WO2008021552A3 - Biased ligands and methods of identifying same - Google Patents

Biased ligands and methods of identifying same Download PDF

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Publication number
WO2008021552A3
WO2008021552A3 PCT/US2007/018394 US2007018394W WO2008021552A3 WO 2008021552 A3 WO2008021552 A3 WO 2008021552A3 US 2007018394 W US2007018394 W US 2007018394W WO 2008021552 A3 WO2008021552 A3 WO 2008021552A3
Authority
WO
WIPO (PCT)
Prior art keywords
methods
protein
ligands
grk
arrestin
Prior art date
Application number
PCT/US2007/018394
Other languages
French (fr)
Other versions
WO2008021552A9 (en
WO2008021552A2 (en
Inventor
Robert J Lefkowitz
Keshava Rajagopal
Erin J Whalen
Matthew T Drake
Jonathan D Violin
Howard A Rockman
Scott M Dewire
Original Assignee
Univ Duke
Robert J Lefkowitz
Keshava Rajagopal
Erin J Whalen
Matthew T Drake
Jonathan D Violin
Howard A Rockman
Scott M Dewire
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Univ Duke, Robert J Lefkowitz, Keshava Rajagopal, Erin J Whalen, Matthew T Drake, Jonathan D Violin, Howard A Rockman, Scott M Dewire filed Critical Univ Duke
Publication of WO2008021552A2 publication Critical patent/WO2008021552A2/en
Publication of WO2008021552A9 publication Critical patent/WO2008021552A9/en
Publication of WO2008021552A3 publication Critical patent/WO2008021552A3/en

Links

Classifications

    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/726—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH

Abstract

The present invention relates to G protein-coupled receptor ligands having a relative efficacy for stimulating β-arrestin/G protein-coupled receptor kinase (GRK) function (e.g., signaling) that is greater than their relative efficacy for stimulating G-protein signaling function. These 'β-arrestin/GRK biased ligands' can act as agonists or antagonists of G protein-mediated signaling and agonists of β-arrestin/GRK-mediated signal transduction. The invention further relates to methods of identifying such ligands and to methods of using same in a variety of therapeutic settings.
PCT/US2007/018394 2006-08-18 2007-08-20 Biased ligands and methods of identifying same WO2008021552A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83847406P 2006-08-18 2006-08-18
US60/838,474 2006-08-18

Publications (3)

Publication Number Publication Date
WO2008021552A2 WO2008021552A2 (en) 2008-02-21
WO2008021552A9 WO2008021552A9 (en) 2008-05-29
WO2008021552A3 true WO2008021552A3 (en) 2008-11-06

Family

ID=39082807

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/018394 WO2008021552A2 (en) 2006-08-18 2007-08-20 Biased ligands and methods of identifying same

Country Status (1)

Country Link
WO (1) WO2008021552A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009151542A2 (en) * 2008-05-27 2009-12-17 Duke University Nicotinic acid receptor ligands
WO2016196750A1 (en) * 2015-06-03 2016-12-08 Trevena, Inc. Beta-arrestin effectors and compositions and methods of use thereof
WO2017185061A1 (en) 2016-04-21 2017-10-26 Astrocyte Pharmaceuticals, Inc. Compounds and methods for treating neurological and cardiovascular conditions
US11866482B2 (en) 2018-02-07 2024-01-09 Duke University System and method for homogenous GPCR phosphorylation and identification of beta-2 adrenergic receptor positive allosteric modulators
JP7311855B2 (en) 2018-02-09 2023-07-20 アストロサイト ファーマシューティカルズ， インコーポレイテッド Compounds and methods for treating addiction and related disorders
KR20210093864A (en) 2018-09-26 2021-07-28 아스트로사이트 파마슈티컬스, 인코포레이티드 Polymorphic compounds and uses thereof
IL305784A (en) * 2021-03-09 2023-11-01 Chronic Airway Therapeutics Ltd Use of nadolol to treat chronic obstructive pulmonary disease by blockage of the arrestin-2 pathway

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6358990B1 (en) * 1997-10-15 2002-03-19 Boehringer Mannheim Pharmaceuticals Corp. Method for treating Alzheimer's disease
US6673931B2 (en) * 1999-04-27 2004-01-06 Hoffman-La Roche Inc. Naphthalenyl piperidines as renin inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6358990B1 (en) * 1997-10-15 2002-03-19 Boehringer Mannheim Pharmaceuticals Corp. Method for treating Alzheimer's disease
US6673931B2 (en) * 1999-04-27 2004-01-06 Hoffman-La Roche Inc. Naphthalenyl piperidines as renin inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BORRELLO F. ET AL.: "Reappraisal of beta-blocker therapy in the acute and chronic post-myocardial infarction period", no. 4, SUPPL. 3, 2003 *

Also Published As

Publication number Publication date
WO2008021552A9 (en) 2008-05-29
WO2008021552A2 (en) 2008-02-21

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