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Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain

  1. Author:
    Zhao, X. Z.
    Hymel, D.
    Burke, T. R.

  2. Author Address

    Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, United States. Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, United States. Electronic address: burkete@helix.nih.gov.
    1. Year: 2016
    2. Date: 15-Oct
    3. Epub Date: 9/15/2016
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 26
    2. 20
    3. Pages: 5009-5012
  4. Type of Article: Article
  5. ISSN: 0960-894X (Print) 0960-894x
  1. Abstract:

    By a process involving initial screening of a set of 87 aldehydes using an oxime ligation-based strategy, we were able to achieve a several-fold affinity enhancement over one of the most potent previously known polo-like kinase 1 (Plk1) polo-box domain (PBD) binding inhibitors. This improved binding may result by accessing a newly identified auxiliary region proximal to a key hydrophobic cryptic pocket on the surface of the protein. Our findings could have general applicability to the design of PBD-binding antagonists.

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External Sources

  1. View Full Text
  2. DOI: 10.1016/j.bmcl.2016.08.098
  3. PMID: 27624074
  4. PMCID: PMC5061138
  5. View record in Web of Science®
  6. WOS: 000385498500031
  7. NIHMSID: NIHMS816092

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