skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Orthosteric and allosteric action of the C5a receptor antagonists

Journal Article · · Nature Structural & Molecular Biology

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
FOREIGN
OSTI ID:
1502204
Journal Information:
Nature Structural & Molecular Biology, Vol. 25, Issue 6; ISSN 1545-9993
Publisher:
Nature Publishing Group
Country of Publication:
United States
Language:
ENGLISH

References (66)

International Union of Basic and Clinical Pharmacology. LXXXVII. Complement Peptide C5a, C4a, and C3a Receptors journal January 2013
Protein structure and dynamics studied by mass spectrometry: H/D exchange, hydroxyl radical labeling, and related approaches journal August 2008
Role of the carboxyl terminal di-leucine in phosphorylation and internalization of C5a receptor journal June 2008
Crystallizing Membrane Proteins for Structure Determination: Use of Lipidic Mesophases journal June 2009
Crystal structure of the chemokine receptor CXCR4 in complex with a viral chemokine journal January 2015
High-resolution crystal structure of human protease-activated receptor 1 journal December 2012
Comparative Agonist/Antagonist Responses in Mutant Human C5a Receptors Define the Ligand Binding Site journal January 2005
Two-site binding of C5a by its receptor: an alternative binding paradigm for G protein-coupled receptors. journal February 1994
Potent Cyclic Antagonists of the Complement C5a Receptor on Human Polymorphonuclear Leukocytes. Relationships between Structures and Activity journal March 2004
Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40 journal June 2017
Targeting the minor pocket of C5aR for the rational design of an oral allosteric inhibitor for inflammatory and neuropathic pain relief journal November 2014
MolProbity: More and better reference data for improved all-atom structure validation: PROTEIN SCIENCE.ORG journal November 2017
Inhibiting the C5–C5a receptor axis journal August 2011
Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727 journal January 2018
C5a-Stimulated Recruitment of  -Arrestin2 to the Nonsignaling 7-Transmembrane Decoy Receptor C5L2 journal July 2009
Structural basis for selectivity and diversity in angiotensin II receptors journal April 2017
Fusion Partner Toolchest for the Stabilization and Crystallization of G Protein-Coupled Receptors journal June 2012
Complement C5a Receptor Facilitates Cancer Metastasis by Altering T-Cell Responses in the Metastatic Niche journal May 2014
Structure of the agonist-bound neurotensin receptor journal October 2012
Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions journal July 2012
Formyl peptide receptor-mediated ERK1/2 activation occurs through Gi and is not dependent on β-arrestin1/2 journal February 2008
Contribution of complement activation pathways to neuropathology differs among mouse models of Alzheimer's disease journal January 2011
Molecular Characterization of the Gerbil C5a Receptor and Identification of a Transmembrane Domain V Amino Acid That Is Crucial for Small Molecule Antagonist Interaction journal October 2005
Function, structure and therapeutic potential of complement C5a receptors journal October 2007
Discovery of an irreversible HCV NS5B polymerase inhibitor journal December 2013
Activation mechanism of endothelin ETB receptor by endothelin-1 journal September 2016
The role of the anaphylatoxins in health and disease journal September 2009
An Activation Switch in the Ligand Binding Pocket of the C5a Receptor journal November 2000
Active immunization against complement factor C5a: a new therapeutic approach for Alzheimer’s disease journal August 2015
Pivotal Advance: Interconversion between pure chemotactic ligands and chemoattractant/secretagogue ligands of neutrophil C5a receptor by a single amino acid substitution journal January 2010
Identification of a Potent and Orally Active Non-peptide C5a Receptor Antagonist journal October 2002
Structural Basis for Apelin Control of the Human Apelin Receptor journal June 2017
Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse journal September 2006
Structure of a nanobody-stabilized active state of the β2 adrenoceptor journal January 2011
Modulation of the antitumor immune response by complement journal September 2008
Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study journal October 2016
Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists journal October 2010
MolProbity : all-atom structure validation for macromolecular crystallography journal December 2009
Two disparate ligand-binding sites in the human P2Y1 receptor journal March 2015
Coot model-building tools for molecular graphics journal November 2004
Role of c5a in Inflammatory Responses journal April 2005
C5a and pain development: An old molecule, a new target journal October 2016
Crystal structure of the β2 adrenergic receptor–Gs protein complex journal July 2011
Randomized Trial of C5a Receptor Inhibitor Avacopan in ANCA-Associated Vasculitis journal April 2017
Complement drives glucosylceramide accumulation and tissue inflammation in Gaucher disease journal February 2017
Conserved waters mediate structural and functional activation of family A (rhodopsin-like) G protein-coupled receptors journal May 2009
Effective Application of Bicelles for Conformational Analysis of G Protein-Coupled Receptors by Hydrogen/Deuterium Exchange Mass Spectrometry journal March 2015
PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010
Low-Molecular-Weight Peptidic and Cyclic Antagonists of the Receptor for the Complement Factor C5a journal June 1999
Mapping the Ligand-Binding Site on the C5a Receptor:  Arginine 74 of C5a Contacts Aspartate 282 of the C5a Receptor journal November 2001
Rapid Context-Dependent Ligand Desolvation in Molecular Docking journal August 2010
Constitutive Activation and Endocytosis of the Complement Factor 5a Receptor: Evidence for Multiple Activated Conformations of a G Protein-Coupled Receptor journal December 2002
Molecular control of δ-opioid receptor signalling journal January 2014
C5a Receptor Activation: GENETIC IDENTIFICATION OF CRITICAL RESIDUES IN FOUR TRANSMEMBRANE HELICES journal May 1999
Biologically Active Conformer of the Effector Region of Human C5a and Modulatory Effects of N-Terminal Receptor Binding Determinants on Activity journal March 1997
Recent developments in low molecular weight complement inhibitors journal December 2009
Structural insights into µ-opioid receptor activation journal August 2015
Identification and Characterization of NDT 9513727 [ N , N -bis(1,3-Benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1 H -imidazole-5-methanamine], a Novel, Orally Bioavailable C5a Receptor Inverse Agonist journal August 2008
Enhancement of Human Cancer Cell Motility and Invasiveness by Anaphylatoxin C5a via Aberrantly Expressed C5a Receptor (CD88) journal January 2013
Modeling Molecular Mechanisms of Binding of the Anaphylatoxin C5a to the C5a Receptor journal March 2008
Identification of Phosphorylation Codes for Arrestin Recruitment by G Protein-Coupled Receptors journal July 2017
C5L2: a controversial receptor of complement anaphylatoxin, C5a journal March 2013
[20] Processing of X-ray diffraction data collected in oscillation mode book January 1997
C5a Receptor Oligomerization: I. DISULFIDE TRAPPING REVEALS OLIGOMERS AND POTENTIAL CONTACT SURFACES IN A G PROTEIN-COUPLED RECEPTOR journal June 2003
Immunological effects and therapeutic role of C5a in cancer journal November 2014
Phaser crystallographic software journal July 2007

Similar Records

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists
Journal Article · Wed Dec 07 00:00:00 EST 2016 · Nature (London) · OSTI ID:1502204

Crystal structure of the adenosine A2A receptor bound to an antagonist reveals a potential allosteric pocket
Journal Article · Mon Feb 06 00:00:00 EST 2017 · Proceedings of the National Academy of Sciences of the United States of America · OSTI ID:1502204

Dihydromorphine-peptide hybrids with delta receptor agonistic and mu receptor antagonistic actions
Journal Article · Wed Mar 05 00:00:00 EST 1986 · Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) · OSTI ID:1502204

Related Subjects