Development of Inhibitors Targeting Hypoxia-Inducible Factor 1 and 2 for Cancer Therapy.

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Show simple item record Yu, Tianchi en Tang, Bo en Sun, Xueying en 2020-05-05T21:53:24Z en 2017-05 en
dc.identifier.citation Yonsei medical journal 58(3):489-496 May 2017 en
dc.identifier.issn 0513-5796 en
dc.identifier.uri en
dc.description.abstract Hypoxia is frequently observed in solid tumors and also one of the major obstacles for effective cancer therapies. Cancer cells take advantage of their ability to adapt hypoxia to initiate a special transcriptional program that renders them more aggressive biological behaviors. Hypoxia-inducible factors (HIFs) are the key factors that control hypoxia-inducible pathways by regulating the expression of a vast array of genes involved in cancer progression and treatment resistance. HIFs, mainly HIF-1 and -2, have become potential targets for developing novel cancer therapeutics. This article reviews the updated information in tumor HIF pathways, particularly recent advances in the development of HIF inhibitors. These inhibitors interfere with mRNA expression, protein synthesis, protein degradation and dimerization, DNA binding and transcriptional activity of HIF-1 and -2, or both. Despite efforts in the past two decades, no agents directly inhibiting HIFs have been approved for treating cancer patients. By analyzing results of the published reports, we put the perspectives at the end of the article. The therapeutic efficacy of HIF inhibitors may be improved if more efforts are devoted on developing agents that are able to simultaneously target HIF-1 and -2, increasing the penetrating capacity of HIF inhibitors, and selecting suitable patient subpopulations for clinical trials. en
dc.format.medium Print en
dc.language eng en
dc.relation.ispartofseries Yonsei medical journal en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. en
dc.rights.uri en
dc.rights.uri en
dc.subject Humans en
dc.subject Neoplasms en
dc.subject RNA, Messenger en
dc.subject Antineoplastic Agents en
dc.subject Genes, Tumor Suppressor en
dc.subject Basic Helix-Loop-Helix Transcription Factors en
dc.subject Hypoxia-Inducible Factor 1 en
dc.subject Hypoxia-Inducible Factor 1, alpha Subunit en
dc.subject Transcriptional Activation en
dc.title Development of Inhibitors Targeting Hypoxia-Inducible Factor 1 and 2 for Cancer Therapy. en
dc.type Journal Article en
dc.identifier.doi 10.3349/ymj.2017.58.3.489 en
pubs.issue 3 en
pubs.begin-page 489 en
pubs.volume 58 en
dc.rights.holder Copyright: Yonsei University College of Medicine en
dc.identifier.pmid 28332352 en
pubs.end-page 496 en
pubs.publication-status Published en
dc.rights.accessrights en
pubs.subtype review-article en
pubs.subtype Review en
pubs.subtype Journal Article en
pubs.elements-id 619759 en
dc.identifier.eissn 1976-2437 en
pubs.record-created-at-source-date 2017-03-23 en
pubs.dimensions-id 28332352 en

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