WO2001077172A3 - Non-endogenous, constitutively activated known g protein-coupled receptors - Google Patents

Non-endogenous, constitutively activated known g protein-coupled receptors Download PDF

Info

Publication number
WO2001077172A3
WO2001077172A3 PCT/US2001/011098 US0111098W WO0177172A3 WO 2001077172 A3 WO2001077172 A3 WO 2001077172A3 US 0111098 W US0111098 W US 0111098W WO 0177172 A3 WO0177172 A3 WO 0177172A3
Authority
WO
WIPO (PCT)
Prior art keywords
endogenous
protein
coupled receptors
constitutively activated
agonists
Prior art date
Application number
PCT/US2001/011098
Other languages
French (fr)
Other versions
WO2001077172A2 (en
Inventor
Karin Lehmann-Bruinsma
Chen W Liaw
I-Lin Lin
Original Assignee
Arena Pharm Inc
Karin Lehmann-Bruinsma
Chen W Liaw
I-Lin Lin
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 Arena Pharm Inc, Karin Lehmann-Bruinsma, Chen W Liaw, I-Lin Lin filed Critical Arena Pharm Inc
Priority to JP2001575642A priority Critical patent/JP2003532057A/en
Priority to EP01923167A priority patent/EP1301594A2/en
Priority to NZ521158A priority patent/NZ521158A/en
Priority to MXPA02009902A priority patent/MXPA02009902A/en
Priority to IL15213601A priority patent/IL152136A0/en
Priority to CA002402392A priority patent/CA2402392A1/en
Priority to AU2001249885A priority patent/AU2001249885A1/en
Publication of WO2001077172A2 publication Critical patent/WO2001077172A2/en
Publication of WO2001077172A3 publication Critical patent/WO2001077172A3/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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones
    • C07K14/723—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH receptor
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/10—Screening for compounds of potential therapeutic value involving cells

Abstract

The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is known ('known GPCRs'), and most particularly to mutated (non-endogenous) versions of the knowns GPCRs for use, most preferably in screening assays for the direct identification of candidate compounds as inverse agonists, agonists and partial agonists.
PCT/US2001/011098 2000-04-07 2001-04-05 Non-endogenous, constitutively activated known g protein-coupled receptors WO2001077172A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
JP2001575642A JP2003532057A (en) 2000-04-07 2001-04-05 Non-endogenous, constitutively activated known G protein-coupled receptor
EP01923167A EP1301594A2 (en) 2000-04-07 2001-04-05 Non-endogenous, consstitutively activated known g protein-coupled receptors
NZ521158A NZ521158A (en) 2000-04-07 2001-04-05 Non-endogenous, constitutively activated known G protein-coupled receptors
MXPA02009902A MXPA02009902A (en) 2000-04-07 2001-04-05 Methods for screening and identifying host pathogen defense genes.
IL15213601A IL152136A0 (en) 2000-04-07 2001-04-05 Non-endogenous, constitutively activated known g protein-coupled receptors
CA002402392A CA2402392A1 (en) 2000-04-07 2001-04-05 Non-endogenous, constitutively activated known g protein-coupled receptors
AU2001249885A AU2001249885A1 (en) 2000-04-07 2001-04-05 Non-endogenous, constitutively activated known g protein-coupled receptors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19574700P 2000-04-07 2000-04-07
US60/195,747 2000-04-07

Publications (2)

Publication Number Publication Date
WO2001077172A2 WO2001077172A2 (en) 2001-10-18
WO2001077172A3 true WO2001077172A3 (en) 2003-01-30

Family

ID=22722621

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/011098 WO2001077172A2 (en) 2000-04-07 2001-04-05 Non-endogenous, constitutively activated known g protein-coupled receptors

Country Status (10)

Country Link
US (3) US6806054B2 (en)
EP (1) EP1301594A2 (en)
JP (1) JP2003532057A (en)
CN (1) CN1420929A (en)
AU (1) AU2001249885A1 (en)
CA (1) CA2402392A1 (en)
IL (1) IL152136A0 (en)
MX (1) MXPA02009902A (en)
NZ (1) NZ521158A (en)
WO (1) WO2001077172A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9562049B2 (en) 2012-12-21 2017-02-07 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases

Families Citing this family (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000189171A (en) 1998-12-25 2000-07-11 Banyu Pharmaceut Co Ltd New guanosine triphosphate(gtp)-binding protein conjugated receptor protein
US20030143668A1 (en) * 2001-06-18 2003-07-31 National Institute Of Advanced Industrial Guanosine triphosphate-binding protein coupled receptors
WO2003023007A2 (en) 2001-09-07 2003-03-20 Bristol-Myers Squibb Company Polynucleotide encoding a novel human g-protein coupled receptor, hgprbmy39
WO2003065006A2 (en) * 2002-01-31 2003-08-07 Millennium Pharmaceuticals, Inc. Methods and compositions for treating cancer
WO2003066672A1 (en) * 2002-02-08 2003-08-14 Nakoshi, Hideo Peptides
CA2483701A1 (en) 2002-04-24 2003-11-06 Banyu Pharmaceutical Co., Ltd. Constitutively active histamine h3 receptor mutants and uses thereof
AU2003240468A1 (en) * 2002-05-02 2003-11-17 Bayer Aktiengesellschaft Diagnostics and therapeutics for diseases associated with neurotensin receptor 2 (nt2)
AU2003229736A1 (en) * 2002-05-02 2003-11-17 Bayer Aktiengesellschaft Diagnostics and therapeutics for diseases associated with neurotensin receptor 1 (nt1)
EP1364968A1 (en) * 2002-05-23 2003-11-26 Bayer Aktiengesellschaft Diagnostics and therapeutics for diseases associated with arginine vasopressin receptor 1 (AVPR1)
EP1365244A1 (en) * 2002-05-23 2003-11-26 Bayer Ag Diagnostics and therapeutics for diseases associated with arginine vasopressin receptor 2 (AVPR2)
EP1365247A1 (en) * 2002-05-23 2003-11-26 Bayer Ag Diagnostics and therapeutics for diseases associated with arginine vasopressin receptor 3 (AVPR3)
SE0202240D0 (en) * 2002-07-17 2002-07-17 Astrazeneca Ab Genes
WO2004071396A2 (en) * 2003-02-17 2004-08-26 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with parathyroid hormone receptor 2 (pthr2)
WO2004073587A2 (en) * 2003-02-19 2004-09-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with parathyroid hormone receptor 1 (pthr1)
US20070276024A1 (en) * 2003-10-09 2007-11-29 Inverseon , Inc. Methods for Treating Diseases and Conditions with Inverse Agonists and for Screening for Agents Acting as Inverse Agonists
EP1684764A2 (en) * 2003-10-09 2006-08-02 Inverseon, Inc. Methods for treating diseases and conditions with inverse agonists and for screening for agents acting as inverse agonists
BR122018071808B8 (en) 2003-11-06 2020-06-30 Seattle Genetics Inc conjugate
AU2003300239A1 (en) 2003-12-29 2005-07-21 Galapagos Genomics N.V. Modulators of bone homeostasis identified in a high-throughput screen
WO2005114206A2 (en) * 2004-05-13 2005-12-01 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with serotonin 5-ht5a receptor (5ht5a)
JP5234734B2 (en) 2004-06-01 2013-07-10 ジェネンテック， インコーポレイテッド Antibody-drug conjugates and methods
EP3088004B1 (en) 2004-09-23 2018-03-28 Genentech, Inc. Cysteine engineered antibodies and conjugates
US20100111856A1 (en) 2004-09-23 2010-05-06 Herman Gill Zirconium-radiolabeled, cysteine engineered antibody conjugates
US7528175B2 (en) * 2004-10-08 2009-05-05 Inverseon, Inc. Method of treating airway diseases with beta-adrenergic inverse agonists
US20070218456A1 (en) * 2006-02-08 2007-09-20 Invitrogen Corporation Cellular assays for signaling receptors
PL2007910T3 (en) * 2006-03-31 2017-04-28 Mobidiag Oy Method and microarray for detecting herpesviruses
DK2216340T3 (en) 2007-10-17 2013-03-11 Univ Cordoba Isoforms of Alternative Treatment Human Type 5 Somatostatin Receptors and Oligonucleotide Pairs for Detection thereof by PCR
RU2010121770A (en) * 2007-10-30 2011-12-10 Интермьюн, Инк. (Us) GENOTYPING AND PHENOTYPING OF HCV
GB0724860D0 (en) * 2007-12-20 2008-01-30 Heptares Therapeutics Ltd Screening
US8470980B2 (en) 2009-09-09 2013-06-25 Centrose, Llc Extracellular targeted drug conjugates
CA2793890C (en) 2010-04-15 2017-08-15 Spirogen Developments Sarl Pyrrolobenzodiazepines and conjugates thereof
JP2013534520A (en) 2010-06-08 2013-09-05 ジェネンテック， インコーポレイテッド Cysteine engineered antibodies and conjugates
US20120121615A1 (en) 2010-11-17 2012-05-17 Flygare John A Alaninyl maytansinol antibody conjugates
EP2707723B1 (en) 2011-05-12 2016-02-10 Genentech, Inc. Multiple reaction monitoring lc-ms/ms method to detect therapeutic antibodies in animal samples using framework signature pepides
CN102276731B (en) * 2011-08-16 2013-03-27 北京大学 High-motion-activity polypeptide capable of inhibiting cocaine induction and application thereof
MX350152B (en) 2011-10-14 2017-08-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof.
WO2013130093A1 (en) 2012-03-02 2013-09-06 Genentech, Inc. Biomarkers for treatment with anti-tubulin chemotherapeutic compounds
DK2906296T3 (en) 2012-10-12 2018-05-22 Adc Therapeutics Sa Pyrrolobenzodiazepine-antibody conjugates
ES2660029T3 (en) 2012-10-12 2018-03-20 Medimmune Limited Antibody-pyrrolobenzodiazepine conjugates
HUE045435T2 (en) 2012-10-12 2019-12-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
CN105050661B (en) 2012-10-12 2018-03-30 Adc疗法责任有限公司 Pyrrolobenzodiazepines Zhuo antibody conjugates
BR112015008173A2 (en) 2012-10-12 2017-11-28 Adc Therapeutics Sarl pyrrolobenzodiazepine-anti-psma antibody conjugates
EP2906250B1 (en) 2012-10-12 2018-05-30 ADC Therapeutics SA Pyrrolobenzodiazepine-anti-psma antibody conjugates
SI2906251T1 (en) 2012-10-12 2018-01-31 Adc Therapeutics Sa Pyrrolobenzodiazepine-anti-cd22 antibody conjugates
WO2014140174A1 (en) 2013-03-13 2014-09-18 Spirogen Sàrl Pyrrolobenzodiazepines and conjugates thereof
WO2014140862A2 (en) 2013-03-13 2014-09-18 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
AU2014244245C1 (en) 2013-03-13 2018-04-19 Genentech, Inc. Pyrrolobenzodiazepines and conjugates thereof
TWI636792B (en) 2013-08-12 2018-10-01 建南德克公司 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment
WO2015052535A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015052532A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
EP3054985B1 (en) 2013-10-11 2018-12-26 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
CN105873614B (en) 2013-12-16 2020-10-30 基因泰克公司 Peptidomimetic compounds and antibody-drug conjugates thereof
EA201691023A1 (en) 2013-12-16 2016-10-31 Дженентек, Инк. PEPTIDOMIMETIC CONNECTIONS AND THEIR CONJUGATES ANTIBODIES WITH MEDICINE
MX2016007578A (en) 2013-12-16 2016-10-03 Genentech Inc 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment.
JP6531166B2 (en) 2014-09-10 2019-06-12 メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ Pyrrolobenzodiazepine and its conjugate
AR101844A1 (en) 2014-09-12 2017-01-18 Genentech Inc ANTIBODIES AND GENETICALLY MODIFIED CONJUGATES WITH CYSTEINE
GB201416112D0 (en) 2014-09-12 2014-10-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
EP3191134B1 (en) 2014-09-12 2019-11-20 Genentech, Inc. Anthracycline disulfide intermediates, antibody-drug conjugates and methods
EP3194400A1 (en) 2014-09-17 2017-07-26 Genentech, Inc. Pyrrolobenzodiazepines and antibody disulfide conjugates thereof
BR112017011111A2 (en) 2014-11-25 2017-12-26 Adc Therapeutics Sa pyrrolobenzodiazepine-antibody conjugates
KR20170086121A (en) 2014-12-03 2017-07-25 제넨테크, 인크. Quaternary amine compounds and antibody-drug conjugates thereof
GB201506411D0 (en) 2015-04-15 2015-05-27 Bergenbio As Humanized anti-axl antibodies
GB201506402D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
MA43345A (en) 2015-10-02 2018-08-08 Hoffmann La Roche PYRROLOBENZODIAZEPINE ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
MA43354A (en) 2015-10-16 2018-08-22 Genentech Inc CONJUGATE DRUG CONJUGATES WITH CLOUDY DISULPHIDE
MA45326A (en) 2015-10-20 2018-08-29 Genentech Inc CALICHEAMICIN-ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
GB201601431D0 (en) 2016-01-26 2016-03-09 Medimmune Ltd Pyrrolobenzodiazepines
GB201602359D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201602356D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
WO2017140803A1 (en) 2016-02-16 2017-08-24 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Modulators of tumor immune resistance for the treatment of cancer
US20190054110A1 (en) 2016-02-16 2019-02-21 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Modulators of ccr9 for treating tumor resistance to immune responses
JP6943872B2 (en) 2016-03-25 2021-10-06 ジェネンテック， インコーポレイテッド Multiple whole antibody and antibody complex drug quantification assay
GB201607478D0 (en) 2016-04-29 2016-06-15 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
PL3458101T3 (en) 2016-05-20 2021-05-31 F. Hoffmann-La Roche Ag Protac antibody conjugates and methods of use
US20170370906A1 (en) 2016-05-27 2017-12-28 Genentech, Inc. Bioanalytical analysis of site-specific antibody drug conjugates
WO2017214024A1 (en) 2016-06-06 2017-12-14 Genentech, Inc. Silvestrol antibody-drug conjugates and methods of use
CN109689111B (en) 2016-08-11 2024-04-05 基因泰克公司 Pyrrolobenzodiazepine prodrugs and antibody conjugates thereof
WO2018065501A1 (en) 2016-10-05 2018-04-12 F. Hoffmann-La Roche Ag Methods for preparing antibody drug conjugates
GB201617466D0 (en) 2016-10-14 2016-11-30 Medimmune Ltd Pyrrolobenzodiazepine conjugates
GB201702031D0 (en) 2017-02-08 2017-03-22 Medlmmune Ltd Pyrrolobenzodiazepine-antibody conjugates
DK3544636T3 (en) 2017-02-08 2021-05-10 Adc Therapeutics Sa Pyrrolobenzodiazepine antibody conjugates
DK3612537T3 (en) 2017-04-18 2022-08-08 Medimmune Ltd PYRROLOBENZODIAZEPIN CONJUGATES
CA3057748A1 (en) 2017-04-20 2018-10-25 Adc Therapeutics Sa Combination therapy with an anti-axl antibody-drug conjugate
KR102442736B1 (en) 2017-06-14 2022-09-16 에이디씨 테라퓨틱스 에스에이 Dosage regime for administration of anti-CD19 ADCs
KR102312910B1 (en) 2017-08-18 2021-10-15 메디뮨 리미티드 Pyrrolobenzodiazepine conjugates
TW201920192A (en) 2017-09-20 2019-06-01 韓商Ｐｈ製藥公司 THAILANSTATIN analogs
GB201803342D0 (en) 2018-03-01 2018-04-18 Medimmune Ltd Methods
GB201806022D0 (en) 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
GB201814281D0 (en) 2018-09-03 2018-10-17 Femtogenix Ltd Cytotoxic agents
CN113056287A (en) 2018-10-24 2021-06-29 豪夫迈·罗氏有限公司 Conjugated chemical degradation inducers and methods of use
WO2020123275A1 (en) 2018-12-10 2020-06-18 Genentech, Inc. Photocrosslinking peptides for site specific conjugation to fc-containing proteins
GB201901197D0 (en) 2019-01-29 2019-03-20 Femtogenix Ltd G-A Crosslinking cytotoxic agents
WO2021011799A1 (en) * 2019-07-16 2021-01-21 Fundación Ciencia Para La Vida (Fcv) Inflammatory bowel diseases therapy involving disrupting ccr9:drd5 heteromer assembly
GB2597532A (en) 2020-07-28 2022-02-02 Femtogenix Ltd Cytotoxic compounds

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995000848A1 (en) * 1993-06-23 1995-01-05 The Regents Of The University Of California Compositions and methods for anti-addictive narcotic analgesis acivity screening and treatments
WO1996037775A1 (en) * 1995-05-22 1996-11-28 The Regents Of The University Of California Methods for g protein coupled receptor activity screening
WO1998031828A1 (en) * 1997-01-22 1998-07-23 Cornell Research Foundation, Inc. Constitutively active g protein coupled receptor of hhv 8 and method
WO1998038217A1 (en) * 1997-02-27 1998-09-03 Milt Teitler Constitutively activated serotonin receptors
WO1999052927A1 (en) * 1998-04-14 1999-10-21 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
WO2000006597A2 (en) * 1998-07-31 2000-02-10 Arena Pharmaceuticals, Inc. Endogenous constitutively activated g protein-coupled orphan receptors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6140509A (en) * 1998-06-26 2000-10-31 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
US6358698B1 (en) * 1998-10-07 2002-03-19 Acadia Pharmacueticals Inc. Methods of identifying inverse agonists of the serotonin 2A receptor
US6150393A (en) * 1998-12-18 2000-11-21 Arena Pharmaceuticals, Inc. Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995000848A1 (en) * 1993-06-23 1995-01-05 The Regents Of The University Of California Compositions and methods for anti-addictive narcotic analgesis acivity screening and treatments
WO1996037775A1 (en) * 1995-05-22 1996-11-28 The Regents Of The University Of California Methods for g protein coupled receptor activity screening
WO1998031828A1 (en) * 1997-01-22 1998-07-23 Cornell Research Foundation, Inc. Constitutively active g protein coupled receptor of hhv 8 and method
WO1998038217A1 (en) * 1997-02-27 1998-09-03 Milt Teitler Constitutively activated serotonin receptors
WO1999052927A1 (en) * 1998-04-14 1999-10-21 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
WO2000006597A2 (en) * 1998-07-31 2000-02-10 Arena Pharmaceuticals, Inc. Endogenous constitutively activated g protein-coupled orphan receptors

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BARR ALASTAIR J ET AL: "Agonist-independent activation of Gz by the 5-hydroxytryptamine1A receptor co-expressed in Spodoptera frugiperda cells. Distinguishing inverse agonists from neutral antagonists.", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 272, no. 52, 26 December 1997 (1997-12-26), pages 32979 - 32987, XP002205336, ISSN: 0021-9258 *
EGAN C ET AL: "CREATION OF A CONSTITUTIVELY ACTIVATED STATE OF THE 5-HT2A RECEPTOR BY SITE-DIRECTED MUTAGENESIS: REVELATION OF INVERSE AGONIST ACTIVITY OF ANTAGONISTS", ANNALS OF THE NEW YORK ACADEMY OF SCIENCES, NEW YORK ACADEMY OF SCIENCES, NEW YORK, NY, US, no. 861, 15 December 1998 (1998-12-15), pages 136 - 139, XP008005349, ISSN: 0077-8923 *
KAWANISHI Y ET AL: "Novel mutations in the promoter and coding region of the human 5-HT1A receptor gene and association analysis in schizophrenia.", AMERICAN JOURNAL OF MEDICAL GENETICS. UNITED STATES 7 SEP 1998, vol. 81, no. 5, 7 September 1998 (1998-09-07), pages 434 - 439, XP008005339, ISSN: 0148-7299 *
LEMBO PAOLA M C ET AL: "Multiple phosphorylation sites are required for pathway-selective uncoupling of the 5-hydroxytryptamine-1A receptor by protein kinase C.", MOLECULAR PHARMACOLOGY, vol. 48, no. 6, 1995, pages 1024 - 1029, XP008005340, ISSN: 0026-895X *
MALMBERG ASA ET AL: "Site-directed mutations in the third intracellular loop of the serotonin 5-HT1A receptor alter G protein coupling from Gi to Gs in a ligand-dependent manner.", JOURNAL OF NEUROCHEMISTRY, vol. 75, no. 3, 2000, pages 1283 - 1293, XP008005342, ISSN: 0022-3042 *
PAUWELS P J ET AL: "REVIEW:AMINO ACID DOMAINS INVOLVED IN CONSTITUTIVE ACTIVATION OF G-PROTEIN-COUPLED RECEPTORS", MOLECULAR NEUROBIOLOGY, HUMANA PRESS, US, vol. 17, no. 1/3, 1998, pages 109 - 135, XP000866477, ISSN: 0893-7648 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9562049B2 (en) 2012-12-21 2017-02-07 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases

Also Published As

Publication number Publication date
AU2001249885A1 (en) 2001-10-23
US7097969B2 (en) 2006-08-29
JP2003532057A (en) 2003-10-28
MXPA02009902A (en) 2003-06-17
NZ521158A (en) 2004-08-27
US6806054B2 (en) 2004-10-19
US20030204073A1 (en) 2003-10-30
US20060183164A1 (en) 2006-08-17
CA2402392A1 (en) 2001-10-18
US20050019840A1 (en) 2005-01-27
IL152136A0 (en) 2003-05-29
WO2001077172A2 (en) 2001-10-18
US7381522B2 (en) 2008-06-03
EP1301594A2 (en) 2003-04-16
CN1420929A (en) 2003-05-28

Similar Documents

Publication Publication Date Title
WO2001077172A3 (en) Non-endogenous, constitutively activated known g protein-coupled receptors
WO2000022131A3 (en) Non-endogenous, constitutively activated human g protein-coupled receptors
WO2000031258A3 (en) Human orphan g protein-coupled receptors
WO2002084286A1 (en) Screening method
WO2003068959A1 (en) Novel screening method
WO2003006996A3 (en) Natural ligand of gpcr chemr23 and uses thereof
WO2002042461A3 (en) Endogenous and non-endogenous versions of human g protein-coupled receptors
EP1412372A4 (en) Endogenous and non-endogenous versions of human g protein-coupled receptors
AU4728799A (en) Bivalent binding molecules of 7 transmembrane g protein-coupled receptors
CO5460266A1 (en) NEW SOMATOSTATINE ANALOGS
WO2007001466A3 (en) Peptidomimetic somatostatin receptor subtype 2 ligands and pet imaging agents
WO2000000611A3 (en) 14273 receptor, a g-protein coupled receptor
WO2005009358A3 (en) Conformationally constrained parathyroid hormone (pth) analogs
WO2001049847A3 (en) 26904, 38911, and 39404, seven-transmembrane proteins/g-protein coupled receptors
ATE464893T1 (en) N,N'-DIARYLGUANIDINE AS IL-8 RECEPTOR ANTAGONISTS
WO1999065942A8 (en) Cyclic somatostatin analogs
WO2003070902A3 (en) Receptors and membrane-associated proteins
WO2002044368A1 (en) Novel g protein-coupled receptor proteins and dnas thereof
EP1676861A3 (en) Non-endogenous, constitutively activated human G protein-coupled receptors
WO2003082320A1 (en) Novel screening method
EP1572913A4 (en) Methods for the identification of novel ligands for the g protein-coupled receptor (gpcr) 192
AU2003303351A1 (en) Chimeric protein for the screening of agonists and antagonists of cell signalling pathways that are dependent on g-protein-coupled receptors
EP1424557A4 (en) Use of g protein-coupled receptor protein
WO2004083394A3 (en) Human g protein-coupled receptors and modulators thereof for the treatment of inflammatory disorders
WO2003008445A1 (en) Novel g protein-coupled receptor protein and dna thereof

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 521158

Country of ref document: NZ

WWE Wipo information: entry into national phase

Ref document number: 2402392

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 018073891

Country of ref document: CN

ENP Entry into the national phase

Ref document number: 2001 575642

Country of ref document: JP

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2001249885

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 152136

Country of ref document: IL

WWE Wipo information: entry into national phase

Ref document number: PA/A/2002/009902

Country of ref document: MX

WWE Wipo information: entry into national phase

Ref document number: 2001923167

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 2001923167

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 521158

Country of ref document: NZ

WWG Wipo information: grant in national office

Ref document number: 521158

Country of ref document: NZ

WWW Wipo information: withdrawn in national office

Ref document number: 2001923167

Country of ref document: EP