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Antiangiogenic Activity and in Silico Cereblon Binding Analysis of Novel Thalidomide Analogs

  1. Author:
    Peach,Megan [ORCID]
    Beedie, Shaunna L
    Chau, Cindy H
    Collins, Matthew K [ORCID]
    Markolovic, Suzana
    Luo, Weiming
    Tweedie, David
    Steinebach, Christian [ORCID]
    Greig, Nigel H
    Gütschow, Michael [ORCID]
    Vargesson, Neil [ORCID]
    Nicklaus,Marc
    Figg, William D [ORCID]

  2. Author Address

    Basic Science Program, Chemical Biology Laboratory, Frederick National Laboratory for Cancer Research, National Cancer Institute, Frederick, MD 21701, USA., Molecular Pharmacology Section, Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA., School of Medicine, Medical Sciences & Nutrition, Institute of Medical Sciences, University of Aberdeen, Aberdeen AB25 2ZD, UK., Drug Design & Development Section, Translational Gerontology Branch, National Institute on Aging, NIH, Baltimore, MD 21224, USA., Pharmaceutical Institute, University of Bonn, 53121 Bonn, Germany., Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, NIH, Frederick, MD 21701, USA.,
    1. Year: 2020
    2. Date: DEC
    3. Epub Date: 2020 12 02
  2. Journal: Molecules (Basel, Switzerland)
    1. 25
    2. 23
    3. Pages: 5683
  4. Type of Article: Article
  5. Article Number: 5683
  6. ISSN: 1420-3049
  1. Abstract:

    Due to its antiangiogenic and anti-immunomodulatory activity, thalidomide continues to be of clinical interest despite its teratogenic actions, and efforts to synthesize safer, clinically active thalidomide analogs are continually underway. In this study, a cohort of 27 chemically diverse thalidomide analogs was evaluated for antiangiogenic activity in an ex vivo rat aorta ring assay. The protein cereblon has been identified as the target for thalidomide, and in silico pharmacophore analysis and molecular docking with a crystal structure of human cereblon were used to investigate the cereblon binding abilities of the thalidomide analogs. The results suggest that not all antiangiogenic thalidomide analogs can bind cereblon, and multiple targets and mechanisms of action may be involved.

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External Sources

  1. View Full Text
  2. DOI: 10.3390/molecules25235683
  3. PMID: 33276504
  4. View record in Web of Science®
  5. WOS: 000598022600001
  6. PII : molecules25235683

Library Notes

  1. Fiscal Year: FY2020-2021
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