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Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents.
Wang, Yan-Kai; Huang, Xu-Sheng; Sun, Hao; Ma, Meng-Di; Yu, Hai-Peng; Hu, Wei; Li, Zhi-Yu; Li, Zhong; Luo, Rong-Hua; Tian, Ren-Rong; Xiao, Tai-Fu; Yang, Liu-Meng; Zheng, Yong-Tang; Li, Xun.
Afiliación
  • Wang YK; School of Pharmaceutical Sciences & Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, National Key Laboratory of Advanced Drug Delivery System, Key Laboratory for Biotechnology Drugs of National Health Commission (Shandong Academy of Medic
  • Huang XS; Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science and Yunnan Province, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Acade
  • Sun H; University of Chinese Academy of Sciences, Beijing 100049, China.
  • Ma MD; School of Pharmaceutical Sciences & Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, National Key Laboratory of Advanced Drug Delivery System, Key Laboratory for Biotechnology Drugs of National Health Commission (Shandong Academy of Medic
  • Yu HP; Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science and Yunnan Province, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Acade
  • Hu W; University of Chinese Academy of Sciences, Beijing 100049, China.
  • Li ZY; Shandong University, No. 72 Binhai Road, Qingdao 266237, China.
  • Li Z; Shandong University, No. 72 Binhai Road, Qingdao 266237, China.
  • Luo RH; Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, Department of Chemistry & Biochemistry, Misher College of Arts and Sciences, University of the Sciences, 600 South 43rd Street, Philadelphia, Pennsylvania 19104, United States.
  • Tian RR; Shandong University, No. 72 Binhai Road, Qingdao 266237, China.
  • Xiao TF; Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science and Yunnan Province, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Acade
  • Yang LM; Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science and Yunnan Province, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Acade
  • Zheng YT; Department of Gastrointestinal Surgery, The Second Affiliated Hospital of Kunming Medical University, Kunming 650101, Yunnan, China.
  • Li X; Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science and Yunnan Province, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Acade
ACS Med Chem Lett ; 15(1): 60-68, 2024 Jan 11.
Article en En | MEDLINE | ID: mdl-38229757
ABSTRACT
Bromodomain-containing protein 4 (BRD4) inhibitors have been proven to be a promising option for anti-HIV-1 latency therapeutics. We herein describe the design, synthesis, and anti-HIV-1 latency bioevaluation of triazolopyridine derivatives as BRD4 inhibitors. Among them, compound 13d displayed favorable HIV-1 reactivation and prominent safety profile without triggering abnormal immune activation. It exerted strong synergism when combined with the PKC activator prostratin and has the same BRD4-targeting latency mechanism as observed with JQ1, by stimulating Tat-dependent HIV-1 elongation. Besides, it neither affected the antiviral efficacies of antiviral drugs nor caused secondary infections to uninfected cells and the latency reversing potency of 13d, in turn, was not affected by different classes of antiviral drugs.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2024 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2024 Tipo del documento: Article Pais de publicación: Estados Unidos