藏
页码:585 / 594
页数:10
相关论文
共 44 条
[21]  
JIMENO ML, 1994, UNPUB
[22]  
JONCKHEERE H, 1994, IN PRESS J BIOL CHEM
[23]   CRYSTAL-STRUCTURE AT 3.5 ANGSTROM RESOLUTION OF HIV-1 REVERSE-TRANSCRIPTASE COMPLEXED WITH AN INHIBITOR [J].
KOHLSTAEDT, LA ;
WANG, J ;
FRIEDMAN, JM ;
RICE, PA ;
STEITZ, TA .
SCIENCE, 1992, 256 (5065) :1783-1790
[24]   INHIBITION OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 (HIV-1) REPLICATION BY THE DIPYRIDODIAZEPINONE BI-RG-587 [J].
KOUP, RA ;
MERLUZZI, VJ ;
HARGRAVE, KD ;
ADAMS, J ;
GROZINGER, K ;
ECKNER, RJ ;
SULLIVAN, JL .
JOURNAL OF INFECTIOUS DISEASES, 1991, 163 (05) :966-970
[25]   SYNTHESIS AND ANTI-HIV-1 ACTIVITY OF 4,5,6,7-TETRAHYDRO-5-METHYLIMIDAZO[4,5,1-JK][1,4]BENZODIAZEPIN-2(1H)-ONE (TIBO) DERIVATIVES [J].
KUKLA, MJ ;
BRESLIN, HJ ;
PAUWELS, R ;
FEDDE, CL ;
MIRANDA, M ;
SCOTT, MK ;
SHERRILL, RG ;
RAEYMAEKERS, A ;
VANGELDER, J ;
ANDRIES, K ;
JANSSEN, MAC ;
DECLERQ, E ;
JANSSEN, PAJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (02) :746-751
[26]   MULTIPLE MUTATIONS IN HIV-1 REVERSE-TRANSCRIPTASE CONFER HIGH-LEVEL RESISTANCE TO ZIDOVUDINE (AZT) [J].
LARDER, BA ;
KEMP, SD .
SCIENCE, 1989, 246 (4934) :1155-1158
[27]   INHIBITION OF HIV-1 REPLICATION BY A NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITOR [J].
MERLUZZI, VJ ;
HARGRAVE, KD ;
LABADIA, M ;
GROZINGER, K ;
SKOOG, M ;
WU, JC ;
SHIH, CK ;
ECKNER, K ;
HATTOX, S ;
ADAMS, J ;
ROSEHTHAL, AS ;
FAANES, R ;
ECKNER, RJ ;
KOUP, RA ;
SULLIVAN, JL .
SCIENCE, 1990, 250 (4986) :1411-1413
[29]   A NOVEL LEAD FOR SPECIFIC ANTI-HIV-1 AGENTS - 1-[(2-HYDROXYETHOXY)METHYL]-6-(PHENYLTHIO)THYMINE [J].
MIYASAKA, T ;
TANAKA, H ;
BABA, M ;
HAYAKAWA, H ;
WALKER, RT ;
BALZARINI, J ;
DECLERCQ, E .
JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (12) :2507-2509
[30]  
Nanni Raymond G., 1993, Perspectives in Drug Discovery and Design, V1, P129, DOI 10.1007/BF02171659