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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
Country of Publication:
United States
Language:
English

References (12)

Dimerization, DNA Binding, and Transactivation Properties of Hypoxia-inducible Factor 1 journal July 1996
Hypoxia-Inducible Factors in Physiology and Medicine journal February 2012
Acriflavine inhibits HIF-1 dimerization, tumor growth, and vascularization journal October 2009
Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2 journal July 2015
Identification of Cys255 in HIF-1α as a novel site for development of covalent inhibitors of HIF-1α/ARNT PasB domain protein-protein interaction journal November 2012
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
Structure and Interactions of PAS Kinase N-Terminal PAS Domain journal October 2002
Inhibition of Hypoxia Inducible Factor-2 Transcription: Isolation of Active Modulators from Marine Sponges journal August 2012
Inhibition of Hypoxia Inducible Factor 1—Transcription Coactivator Interaction by a Hydrogen Bond Surrogate α-Helix journal January 2010
Artificial ligand binding within the HIF2α PAS-B domain of the HIF2 transcription factor journal January 2009
Targeting the PAS-A Domain of HIF-1α for Development of Small Molecule Inhibitors of HIF-1 journal July 2006
Role of the Development Scientist in Compound Lead Selection and Optimization journal February 2000

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Related Subjects

59 BASIC BIOLOGICAL SCIENCES
60 APPLIED LIFE SCIENCES