Targeting HIF-2 α in clear cell renal cell carcinoma: A promising therapeutic strategy

Highlights • Antiangiogenic therapies are key therapeutic agents in ccRCC. • The evidence suggests that HIF-2α subunit has a central role in ccRCC over HIF-1α. • PT2385 and PT2399 selectively disrupt the heterodimerization of HIF-2α with HIF-β. • HIF-2α specific antagonists are a promising strategy...

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Bibliographic Details
Published in:	Critical reviews in oncology/hematology Vol. 111; pp. 117 - 123
Main Authors:	Martínez-Sáez, Olga, Borau, Pablo Gajate, Alonso-Gordoa, Teresa, Molina-Cerrillo, Javier, Grande, Enrique
Format:	Journal Article
Language:	English
Published:	Netherlands Elsevier B.V 01-03-2017
Subjects:	Angiogenesis Basic Helix-Loop-Helix Transcription Factors - antagonists & inhibitors Basic Helix-Loop-Helix Transcription Factors - metabolism Carcinoma, Renal Cell - blood supply Carcinoma, Renal Cell - drug therapy Carcinoma, Renal Cell - metabolism Carcinoma, Renal Cell - pathology Dimerization Hematology, Oncology and Palliative Medicine HIF HIF-2α inhibitors Humans Indans - pharmacology Indans - therapeutic use Kidney Neoplasms - blood supply Kidney Neoplasms - drug therapy Kidney Neoplasms - metabolism Kidney Neoplasms - pathology Molecular Targeted Therapy Renal cell carcinoma Sulfones - pharmacology Sulfones - therapeutic use HIF-2α inhibitors renal cell carcinoma HIF angiogenesis Angiogenesis Renal cell carcinoma
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Summary:	Highlights • Antiangiogenic therapies are key therapeutic agents in ccRCC. • The evidence suggests that HIF-2α subunit has a central role in ccRCC over HIF-1α. • PT2385 and PT2399 selectively disrupt the heterodimerization of HIF-2α with HIF-β. • HIF-2α specific antagonists are a promising strategy in the treatment of ccRCC.
Bibliography:	ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-3 content type line 23 ObjectType-Review-1
ISSN:	1040-8428 1879-0461
DOI:	10.1016/j.critrevonc.2017.01.013