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Literature DB >> 23379607

New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1.

Zhao Dang¹, Phong Ho, Lei Zhu, Keduo Qian, Kuo-Hsiung Lee, Li Huang, Chin-Ho Chen.

Abstract

Bevirimat (1, BVM) is an anti-HIV agent that blocks HIV-1 replication by interfering with HIV-1 Gag-SP1 processing at a late stage of viral maturation. However, clinical trials of 1 have revealed a high baseline drug resistance that is attributed to naturally occurring polymorphisms in HIV-1 Gag. To overcome the drug resistance, 28 new derivatives of 1 were synthesized and tested against compound 1-resistant (BVM-R) HIV-1 variants. Among them, compound 6 exhibited much improved activity against several HIV-1 strains carrying BVM-R polymorphisms. Compound 6 was at least 20-fold more potent than 1 against the replication of NL4-3/V370A, which carries the most prevalent clinical BVM-R polymorphism in HIV-1 Gag-SP1. Thus, compound 6 merits further development as a potential anti-AIDS clinical trial candidate.

Entities: CellLine Chemical Disease Gene Mutation Species

Mesh：

Substances：

Year: 2013 PMID： 23379607 PMCID： PMC3600082 DOI： 10.1021/jm3016969

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

25 in total

1. Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents.

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Journal: J Med Chem Date: 1996-03-01 Impact factor: 7.446

2. Quantification of latent tissue reservoirs and total body viral load in HIV-1 infection.

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Journal: Nature Date: 1997-05-08 Impact factor: 49.962

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Journal: Science Date: 1997-11-14 Impact factor: 47.728

4. Role of human immunodeficiency virus (HIV) type 1 envelope in the anti-HIV activity of the betulinic acid derivative IC9564.

Authors: S L Holz-Smith; I C Sun; L Jin; T J Matthews; K H Lee; C H Chen
Journal: Antimicrob Agents Chemother Date: 2001-01 Impact factor: 5.191

Review 5. Betulinic acid derivatives as HIV-1 antivirals.

Authors: Christopher Aiken; Chin Ho Chen
Journal: Trends Mol Med Date: 2005-01 Impact factor: 11.951

6. Transmission of HIV-1 drug-resistant variants: prevalence and effect on treatment outcome.

Authors: Martin R Jakobsen; Martin Tolstrup; Ole S Søgaard; Louise B Jørgensen; Paul R Gorry; Alex Laursen; Lars Ostergaard
Journal: Clin Infect Dis Date: 2010-02-15 Impact factor: 9.079

7. Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells.

Authors: J F Mayaux; A Bousseau; R Pauwels; T Huet; Y Hénin; N Dereu; M Evers; F Soler; C Poujade; E De Clercq
Journal: Proc Natl Acad Sci U S A Date: 1994-04-26 Impact factor: 11.205

8. Recovery of replication-competent HIV despite prolonged suppression of plasma viremia.

Authors: J K Wong; M Hezareh; H F Günthard; D V Havlir; C C Ignacio; C A Spina; D D Richman
Journal: Science Date: 1997-11-14 Impact factor: 47.728

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Journal: Proc Natl Acad Sci U S A Date: 2003-10-22 Impact factor: 11.205

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Authors: Jing Zhou; Xiong Yuan; David Dismuke; Brett M Forshey; Christopher Lundquist; Kuo-Hsiung Lee; Christopher Aiken; Chin Ho Chen
Journal: J Virol Date: 2004-01 Impact factor: 5.103

28 in total

Review 1. Highly resistant HIV-1 proteases and strategies for their inhibition.

Authors: Irene T Weber; Daniel W Kneller; Andres Wong-Sam
Journal: Future Med Chem Date: 2015 Impact factor: 3.808

Review 2. Recent advances in natural anti-HIV triterpenoids and analogs.

Authors: Hai-Feng Wu; Susan L Morris-Natschke; Xu-Dong Xu; Mei-Hua Yang; Yung-Yi Cheng; Shi-Shan Yu; Kuo-Hsiung Lee
Journal: Med Res Rev Date: 2020-07-14 Impact factor: 12.944

3. Alkyl Amine Bevirimat Derivatives Are Potent and Broadly Active HIV-1 Maturation Inhibitors.

Authors: Emiko Urano; Sherimay D Ablan; Rebecca Mandt; Gary T Pauly; Dina M Sigano; Joel P Schneider; David E Martin; Theodore J Nitz; Carl T Wild; Eric O Freed
Journal: Antimicrob Agents Chemother Date: 2015-10-19 Impact factor: 5.191

4. Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity.

Authors: Alicia Regueiro-Ren; Zheng Liu; Yan Chen; Ny Sin; Sing-Yuen Sit; Jacob J Swidorski; Jie Chen; Brian L Venables; Juliang Zhu; Beata Nowicka-Sans; Tricia Protack; Zeyu Lin; Brian Terry; Himadri Samanta; Sharon Zhang; Zhufang Li; Brett R Beno; Xiaohua S Huang; Sandhya Rahematpura; Dawn D Parker; Roy Haskell; Susan Jenkins; Kenneth S Santone; Mark I Cockett; Mark Krystal; Nicholas A Meanwell; Umesh Hanumegowda; Ira B Dicker
Journal: ACS Med Chem Lett Date: 2016-04-22 Impact factor: 4.345

10. Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.

Authors: Yu Zhao; Qiong Gu; Susan L Morris-Natschke; Chin-Ho Chen; Kuo-Hsiung Lee
Journal: J Med Chem Date: 2016-09-22 Impact factor: 7.446