Skip to main content
  • AACR Publications
    • Cancer Discovery
    • Cancer Epidemiology, Biomarkers & Prevention
    • Cancer Immunology Research
    • Cancer Prevention Research
    • Cancer Research
    • Clinical Cancer Research
    • Molecular Cancer Research
    • Molecular Cancer Therapeutics

  • Register
  • Log in
Advertisement

Main menu

  • Home
  • About
    • The Journal
    • AACR Journals
    • Subscriptions
    • Permissions and Reprints
    • Reviewing
  • Articles
    • OnlineFirst
    • Current Issue
    • Past Issues
    • Focus on Computer Resources
    • 75th Anniversary
    • Meeting Abstracts
  • For Authors
    • Information for Authors
    • Author Services
    • Best of: Author Profiles
    • Submit
  • Alerts
    • Table of Contents
    • OnlineFirst
    • Editors' Picks
    • Citations
    • Author/Keyword
  • News
    • Cancer Discovery News
  • AACR Publications
    • Cancer Discovery
    • Cancer Epidemiology, Biomarkers & Prevention
    • Cancer Immunology Research
    • Cancer Prevention Research
    • Cancer Research
    • Clinical Cancer Research
    • Molecular Cancer Research
    • Molecular Cancer Therapeutics

User menu

  • Register
  • Log in

Search

  • Advanced search
Cancer Research
Cancer Research

Advanced Search

  • Home
  • About
    • The Journal
    • AACR Journals
    • Subscriptions
    • Permissions and Reprints
    • Reviewing
  • Articles
    • OnlineFirst
    • Current Issue
    • Past Issues
    • Focus on Computer Resources
    • 75th Anniversary
    • Meeting Abstracts
  • For Authors
    • Information for Authors
    • Author Services
    • Best of: Author Profiles
    • Submit
  • Alerts
    • Table of Contents
    • OnlineFirst
    • Editors' Picks
    • Citations
    • Author/Keyword
  • News
    • Cancer Discovery News
Experimental and Molecular Therapeutics

Abstract #4682: BIIB021, a fully synthetic oral small molecule inhibitor of Hsp90, shows anti-tumor activity in multiple xenograft models.

Gerardo Ibanez, Noelito Timple, Samuel Cho, Christina Boykin, Grace Yco, Cindy Yang, Kevin Hong, Hong Zhang, Ingrid Joseph, Laurie Phillips, Chris Storgard and Karen Lundgren
Gerardo Ibanez
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Noelito Timple
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Samuel Cho
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Christina Boykin
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Grace Yco
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Cindy Yang
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Kevin Hong
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Hong Zhang
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Ingrid Joseph
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Laurie Phillips
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Chris Storgard
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Karen Lundgren
Biogen Idec, San Diego, CA
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
DOI:  Published May 2009
  • Article
  • Info & Metrics
Loading
AACR Annual Meeting-- Apr 18-22, 2009; Denver, CO

Abstract

BIIB021 is a novel synthetic oral inhibitor of heat shock protein 90 (Hsp90) that binds competitively in the Hsp90 ATP binding pocket. Hsp90 is a molecular chaperone that functions in the maturation and stabilization of cellular proteins. Hsp90, in complex with other co-chaperone proteins, catalyzes the conformational changes required for \#8220;client\#8221; protein function via its ATPase activity. Mutant and over-expressed oncoproteins that drive malignant progression are particularly dependent on Hsp90 chaperone activity. In tumor cells, inhibition of Hsp90 results in degradation of these proteins followed by cell death making Hsp90 a target of substantial interest for cancer therapy. In cell-based assays with a variety of human cell lines, BIIB021 induced the degradation of HER-2 and other key client proteins including AKT, ERK, Raf-1, and EGFR. BIIB021 also caused upregulation of the expression of Hsp70 in a manner similar to other Hsp90 inhibitors. Oral administration of BIIB021 led to the degradation of HER-2, the induction of apoptosis and the inhibition of tumor growth in human tumor xenograft models that express high levels of HER-2 (BT474 and N87). BIIB021 also showed antitumor activity in the MCF-7 breast cancer xenograft model (that expressed lower levels of HER-2 and is estrogen receptor (ER) and progesterone receptor (PR) positive) and in the mutant EGRF NSCLC model H1650. Furthermore, the oral administration of BIIB021 in combination with molecularly targeted therapies enhanced the activity of monotherapy alone. BIIB021 is a promising new Hsp90 inhibitor that is fully synthetic and designed to be given orally, thereby supporting flexible therapeutic dosing schedules. BIIB021 is currently undergoing Phase 1 and Phase 2 clinical trials in hematological and solid tumors.

Citation Information: In: Proc Am Assoc Cancer Res; 2009 Apr 18-22; Denver, CO. Philadelphia (PA): AACR; 2009. Abstract nr 4682.

Footnotes

  • 100th AACR Annual Meeting-- Apr 18-22, 2009; Denver, CO

  • American Association for Cancer Research
Back to top
Cancer Research: 69 (9 Supplement)
May 2009
Volume 69, Issue 9 Supplement
  • Table of Contents
  • Index by Author

Sign up for alerts

Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Cancer Research article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Abstract #4682: BIIB021, a fully synthetic oral small molecule inhibitor of Hsp90, shows anti-tumor activity in multiple xenograft models.
(Your Name) has forwarded a page to you from Cancer Research
(Your Name) thought you would be interested in this article in Cancer Research.
Citation Tools
Abstract #4682: BIIB021, a fully synthetic oral small molecule inhibitor of Hsp90, shows anti-tumor activity in multiple xenograft models.
Gerardo Ibanez, Noelito Timple, Samuel Cho, Christina Boykin, Grace Yco, Cindy Yang, Kevin Hong, Hong Zhang, Ingrid Joseph, Laurie Phillips, Chris Storgard and Karen Lundgren
Cancer Res May 1 2009 (69) (9 Supplement) 4682;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Share
Abstract #4682: BIIB021, a fully synthetic oral small molecule inhibitor of Hsp90, shows anti-tumor activity in multiple xenograft models.
Gerardo Ibanez, Noelito Timple, Samuel Cho, Christina Boykin, Grace Yco, Cindy Yang, Kevin Hong, Hong Zhang, Ingrid Joseph, Laurie Phillips, Chris Storgard and Karen Lundgren
Cancer Res May 1 2009 (69) (9 Supplement) 4682;
del.icio.us logo Digg logo Reddit logo Twitter logo CiteULike logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
  • Info & Metrics
Advertisement

Related Articles

Cited By...

More in this TOC Section

Experimental and Molecular Therapeutics

  • Abstract SY14-03: Anaplastic lymphoma kinase (ALK): Normal biology and role in hematopoietic malignancies
  • Abstract SY18-01: Targeting the p53-MDM2 interaction for cancer therapy
  • Abstract SSY01-04: Discovery and validation of genome-wide genetic signatures of chemotherapy susceptibility: A translational model
Show more 3

Novel Agents 3 -- Poster Presentations - Proffered Abstracts

  • Abstract #4684: NVP-BEP800 / VER-82576: A potent orally active Hsp90 chaperone inhibitor evolved by SBDD from Vernalis fragment (\#8220;SeeDs\#8221;) hits and in silco screening hits
  • Abstract #4699: In vitro profiling of new targeted anticancer agents using a 30 cell line panel established from the Oncotest patient-derived tumor xenograft collection
  • Abstract #4689: A novel tumor-specific HSP90 inhibitor with long lasting biological activity
Show more 3
  • Home
  • Alerts
  • Feedback
Facebook  Twitter  LinkedIn  YouTube  RSS

Articles

  • Online First
  • Current Issue
  • Past Issues
  • Meeting Abstracts

Info for

  • Authors
  • Subscribers
  • Advertisers
  • Librarians
  • Reviewers

About Cancer Research

  • About the Journal
  • Editorial Board
  • Permissions
  • Submit a Manuscript
AACR logo

Copyright © 2018 by the American Association for Cancer Research.

Cancer Research Online ISSN: 1538-7445
Cancer Research Print ISSN: 0008-5472
Journal of Cancer Research ISSN: 0099-7013
American Journal of Cancer ISSN: 0099-7374

Advertisement