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Title: Inhibition of HIF-2.alpha. heterodimerization with HIF1.beta. (ARNT)

Patent ·
OSTI ID:1390247
; ; ; ; ; ;

Provided is a method of inhibiting heterodimerization of HIF-2.alpha. to HIF1.beta. (ARNT) comprising binding certain small molecules to the HIF-2.alpha. PAS-B domain cavity but not to HIF1.alpha. and inhibiting HIF-2.alpha. heterodimerization to HIF1.beta. (ARNT) but not inhibiting HIF1.alpha. heterodimerization to HIF1.beta. (ARNT). Those certain small molecules are also referenced synonymously as HIF2-HDI and HIF2.alpha. heterodimerization inhibitors and also simply as certain small molecules.

Research Organization:
Argonne National Laboratory (ANL), Argonne, IL (United States)
Sponsoring Organization:
USDOE
DOE Contract Number:
AC02-06CH11357
Assignee:
The Board of Regents of the University of Texas System
Patent Number(s):
9,757,379
Application Number:
14/442,485
OSTI ID:
1390247
Resource Relation:
Patent File Date: 2013 Nov 14
Country of Publication:
United States
Language:
English

References (16)

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Principles of Ligand Binding within a Completely Buried Cavity in HIF2α PAS-B
  • Key, Jason; Scheuermann, Thomas H.; Anderson, Peter C.
  • Journal of the American Chemical Society, Vol. 131, Issue 48, p. 17647-17654 https://doi.org/10.1021/ja9073062
journal December 2009
Acriflavine inhibits HIF-1 dimerization, tumor growth, and vascularization journal October 2009
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Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2 journal July 2015
Role of the Development Scientist in Compound Lead Selection and Optimization journal February 2000
Structure and Interactions of PAS Kinase N-Terminal PAS Domain journal October 2002

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Related Subjects

59 BASIC BIOLOGICAL SCIENCES
60 APPLIED LIFE SCIENCES