Orthosteric and allosteric action of the C5a receptor antagonists

Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727

(2018) Nathan Robertson et al.   NATURE

Randomized Trial of C5a Receptor Inhibitor Avacopan in ANCA-Associated Vasculitis

(2017) David R.W. Jayne et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Complement drives glucosylceramide accumulation and tissue inflammation in Gaucher disease

(2017) Manoj K. Pandey et al.   NATURE

Structural basis for selectivity and diversity in angiotensin II receptors

(2017) Haitao Zhang et al.   NATURE

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

(2017) Jun Lu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

MolProbity: More and better reference data for improved all-atom structure validation

(2017) Christopher J. Williams et al.   PROTEIN SCIENCE

Structural Basis for Apelin Control of the Human Apelin Receptor

(2017) Yingli Ma et al.   STRUCTURE

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

(2017) Jun Lu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Activation mechanism of endothelin ETB receptor by endothelin-1

(2016) Wataru Shihoya et al.   NATURE

C5a and pain development: An old molecule, a new target

(2016) Andreza U. Quadros et al.   PHARMACOLOGICAL RESEARCH

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

(2016) Pirow Bekker et al.   PLoS One

Active immunization against complement factor C5a: a new therapeutic approach for Alzheimer’s disease

(2015) Christine Landlinger et al.   Journal of Neuroinflammation

Effective Application of Bicelles for Conformational Analysis of G Protein-Coupled Receptors by Hydrogen/Deuterium Exchange Mass Spectrometry

(2015) Nguyen Minh Duc et al.   JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY

Two disparate ligand-binding sites in the human P2Y1 receptor

(2015) Dandan Zhang et al.   NATURE

Structural insights into µ-opioid receptor activation

(2015) Weijiao Huang et al.   NATURE

Crystal structure of the chemokine receptor CXCR4 in complex with a viral chemokine

(2015) L. Qin et al.   SCIENCE

Complement C5a Receptor Facilitates Cancer Metastasis by Altering T-Cell Responses in the Metastatic Niche

(2014) S. K. Vadrevu et al.   CANCER RESEARCH

Immunological effects and therapeutic role of C5a in cancer

(2014) Victoria R Darling et al.   Expert Review of Clinical Immunology

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

Targeting the minor pocket of C5aR for the rational design of an oral allosteric inhibitor for inflammatory and neuropathic pain relief

(2014) Alessio Moriconi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of an irreversible HCV NS5B polymerase inhibitor

(2013) Qingbei Zeng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Enhancement of Human Cancer Cell Motility and Invasiveness by Anaphylatoxin C5a via Aberrantly Expressed C5a Receptor (CD88)

(2013) H. Nitta et al.   CLINICAL CANCER RESEARCH

C5L2: a controversial receptor of complement anaphylatoxin, C5a

(2012) Rui Li et al.   FASEB JOURNAL

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

High-resolution crystal structure of human protease-activated receptor 1

(2012) Cheng Zhang et al.   NATURE

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

(2012) W. Liu et al.   SCIENCE

Fusion Partner Toolchest for the Stabilization and Crystallization of G Protein-Coupled Receptors

(2012) Eugene Chun et al.   STRUCTURE

Contribution of complement activation pathways to neuropathology differs among mouse models of Alzheimer's disease

(2011) Maria I Fonseca et al.   Journal of Neuroinflammation

Inhibiting the C5–C5a receptor axis

(2011) Trent M. Woodruff et al.   MOLECULAR IMMUNOLOGY

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Rapid Context-Dependent Ligand Desolvation in Molecular Docking

(2010) Michael M. Mysinger et al.   Journal of Chemical Information and Modeling

Pivotal Advance: Interconversion between pure chemotactic ligands and chemoattractant/secretagogue ligands of neutrophil C5a receptor by a single amino acid substitution

(2010) Nan Jia et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

MolProbity: all-atom structure validation for macromolecular crystallography

(2009) Vincent B. Chen et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Recent developments in low molecular weight complement inhibitors

(2009) Hongchang Qu et al.   MOLECULAR IMMUNOLOGY

The role of the anaphylatoxins in health and disease

(2009) Andreas Klos et al.   MOLECULAR IMMUNOLOGY

Conserved waters mediate structural and functional activation of family A (rhodopsin-like) G protein-coupled receptors

(2009) T. E. Angel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Crystallizing Membrane Proteins for Structure Determination: Use of Lipidic Mesophases

(2008) Martin Caffrey   Annual Review of Biophysics

Modeling Molecular Mechanisms of Binding of the Anaphylatoxin C5a to the C5a Receptor†

(2008) Gregory V. Nikiforovich et al.   BIOCHEMISTRY

Role of the carboxyl terminal di-leucine in phosphorylation and internalization of C5a receptor

(2008) Elena S. Suvorova et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Protein structure and dynamics studied by mass spectrometry: H/D exchange, hydroxyl radical labeling, and related approaches

(2008) Lars Konermann et al.   JOURNAL OF MASS SPECTROMETRY

Identification and Characterization of NDT 9513727 [N,N-bis(1,3-Benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine], a Novel, Orally Bioavailable C5a Receptor Inverse Agonist

(2008) R. M. Brodbeck et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Modulation of the antitumor immune response by complement

(2008) Maciej M Markiewski et al.   NATURE IMMUNOLOGY

Formyl peptide receptor-mediated ERK1/2 activation occurs through Gi and is not dependent on β-arrestin1/2

(2007) Jeannie M. Gripentrog et al.   CELLULAR SIGNALLING