Recent Advances in the Development of Small-molecule CCR5 Inhibitors for HIV

被引:11
作者
Liu, Tao [1 ]
Weng, Zhiyong [1 ]
Dong, Xiaowu [1 ]
Hu, Yongzhou [1 ]
机构
[1] Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China
关键词
HIV; Entry; Co-receptor; CCR5; Small-molecule inhibitor; Maraviroc; IMMUNODEFICIENCY-VIRUS TYPE-1; CHEMOKINE RECEPTOR ANTAGONISTS; INFECTION IN-VITRO; BIOLOGICAL EVALUATION; ANTI-HIV-1; AGENTS; HIGHLY POTENT; ANTIVIRAL ACTIVITY; ENTRY INHIBITORS; VIRAL ENTRY; PART;
D O I
10.2174/13895575110091277
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
CCR5 (C-C chemokine receptor type 5) is a chemokine receptor that has been identified as a major HIV coreceptor in viral entry and therefore is a highly validated target for the development of new anti-HIV drugs. Here, we discuss the insights gained so far relevant to the development of small-molecule CCR5 inhibitors for the treatment of HIV, and highlight small-molecule CCR5 inhibitors that are currently under preclinical and clinical trials.
引用
收藏
页码:1277 / 1292
页数:16
相关论文
共 107 条
  • [1] Pharmacokinetics and short-term safety of 873140, a novel CCR5 antagonist, in healthy adult subjects
    Adkison, KK
    Shachoy-Clark, A
    Fang, L
    Lou, Y
    O'Mara, K
    Berrey, MM
    Piscitelli, SC
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2005, 49 (07) : 2802 - 2806
  • [2] The discovery of CCR5 receptor antagonists for the treatment of HIV infection: Hit-to-lead studies
    Armour, Duncan
    de Groot, Marcel J.
    Edwards, Martin
    Perros, Manos
    Price, David A.
    Stammen, Blanda L.
    Wood, Anthony
    [J]. CHEMMEDCHEM, 2006, 1 (07) : 706 - +
  • [3] TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans
    Baba, M
    Takashima, K
    Miyake, H
    Kanzaki, N
    Teshima, K
    Wang, X
    Shiraishi, M
    Iizawa, Y
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2005, 49 (11) : 4584 - 4591
  • [4] Recent advances of CCR5 antagonists
    Baba, Masanori
    [J]. CURRENT OPINION IN HIV AND AIDS, 2006, 1 (05) : 367 - 372
  • [5] Bajacan J.V., 2008, OPEN ALL AREAS CHEM, P188
  • [6] Chemokine receptors as HIV-1 coreceptors: Roles in viral entry, tropism, and disease
    Berger, EA
    Murphy, PM
    Farber, JM
    [J]. ANNUAL REVIEW OF IMMUNOLOGY, 1999, 17 : 657 - 700
  • [7] How many more AIDS deaths?
    Bongaarts, John
    Pelletier, Francois
    Gerland, Patrick
    [J]. LANCET, 2010, 375 (9709) : 103 - 104
  • [8] Bourque E., 2008, Chemokine receptor binding compounds, Patent No. 08070758
  • [9] Brown D.S., 2008, Piperidine derivative used for treating chemokine receptor 5 mediated diseases, Patent No. 08071931
  • [10] Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas
    Burrows, JN
    Cumming, JG
    Fillery, SM
    Hamlin, GA
    Hudson, JA
    Jackson, RJ
    McLaughlin, S
    Shaw, JS
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (01) : 25 - 28