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 16: Novel Agents: Targets and Mechanisms

Identification of a small molecule inhibitor of hypoxia-inducible factor (HIF) pathway.

Chalet Tan, Anthony J. Roecker, Rita Noronha, Ainsley C. Nicholson, Dawn Post, Wei Zhou, Paraskevi Giannakakou, Kyriacos C. Nicolaou and Erwin G. Van Meir
Chalet Tan
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Anthony J. Roecker
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Rita Noronha
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Ainsley C. Nicholson
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Dawn Post
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Wei Zhou
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Paraskevi Giannakakou
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Kyriacos C. Nicolaou
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Erwin G. Van Meir
Emory University, Atlanta, GA and The Scripps Research Institute, La Jolla, CA.
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
DOI:  Published April 2004
  • Article
  • Info & Metrics
Loading
Proc Amer Assoc Cancer Res, Volume 45, 2004

Abstract

2047

Hypoxia response in solid tumors is largely mediated by the hypoxia inducible factor-1 (HIF-1), a heterodimer composed of oxygen-regulated HIF-1α and constitutively expressed HIF-1β subunits. HIF-1 controls the expression of more than 40 target genes, which plays crucial roles in tumor growth by activating anaerobic metabolism, increasing resistance to apoptosis and the production of angiogenic factors. In human cancers, HIF-1α is overexpressed as a result of intratumoral hypoxia and genetic alterations affecting key oncogenes and tumor suppressor genes. Inhibition of HIF-1 activity is therefore considered as a novel molecular target for tumor therapy. In our laboratory, we have screened a 10,000-membered natural product-like combinatorial library and identified a small molecule which specifically inhibits HIF/HRE pathways. It has low cytotoxicity under normoxia and hypoxia, while specifically decreasing HIF-1α levels in glioma cell lines induced by hypoxia in a dose- and time-dependent manner with IC50 7 μM. This inhibitor could serve as a lead compound for the development of clinically useful agents for cancer therapy targeting tumor hypoxia.

  • American Association for Cancer Research
Previous
Back to top
April 2004
Volume 64, Issue 7 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.
Identification of a small molecule inhibitor of hypoxia-inducible factor (HIF) pathway.
(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
Identification of a small molecule inhibitor of hypoxia-inducible factor (HIF) pathway.
Chalet Tan, Anthony J. Roecker, Rita Noronha, Ainsley C. Nicholson, Dawn Post, Wei Zhou, Paraskevi Giannakakou, Kyriacos C. Nicolaou and Erwin G. Van Meir
Cancer Res April 1 2004 (64) (7 Supplement) 471-472;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Share
Identification of a small molecule inhibitor of hypoxia-inducible factor (HIF) pathway.
Chalet Tan, Anthony J. Roecker, Rita Noronha, Ainsley C. Nicholson, Dawn Post, Wei Zhou, Paraskevi Giannakakou, Kyriacos C. Nicolaou and Erwin G. Van Meir
Cancer Res April 1 2004 (64) (7 Supplement) 471-472;
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

  • Comparative in vitro analysis of C1311 activity in a panel of colorectal cell lines against standard colon cancer chemotherapies.
  • Simvastatin inhibits small cell lung cancer growth in vitro and in vivo: Correlation with selective down regulation of H-Ras.
  • Aplidine potentiates the cytotoxic effect of cytosine arabinoside in experimental leukemia models in vitro and in vivo.
Show more Experimental and Molecular Therapeutics 16: Novel Agents: Targets and Mechanisms
  • 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