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

Bruick, Richard K.; Caldwell, Charles G.; Frantz, Doug E.; Gardner, Kevin H.; MacMillan, John B.; Scheuermann, Thomas H.; Tambar, Uttam K.

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

Abstract

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.

Inventors:: Bruick, Richard K.; Caldwell, Charles G.; Frantz, Doug E.; Gardner, Kevin H.; MacMillan, John B.; Scheuermann, Thomas H.; Tambar, Uttam K.

Issue Date:: Tue Sep 12 00:00:00 EDT 2017

Research Org.:: Argonne National Laboratory (ANL), Argonne, IL (United States)

Sponsoring Org.:: USDOE

OSTI Identifier:: 1390247

Patent Number(s):: 9757379

Application Number:: 14/442,485

Assignee:: The Board of Regents of the University of Texas System

Patent Classifications (CPCs):: A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

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A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
A61K31/136 - having the amino group directly attached to the aromatic ring, e.g. benzeneamine
A61K31/4184 - condensed with carbocyclic rings, e.g. benzimidazoles
A61K31/4192 - 1,2,3-Triazoles
A61K31/4245 - Oxadiazoles
A61K31/519 - ortho- or peri-condensed with heterocyclic rings

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
A61P35/00 - Antineoplastic agents

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DOE Contract Number:: AC02-06CH11357

Resource Type:: Patent

Resource Relation:: Patent File Date: 2013 Nov 14

Country of Publication:: United States

Language:: English

Subject:: 59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES

Citation Formats


                    Bruick, Richard K., Caldwell, Charles G., Frantz, Doug E., Gardner, Kevin H., MacMillan, John B., Scheuermann, Thomas H., and Tambar, Uttam K. Inhibition of HIF-2.alpha. heterodimerization with HIF1.beta. (ARNT).  United States: N. p., 2017. 
        Web.

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                    Bruick, Richard K., Caldwell, Charles G., Frantz, Doug E., Gardner, Kevin H., MacMillan, John B., Scheuermann, Thomas H., & Tambar, Uttam K. Inhibition of HIF-2.alpha. heterodimerization with HIF1.beta. (ARNT).  United States.

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                    Bruick, Richard K., Caldwell, Charles G., Frantz, Doug E., Gardner, Kevin H., MacMillan, John B., Scheuermann, Thomas H., and Tambar, Uttam K. Tue .  
        "Inhibition of HIF-2.alpha. heterodimerization with HIF1.beta. (ARNT)".  United States.  https://www.osti.gov/servlets/purl/1390247.

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@article{osti_1390247,

  title        = {Inhibition of HIF-2.alpha. heterodimerization with HIF1.beta. (ARNT)},

  author       = {Bruick, Richard K. and Caldwell, Charles G. and Frantz, Doug E. and Gardner, Kevin H. and MacMillan, John B. and Scheuermann, Thomas H. and Tambar, Uttam K.},

  abstractNote = {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.},

  doi          = {},

  journal      = {},
number       = ,

  volume       = ,

  place        = {United States},

  year         = {Tue Sep 12 00:00:00 EDT 2017},

  month        = {Tue Sep 12 00:00:00 EDT 2017}

}

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Works referenced in this record:

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Ohnishi, Noriyuki; Matsui, Shuichi; Kondo, Tomoyuki
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Triarylmethane Analogs And Their Use In Treating Cancers
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Methods To Regulate Glucose Metabolism
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Kuo, Calvin J.; Wei, Kevin
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Inhibition of Hypoxia Inducible Factor 1—Transcription Coactivator Interaction by a Hydrogen Bond Surrogate α-Helix
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Henchey, Laura K.; Kushal, Swati; Dubey, Ramin
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Artificial ligand binding within the HIF2α PAS-B domain of the HIF2 transcription factor
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Scheuermann, T. H.; Tomchick, D. R.; Machius, M.
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Similar Records

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

Abstract

Citation Formats

Dicyclohexylethylene derivative patent, June 1997

Foreign PAS ligands regulate PAS domain function patent-application, April 2005

Triarylmethane Analogs And Their Use In Treating Cancers patent-application, July 2009

Methods To Regulate Glucose Metabolism patent-application, December 2010

Inhibition of Hypoxia Inducible Factor 1—Transcription Coactivator Interaction by a Hydrogen Bond Surrogate α-Helix journal, January 2010

Dimerization, DNA Binding, and Transactivation Properties of Hypoxia-inducible Factor 1 journal, July 1996

Principles of Ligand Binding within a Completely Buried Cavity in HIF2α PAS-B journal, December 2009

Acriflavine inhibits HIF-1 dimerization, tumor growth, and vascularization journal, October 2009

Inhibition of Hypoxia Inducible Factor-2 Transcription: Isolation of Active Modulators from Marine Sponges journal, August 2012

Targeting the PAS-A Domain of HIF-1α for Development of Small Molecule Inhibitors of HIF-1 journal, July 2006

Artificial ligand binding within the HIF2α PAS-B domain of the HIF2 transcription factor journal, January 2009

Hypoxia-Inducible Factors in Physiology and Medicine journal, February 2012

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

Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2 journal, July 2015

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Structure and Interactions of PAS Kinase N-Terminal PAS Domain journal, October 2002

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patent, June 1997

Foreign PAS ligands regulate PAS domain function
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Triarylmethane Analogs And Their Use In Treating Cancers
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Methods To Regulate Glucose Metabolism
patent-application, December 2010

Inhibition of Hypoxia Inducible Factor 1—Transcription Coactivator Interaction by a Hydrogen Bond Surrogate α-Helix
journal, January 2010

Dimerization, DNA Binding, and Transactivation Properties of Hypoxia-inducible Factor 1
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Principles of Ligand Binding within a Completely Buried Cavity in HIF2α PAS-B
journal, December 2009

Acriflavine inhibits HIF-1 dimerization, tumor growth, and vascularization
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Inhibition of Hypoxia Inducible Factor-2 Transcription: Isolation of Active Modulators from Marine Sponges
journal, August 2012

Targeting the PAS-A Domain of HIF-1α for Development of Small Molecule Inhibitors of HIF-1
journal, July 2006

Artificial ligand binding within the HIF2α PAS-B domain of the HIF2 transcription factor
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Hypoxia-Inducible Factors in Physiology and Medicine
journal, February 2012

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

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journal, July 2015

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journal, October 2002