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Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins

  1. Author:
    Wang, G. P.
    Nikolovska-Coleska, Z.
    Yang, C. Y.
    Wang, R. X.
    Tang, G. Z.
    Guo, J.
    Shangary, S.
    Qiu, S.
    Gao, W.
    Yang, D. J.
    Meagher, J.
    Stuckey, J.
    Krajewski, K.
    Jiang, S.
    Roller, P. P.
    Abaan, H. O.
    Tomita, Y.
    Wang, S. M.

  2. Author Address

    Univ Michigan, Ctr Comprehens Canc, Ann Arbor, MI 48109 USA. Univ Michigan, Dept Internal Med, Ann Arbor, MI 48109 USA. Univ Michigan, Dept Pharmacol & Med Chem, Ann Arbor, MI 48109 USA. Univ Michigan, Inst Life Sci, Ann Arbor, MI 48109 USA. NCI, Lab Med Chem, NIH, Frederick, MD 21702 USA. Georgetown Univ, Lombardi Comprehens Canc Ctr, Med Ctr, Washington, DC 20057 USA.;Wang, SM, Univ Michigan, Ctr Comprehens Canc, 1500 E Med Ctr Dr, Ann Arbor, MI 48109 USA.;shaomeng@umich.edu
    1. Year: 2006
    2. Date: Oct
  2. Journal: Journal of Medicinal Chemistry
    1. 49
    2. 21
    3. Pages: 6139-6142
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    A structure-based approach was employed to design a new class of small-molecule inhibitors of Bcl-2. The most potent compound 5 (TW-37) binds to Bcl-2 with a K-i value of 290 nM and also to BclxL and Mcl-1 with high affinities. Compound 5 potently inhibits cell growth in PC-3 prostate cancer cells with an IC50 value of 200 nM and effectively induces apoptosis in a dose-dependent manner.

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External Sources

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  2. DOI: 10.1021/jm060460o
  3. View record in Web of Science®
  4. WOS: 000241192400001

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