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 2017-03, Vol.111, p.117-123
Main Authors: Martínez-Sáez, Olga, Borau, Pablo Gajate, Alonso-Gordoa, Teresa, Molina-Cerrillo, Javier, Grande, Enrique
Format: Article
Language:English
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
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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.
ISSN:1040-8428
1879-0461
DOI:10.1016/j.critrevonc.2017.01.013