Literature DB >> 16420027

HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent.

Vasu Nair1, Guochen Chi, Roger Ptak, Nouri Neamati.   

Abstract

HIV integrase is essential for HIV replication. However, there are currently no integrase inhibitors in clinical use for AIDS. We have discovered a conceptually new beta-diketo acid that is a powerful inhibitor of both the 3'-processing and strand transfer steps of HIV-1 integrase. The in vitro anti-HIV data of this inhibitor were remarkable as exemplified by its highly potent antiviral therapeutic efficacy against HIV(TEKI) and HIV-1(NL4)(-)(3) replication in PBMC (TI >4,000 and >10,000, respectively).

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Year:  2006        PMID： 16420027      PMCID： PMC2518396          DOI： 10.1021/jm0508890

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  26 in total

Review 1.  Small-molecule HIV-1 integrase inhibitors: the 2001-2002 update.

Authors:  Raveendra Dayam; Nouri Neamati
Journal:  Curr Pharm Des       Date:  2003       Impact factor: 3.116

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Journal:  Annu Rev Biochem       Date:  1994       Impact factor: 23.643

Review 3.  Integrase inhibitors to treat HIV/AIDS.

Authors:  Yves Pommier; Allison A Johnson; Christophe Marchand
Journal:  Nat Rev Drug Discov       Date:  2005-03       Impact factor: 84.694

4.  Probing interactions between viral DNA and human immunodeficiency virus type 1 integrase using dinucleotides.

Authors:  A Mazumder; H Uchida; N Neamati; S Sunder; M Jaworska-Maslanka; E Wickstrom; F Zeng; R A Jones; R F Mandes; H K Chenault; Y Pommier
Journal:  Mol Pharmacol       Date:  1997-04       Impact factor: 4.436

Review 5.  The human immunodeficiency virus: infectivity and mechanisms of pathogenesis.

Authors:  A S Fauci
Journal:  Science       Date:  1988-02-05       Impact factor: 47.728

6.  Selective transcription and modulation of resting T cell activity by preintegrated HIV DNA.

Authors:  Y Wu; J W Marsh
Journal:  Science       Date:  2001-08-24       Impact factor: 47.728

7.  HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase.

Authors:  A S Espeseth; P Felock; A Wolfe; M Witmer; J Grobler; N Anthony; M Egbertson; J Y Melamed; S Young; T Hamill; J L Cole; D J Hazuda
Journal:  Proc Natl Acad Sci U S A       Date:  2000-10-10       Impact factor: 11.205

Review 8.  In search of a selective antiviral chemotherapy.

Authors:  E De Clercq
Journal:  Clin Microbiol Rev       Date:  1997-10       Impact factor: 26.132

9.  New class of HIV integrase inhibitors that block viral replication in cell culture.

Authors:  Christophe Pannecouque; Wim Pluymers; Bénédicte Van Maele; Victor Tetz; Peter Cherepanov; Erik De Clercq; Myriam Witvrouw; Zeger Debyser
Journal:  Curr Biol       Date:  2002-07-23       Impact factor: 10.834

10.  Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques.

Authors:  Daria J Hazuda; Steven D Young; James P Guare; Neville J Anthony; Robert P Gomez; John S Wai; Joseph P Vacca; Larry Handt; Sherri L Motzel; Hilton J Klein; Geethanjali Dornadula; Robert M Danovich; Marc V Witmer; Keith A A Wilson; Lynda Tussey; William A Schleif; Lori S Gabryelski; Lixia Jin; Michael D Miller; Danilo R Casimiro; Emilio A Emini; John W Shiver
Journal:  Science       Date:  2004-07-08       Impact factor: 47.728
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  13 in total

1.  Double Variational Binding--(SMILES) Conformational Analysis by Docking Mechanisms for Anti-HIV Pyrimidine Ligands.

Authors:  Mihai V Putz; Nicoleta A Dudaș; Adriana Isvoran
Journal:  Int J Mol Sci       Date:  2015-08-18       Impact factor: 5.923

2.  Solid-state tautomeric structure and invariom refinement of a novel and potent HIV integrase inhibitor.

Authors:  John Bacsa; Maurice Okello; Pankaj Singh; Vasu Nair
Journal:  Acta Crystallogr C       Date:  2013-02-14       Impact factor: 1.172

3.  A novel diketo phosphonic acid that exhibits specific, strand-transfer inhibition of HIV integrase and anti-HIV activity.

Authors:  Guochen Chi; Vasu Nair; Elena Semenova; Yves Pommier
Journal:  Bioorg Med Chem Lett       Date:  2006-12-15       Impact factor: 2.823

Review 4.  Alkynoates as Versatile and Powerful Chemical Tools for the Rapid Assembly of Diverse Heterocycles under Transition-Metal Catalysis: Recent Developments and Challenges.

Authors:  Imtiaz Khan; Aliya Ibrar; Sumera Zaib
Journal:  Top Curr Chem (Cham)       Date:  2021-01-05

5.  A novel molecule with notable activity against multi-drug resistant tuberculosis.

Authors:  Vasu Nair; Maurice O Okello; Naveen K Mangu; Byung I Seo; Machhindra G Gund
Journal:  Bioorg Med Chem Lett       Date:  2015-01-28       Impact factor: 2.823

6.  Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity.

Authors:  Byung I Seo; Vinod R Uchil; Maurice Okello; Sanjay Mishra; Xiao-Hui Ma; Malik Nishonov; Qingning Shu; Guochen Chi; Vasu Nair
Journal:  ACS Med Chem Lett       Date:  2011-10-05       Impact factor: 4.345

7.  A quantum mechanic/molecular mechanic study of the wild-type and N155S mutant HIV-1 integrase complexed with diketo acid.

Authors:  Cláudio Nahum Alves; Sergio Martí; Raquel Castillo; Juan Andrés; Vicent Moliner; Iñaki Tuñón; Estanislao Silla
Journal:  Biophys J       Date:  2007-11-02       Impact factor: 4.033

8.  A novel anti-HIV active integrase inhibitor with a favorable in vitro cytochrome P450 and uridine 5'-diphospho-glucuronosyltransferase metabolism profile.

Authors:  Maurice O Okello; Sanjay Mishra; Malik Nishonov; Marie K Mankowski; Julie D Russell; Jiayi Wei; Priscilla A Hogan; Roger G Ptak; Vasu Nair
Journal:  Antiviral Res       Date:  2013-04-18       Impact factor: 5.970

9.  A novel strategy to assemble the beta-diketo acid pharmacophore of HIV integrase inhibitors on purine nucleobase scaffolds.

Authors:  Vinod Uchil; Byung Seo; Vasu Nair
Journal:  J Org Chem       Date:  2007-10-05       Impact factor: 4.354

10.  Pharmacokinetics and dose-range finding toxicity of a novel anti-HIV active integrase inhibitor.

Authors:  Vasu Nair; Maurice Okello; Sanjay Mishra; Jon Mirsalis; Kathleen O'Loughlin; Yu Zhong
Journal:  Antiviral Res       Date:  2014-05-10       Impact factor: 5.970
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