Skip NavigationSkip to Content
Return Return to Search Results

Methoxychalcone inhibitors of androgen receptor translocation and function

  1. Author:
    Kim, Y. S.
    Kumar, V.
    Lee, S.
    Iwai, A.
    Neckers, L.
    Malhotra, S. V.
    Trepel, J. B.

  2. Author Address

    [Kumar, Vineet; Malhotra, Sanjay V.] Natl Canc Inst Frederick, Lab Synthet Chem, Dev Therapeut Program Support, SAIC Frederick, Frederick, MD 21702 USA. [Kim, Yeong Sang; Lee, Sunmin; Trepel, Jane B.] NCI, Med Oncol Branch, NIH, Bethesda, MD 20892 USA. [Iwai, Aki; Neckers, Len] NCI, Urol Oncol Branch, NIH, Bethesda, MD 20892 USA.;Malhotra, SV (reprint author), Natl Canc Inst Frederick, Lab Synthet Chem, Dev Therapeut Program Support, SAIC Frederick, 1050 Boyles St, Frederick, MD 21702 USA;malhotrasa@mail.nih.gov trepelj@mail.nih.gov
    1. Year: 2012
    2. Date: Mar
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 22
    2. 5
    3. Pages: 2105-2109
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    Androgen receptor activity drives incurable castrate-resistant prostate cancer. All approved antiandrogens inhibit androgen receptor-driven transcription, and in addition the second-generation antiandrogen MDV3100 inhibits ligand-activated androgen receptor nuclear translocation, via an unknown mechanism. Here, we report methoxychalcones that lock the heat shock protein 90-androgen receptor complex in the cytoplasm in an androgen-non-responsive state, thus demonstrating a novel chemical scaffold for antiandrogen development and a unique mechanism of antiandrogen activity. Published by Elsevier Ltd.

    See More

  1. Keywords:

External Sources

  1. View Full Text
  2. DOI: 10.1016/j.bmcl.2011.12.141
  3. View record in Web of Science®
  4. WOS: 000300451200053

Library Notes

  1. Fiscal Year: FY2011-2012
NCI at Frederick

You are leaving a government website.

This external link provides additional information that is consistent with the intended purpose of this site. The government cannot attest to the accuracy of a non-federal site.

Linking to a non-federal site does not constitute an endorsement by this institution or any of its employees of the sponsors or the information and products presented on the site. You will be subject to the destination site's privacy policy when you follow the link.

ContinueCancel