Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism

ter Haar, Ernst; Koth, Christopher M.; Abdul-Manan, Norzehan; Swenson, Lora; Coll, Joyce T.; Lippke, Judith A.; Lepre, Christopher A.; Garcia-Guzman, Miguel; Moore, Jonathan M.

doi:10.1016/j.str.2010.05.014

Title: Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism

Authors:: ter Haar, Ernst; Koth, Christopher M.; Abdul-Manan, Norzehan; Swenson, Lora; Coll, Joyce T.; Lippke, Judith A.; Lepre, Christopher A.; Garcia-Guzman, Miguel; Moore, Jonathan M.

Publication Date:: Wed Sep 01 00:00:00 EDT 2010

Sponsoring Org.:: USDOE

OSTI Identifier:: 1198143

Resource Type:: Published Article

Journal Name:: Structure

Additional Journal Information:: Journal Name: Structure Journal Volume: 18 Journal Issue: 9; Journal ID: ISSN 0969-2126

Publisher:: Elsevier

Country of Publication:: United Kingdom

Language:: English

Citation Formats


                    ter Haar, Ernst, Koth, Christopher M., Abdul-Manan, Norzehan, Swenson, Lora, Coll, Joyce T., Lippke, Judith A., Lepre, Christopher A., Garcia-Guzman, Miguel, and Moore, Jonathan M. Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism.  United Kingdom: N. p., 2010. 
Web.  doi:10.1016/j.str.2010.05.014.

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                    ter Haar, Ernst, Koth, Christopher M., Abdul-Manan, Norzehan, Swenson, Lora, Coll, Joyce T., Lippke, Judith A., Lepre, Christopher A., Garcia-Guzman, Miguel, & Moore, Jonathan M. Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism.  United Kingdom.  https://doi.org/10.1016/j.str.2010.05.014

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                    ter Haar, Ernst, Koth, Christopher M., Abdul-Manan, Norzehan, Swenson, Lora, Coll, Joyce T., Lippke, Judith A., Lepre, Christopher A., Garcia-Guzman, Miguel, and Moore, Jonathan M. Wed .  
"Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism".  United Kingdom.  https://doi.org/10.1016/j.str.2010.05.014.

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@article{osti_1198143,

  title        = {Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism},

  author       = {ter Haar, Ernst and Koth, Christopher M. and Abdul-Manan, Norzehan and Swenson, Lora and Coll, Joyce T. and Lippke, Judith A. and Lepre, Christopher A. and Garcia-Guzman, Miguel and Moore, Jonathan M.},

  abstractNote = {},

  doi          = {10.1016/j.str.2010.05.014},

  journal      = {Structure},

  number       = 9,

  volume       = 18,

  place        = {United Kingdom},

  year         = {Wed Sep 01 00:00:00 EDT 2010},

  month        = {Wed Sep 01 00:00:00 EDT 2010}

}

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Title: Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism

Citation Formats

Crystal Structure of the Ligand-bound Glucagon-like Peptide-1 Receptor Extracellular Domain journal, February 2008

Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine journal, October 2007

Molecular Recognition of Corticotropin-releasing Factor by Its G-protein-coupled Receptor CRFR1 journal, November 2008

Receptor Activity-modifying Protein 1 Determines the Species Selectivity of Non-peptide CGRP Receptor Antagonists journal, April 2002

Protein-Protein Interaction and Not Glycosylation Determines the Binding Selectivity of Heterodimers between the Calcitonin Receptor-like Receptor and the Receptor Activity-modifying Proteins journal, August 2001

Solution structure and mutational analysis of pituitary adenylate cyclase-activating polypeptide binding to the extracellular domain of PAC1-R S journal, May 2007

Cgrp May Play A Causative Role in Migraine journal, February 2002

Treatment of migraine attacks based on the interaction with the trigemino-cerebrovascular system journal, January 2008

Identification and Pharmacological Characterization of Domains Involved in Binding of CGRP Receptor Antagonists to the Calcitonin-like Receptor journal, January 2006

The N-Terminal Extracellular Domain 23−60 of the Calcitonin Receptor-Like Receptor in Chimeras with the Parathyroid Hormone Receptor Mediates Association with Receptor Activity-Modifying Protein 1 journal, March 2005

Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial journal, December 2008

Potent benzimidazolone-based CGRP receptor antagonists journal, December 2008

The extreme N-terminus of the calcitonin-like receptor contributes to the selective interaction with adrenomedullin or calcitonin gene-related peptide journal, October 2002

Non-peptidic antagonists of the CGRP receptor, BIBN4096BS and MK-0974, interact with the calcitonin receptor-like receptor via methionine-42 and RAMP1 via tryptophan-74 journal, January 2010

Crystal structure of the incretin-bound extracellular domain of a G protein-coupled receptor journal, August 2007

Crystal structure of the human receptor activity-modifying protein 1 extracellular domain journal, November 2008

Structure of the N-terminal domain of a type B1 G protein-coupled receptor in complex with a peptide ligand journal, March 2007

CGRP antagonists: unravelling the role of CGRP in migraine journal, November 2007

Mapping interaction sites within the N-terminus of the calcitonin gene-related peptide receptor; the role of residues 23–60 of the calcitonin receptor-like receptor journal, January 2010

Calcitonin Gene–Related Peptide Receptor Antagonist BIBN 4096 BS for the Acute Treatment of Migraine journal, March 2004

NMR structure and peptide hormone binding site of the first extracellular domain of a type B1 G protein-coupled receptor journal, August 2004

CL/RAMP2 and CL/RAMP3 produce pharmacologically distinct adrenomedullin receptors: a comparison of effects of adrenomedullin22-52 , CGRP8-37 and BIBN4096BS journal, October 2003

Refolding and Characterization of a Soluble Ectodomain Complex of the Calcitonin Gene-Related Peptide Receptor journal, March 2010

Binding properties of the novel, non-peptide CGRP receptor antagonist radioligand, [3H]BIBN4096BS journal, May 2002

Caprolactams as potent CGRP receptor antagonists for the treatment of migraine journal, September 2007

Molecular recognition of parathyroid hormone by its G protein-coupled receptor journal, March 2008

Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist journal, February 2000

Identification of the Human Receptor Activity-modifying Protein 1 Domains Responsible for Agonist Binding Specificity journal, June 2003

Examining the binding properties of MK-0974: A CGRP receptor antagonist for the acute treatment of migraine journal, January 2009

The discovery of highly potent CGRP receptor antagonists journal, January 2009

Vasoactive peptide release in the extracerebral circulation of humans during migraine headache journal, August 1990

RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor journal, May 1998

Crystal Structure of the Ligand-bound Glucagon-like Peptide-1 Receptor Extracellular Domain
journal, February 2008

Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine
journal, October 2007

Molecular Recognition of Corticotropin-releasing Factor by Its G-protein-coupled Receptor CRFR1
journal, November 2008

Receptor Activity-modifying Protein 1 Determines the Species Selectivity of Non-peptide CGRP Receptor Antagonists
journal, April 2002

Protein-Protein Interaction and Not Glycosylation Determines the Binding Selectivity of Heterodimers between the Calcitonin Receptor-like Receptor and the Receptor Activity-modifying Proteins
journal, August 2001

Solution structure and mutational analysis of pituitary adenylate cyclase-activating polypeptide binding to the extracellular domain of PAC1-R _S
journal, May 2007

Cgrp May Play A Causative Role in Migraine
journal, February 2002

Treatment of migraine attacks based on the interaction with the trigemino-cerebrovascular system
journal, January 2008

Identification and Pharmacological Characterization of Domains Involved in Binding of CGRP Receptor Antagonists to the Calcitonin-like Receptor
journal, January 2006

The N-Terminal Extracellular Domain 23−60 of the Calcitonin Receptor-Like Receptor in Chimeras with the Parathyroid Hormone Receptor Mediates Association with Receptor Activity-Modifying Protein 1
journal, March 2005

Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial
journal, December 2008

Potent benzimidazolone-based CGRP receptor antagonists
journal, December 2008

The extreme N-terminus of the calcitonin-like receptor contributes to the selective interaction with adrenomedullin or calcitonin gene-related peptide
journal, October 2002

Non-peptidic antagonists of the CGRP receptor, BIBN4096BS and MK-0974, interact with the calcitonin receptor-like receptor via methionine-42 and RAMP1 via tryptophan-74
journal, January 2010

Crystal structure of the incretin-bound extracellular domain of a G protein-coupled receptor
journal, August 2007

Crystal structure of the human receptor activity-modifying protein 1 extracellular domain
journal, November 2008

Structure of the N-terminal domain of a type B1 G protein-coupled receptor in complex with a peptide ligand
journal, March 2007

CGRP antagonists: unravelling the role of CGRP in migraine
journal, November 2007

Mapping interaction sites within the N-terminus of the calcitonin gene-related peptide receptor; the role of residues 23–60 of the calcitonin receptor-like receptor
journal, January 2010

Calcitonin Gene–Related Peptide Receptor Antagonist BIBN 4096 BS for the Acute Treatment of Migraine
journal, March 2004

NMR structure and peptide hormone binding site of the first extracellular domain of a type B1 G protein-coupled receptor
journal, August 2004

CL/RAMP2 and CL/RAMP3 produce pharmacologically distinct adrenomedullin receptors: a comparison of effects of adrenomedullin_22-52 , CGRP_8-37 and BIBN4096BS
journal, October 2003

Refolding and Characterization of a Soluble Ectodomain Complex of the Calcitonin Gene-Related Peptide Receptor
journal, March 2010

Binding properties of the novel, non-peptide CGRP receptor antagonist radioligand, [3H]BIBN4096BS
journal, May 2002

Caprolactams as potent CGRP receptor antagonists for the treatment of migraine
journal, September 2007

Molecular recognition of parathyroid hormone by its G protein-coupled receptor
journal, March 2008

Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist
journal, February 2000

Identification of the Human Receptor Activity-modifying Protein 1 Domains Responsible for Agonist Binding Specificity
journal, June 2003

Examining the binding properties of MK-0974: A CGRP receptor antagonist for the acute treatment of migraine
journal, January 2009

The discovery of highly potent CGRP receptor antagonists
journal, January 2009

Vasoactive peptide release in the extracerebral circulation of humans during migraine headache
journal, August 1990

RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor
journal, May 1998