Literature DB >> 7537030

Action of uracil analogs on human immunodeficiency virus type 1 and its reverse transcriptase.

G Piras1, G E Dutschman, G J Im, B C Pan, S H Chu, Y C Cheng.   

Abstract

Three structural analogs of 5-ethyl-1-benzyloxymethyl-6-(phenylthio)uracil (E-BPU) inhibited human immunodeficiency virus type 1 (HIV-1) replication without cytotoxicity in vitro and were more potent than azidothymidine and were as potent as E-BPU. The target of these compounds is HIV-1 reverse transcriptase. Reverse transcriptases resistant to nevirapine (tyrosine at position 181 to cysteine) and TIBO R82150 (leucine at position 100 to isoleucine) are cross resistant to E-BPU analogs. Nevirapine- or TIBO R82150-resistant HIV-1 were cross resistant to E-BPU analogs but were inhibited at concentrations 11- to 135-fold lower than the cytotoxic doses.

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Year:  1995        PMID： 7537030      PMCID： PMC162575          DOI： 10.1128/AAC.39.2.539

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  15 in total

Review 1.  HIV resistance to reverse transcriptase inhibitors.

Authors:  E De Clercq
Journal:  Biochem Pharmacol       Date:  1994-01-20       Impact factor: 5.858

2.  Human immunodeficiency virus type 1 mutants resistant to nonnucleoside inhibitors of reverse transcriptase arise in tissue culture.

Authors:  D Richman; C K Shih; I Lowy; J Rose; P Prodanovich; S Goff; J Griffin
Journal:  Proc Natl Acad Sci U S A       Date:  1991-12-15       Impact factor: 11.205

3.  Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives.

Authors:  R Pauwels; K Andries; J Desmyter; D Schols; M J Kukla; H J Breslin; A Raeymaeckers; J Van Gelder; R Woestenborghs; J Heykants
Journal:  Nature       Date:  1990-02-01       Impact factor: 49.962

4.  Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors.

Authors:  J H Nunberg; W A Schleif; E J Boots; J A O'Brien; J C Quintero; J M Hoffman; E A Emini; M E Goldman
Journal:  J Virol       Date:  1991-09       Impact factor: 5.103

5.  An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives.

Authors:  Z Debyser; R Pauwels; K Andries; J Desmyter; M Kukla; P A Janssen; E De Clercq
Journal:  Proc Natl Acad Sci U S A       Date:  1991-02-15       Impact factor: 11.205

6.  Potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by 5-ethyl-6-phenylthiouracil derivatives through their interaction with the HIV-1 reverse transcriptase.

Authors:  M Baba; E De Clercq; H Tanaka; M Ubasawa; H Takashima; K Sekiya; I Nitta; K Umezu; H Nakashima; S Mori
Journal:  Proc Natl Acad Sci U S A       Date:  1991-03-15       Impact factor: 11.205

7.  Identification of the amino acid in the human immunodeficiency virus type 1 reverse transcriptase involved in the pyrophosphate binding of antiviral nucleoside triphosphate analogs and phosphonoformate. Implications for multiple drug resistance.

Authors:  G J Im; E Tramontano; C J Gonzalez; Y C Cheng
Journal:  Biochem Pharmacol       Date:  1993-12-14       Impact factor: 5.858

8.  HIV-1 reverse transcriptase inhibition by a dipyridodiazepinone derivative: BI-RG-587.

Authors:  E Tramontano; Y C Cheng
Journal:  Biochem Pharmacol       Date:  1992-03-17       Impact factor: 5.858

9.  Crystal structure at 3.5 A resolution of HIV-1 reverse transcriptase complexed with an inhibitor.

Authors:  L A Kohlstaedt; J Wang; J M Friedman; P A Rice; T A Steitz
Journal:  Science       Date:  1992-06-26       Impact factor: 47.728

10.  A single conservative amino acid substitution in the reverse transcriptase of human immunodeficiency virus-1 confers resistance to (+)-(5S)-4,5,6,7-tetrahydro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4,5, 1- jk][1,4]benzodiazepin-2(1H)-thione (TIBO R82150).

Authors:  J W Mellors; G J Im; E Tramontano; S R Winkler; D J Medina; G E Dutschman; H Z Bazmi; G Piras; C J Gonzalez; Y C Cheng
Journal:  Mol Pharmacol       Date:  1993-01       Impact factor: 4.436
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