Literature DB >> 9624498

Antiviral activities of 9-R-2-phosphonomethoxypropyl adenine (PMPA) and bis(isopropyloxymethylcarbonyl)PMPA against various drug-resistant human immunodeficiency virus strains.

R V Srinivas1, A Fridland.   

Abstract

9-R-2-Phosphonomethoxypropyl adenine (PMPA) is an acyclic nucleoside phosphonate analog that has demonstrated efficacy against human immunodeficiency virus (HIV). We recently described the synthesis, metabolism, and biological activities of bis(isopropyloxymethylcarbonyl)PMPA [bis(poc)PMPA] as an orally bioavailable prodrug for PMPA. Among a large panel of drug-resistant HIV type 1 variants, only the K65R virus was resistant to PMPA. K65R virus also showed reduced susceptibility to bis(poc)PMPA, although the prodrug could still inhibit these viruses at submicromolar, nontoxic concentrations. Among a panel of seven primary clinical isolates from patients with diverse treatment histories, only one isolate showed reduced susceptibility to PMPA and was found to carry three mutations (M41L, T69N, R73K) in its reverse transcriptase catalytic domain.

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Year:  1998        PMID： 9624498      PMCID： PMC105626     

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


  29 in total

1.  Multiple mutations in HIV-1 reverse transcriptase confer high-level resistance to zidovudine (AZT).

Authors:  B A Larder; S D Kemp
Journal:  Science       Date:  1989-12-01       Impact factor: 47.728

2.  Resistance to ddI and sensitivity to AZT induced by a mutation in HIV-1 reverse transcriptase.

Authors:  M H St Clair; J L Martin; G Tudor-Williams; M C Bach; C L Vavro; D M King; P Kellam; S D Kemp; B A Larder
Journal:  Science       Date:  1991-09-27       Impact factor: 47.728

3.  Anti-human immunodeficiency virus activity and cellular metabolism of a potential prodrug of the acyclic nucleoside phosphonate 9-R-(2-phosphonomethoxypropyl)adenine (PMPA), Bis(isopropyloxymethylcarbonyl)PMPA.

Authors:  B L Robbins; R V Srinivas; C Kim; N Bischofberger; A Fridland
Journal:  Antimicrob Agents Chemother       Date:  1998-03       Impact factor: 5.191

4.  Characterization of human immunodeficiency viruses resistant to oxathiolane-cytosine nucleosides.

Authors:  R F Schinazi; R M Lloyd; M H Nguyen; D L Cannon; A McMillan; N Ilksoy; C K Chu; D C Liotta; H Z Bazmi; J W Mellors
Journal:  Antimicrob Agents Chemother       Date:  1993-04       Impact factor: 5.191

5.  Convergent combination therapy can select viable multidrug-resistant HIV-1 in vitro.

Authors:  B A Larder; P Kellam; S D Kemp
Journal:  Nature       Date:  1993-09-30       Impact factor: 49.962

6.  Nevirapine resistance mutations of human immunodeficiency virus type 1 selected during therapy.

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7.  Fifth mutation in human immunodeficiency virus type 1 reverse transcriptase contributes to the development of high-level resistance to zidovudine.

Authors:  P Kellam; C A Boucher; B A Larder
Journal:  Proc Natl Acad Sci U S A       Date:  1992-03-01       Impact factor: 11.205

8.  Metabolism and in vitro antiretroviral activities of bis(pivaloyloxymethyl) prodrugs of acyclic nucleoside phosphonates.

Authors:  R V Srinivas; B L Robbins; M C Connelly; Y F Gong; N Bischofberger; A Fridland
Journal:  Antimicrob Agents Chemother       Date:  1993-10       Impact factor: 5.191

9.  Human immunodeficiency virus type 1 pol gene mutations which cause decreased susceptibility to 2',3'-dideoxycytidine.

Authors:  J E Fitzgibbon; R M Howell; C A Haberzettl; S J Sperber; D J Gocke; D T Dubin
Journal:  Antimicrob Agents Chemother       Date:  1992-01       Impact factor: 5.191

10.  Combination therapy with zidovudine and didanosine selects for drug-resistant human immunodeficiency virus type 1 strains with unique patterns of pol gene mutations.

Authors:  R W Shafer; M J Kozal; M A Winters; A K Iversen; D A Katzenstein; M V Ragni; W A Meyer; P Gupta; S Rasheed; R Coombs
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  26 in total

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Journal:  Antimicrob Agents Chemother       Date:  2002-05       Impact factor: 5.191

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3.  Antiretroviral Drug Resistance in HIV-1.

Authors: 
Journal:  Curr Infect Dis Rep       Date:  1999-08       Impact factor: 3.725

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Authors:  Phalguni Gupta; Deena Ratner; Ming Ding; Bruce Patterson; Lisa C Rohan; Todd A Reinhart; Velpandi Ayyavoo; Xioli Huang; Dorothy L Patton; Bharat Ramratnam; Alexander M Cole
Journal:  J Acquir Immune Defic Syndr       Date:  2012-08-15       Impact factor: 3.731

5.  Pharmacokinetic and safety analyses of tenofovir and tenofovir-emtricitabine vaginal tablets in pigtailed macaques.

Authors:  Lara E Pereira; Meredith R Clark; David R Friend; David A Garber; Janet M McNicholl; R Michael Hendry; Gustavo F Doncel; James M Smith
Journal:  Antimicrob Agents Chemother       Date:  2014-02-24       Impact factor: 5.191

6.  Tenofovir diphosphate concentrations and prophylactic effect in a macaque model of rectal simian HIV transmission.

Authors:  Peter L Anderson; David V Glidden; Lane R Bushman; Walid Heneine; J Gerardo García-Lerma
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7.  Acyclic nucleoside bisphosphonates: synthesis and properties of chiral 2-amino-4,6-bis[(phosphonomethoxy)alkoxy]pyrimidines.

Authors:  Petra Doláková; Martin Dracínský; Milena Masojídková; Veronika Solínová; Václav Kasicka; Antonín Holý
Journal:  Eur J Med Chem       Date:  2008-10-02       Impact factor: 6.514

Review 8.  Clinical potential of the acyclic nucleoside phosphonates cidofovir, adefovir, and tenofovir in treatment of DNA virus and retrovirus infections.

Authors:  Erik De Clercq
Journal:  Clin Microbiol Rev       Date:  2003-10       Impact factor: 26.132

9.  Memory CD4(+) T cells are the earliest detectable human immunodeficiency virus type 1 (HIV-1)-infected cells in the female genital mucosal tissue during HIV-1 transmission in an organ culture system.

Authors:  Phalguni Gupta; Kelly B Collins; Deena Ratner; Simon Watkins; Gregory J Naus; Daniel V Landers; Bruce K Patterson
Journal:  J Virol       Date:  2002-10       Impact factor: 5.103

10.  Novel recombinant virus assay for measuring susceptibility of human immunodeficiency virus type 1 group M subtypes to clinically approved drugs.

Authors:  Kris Covens; Nathalie Dekeersmaeker; Yoeri Schrooten; Jan Weber; Dominique Schols; Miguel E Quiñones-Mateu; Anne-Mieke Vandamme; Kristel Van Laethem
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