Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
Journal of Medicinal Chemistry, 2020 Structure-activity relationships for a series of small-molecule thiophenes resulted in potent and selective antagonism of human Complement C3a receptor. The compounds are about 100-fold more potent than the most reported antagonist SB290157.
J. Rowley +11 more
semanticscholar +4 more sources
Regulation of C3a receptor signaling in human mast cells by G protein coupled receptor kinases. [PDF]
PLoS ONE, 2011 The complement component C3a activates human mast cells via its cell surface G protein coupled receptor (GPCR) C3aR. For most GPCRs, agonist-induced receptor phosphorylation leads to receptor desensitization, internalization as well as activation of ...
Qiang Guo +3 more
doaj +4 more sources
C3a receptor blockade protects podocytes from injury in diabetic nephropathy. [PDF]
JCI Insight, 2020 Renal activation of the complement system has been described in patients with diabetic nephropathy (DN), although its pathological relevance is still ill-defined.
Morigi M +10 more
europepmc +2 more sources
Complement peptide C3a receptor 1 promotes optic nerve degeneration in DBA/2J mice. [PDF]
J Neuroinflammation, 2020 The risk of glaucoma increases significantly with age and exposure to elevated intraocular pressure, two factors linked with neuroinflammation. The complement cascade is a complex immune process with many bioactive end-products, including mediators of ...
Harder JM +7 more
europepmc +2 more sources
C3a receptor antagonist therapy is protective with or without thrombolysis in murine thromboembolic stroke. [PDF]
Br J Pharmacol, 2020 Intravenous thrombolysis (IVT) after stroke enhances C3a generation, which may abrogate the benefits of reperfusion. The C3aR antagonist SB290157 is neuroprotective following transient but not permanent middle cerebral artery occlusion (MCAo).
Ahmad S +10 more
europepmc +2 more sources
Knockout of the C3a receptor protects against renal ischemia reperfusion injury by reduction of NETs formation. [PDF]
Cell Mol Life Sci, 2023 Wu X +10 more
europepmc +2 more sources
C3a is made by proximal tubular HK-2 cells and activates them via the C3a receptor [PDF]
Kidney International, 1999 C3a is made by proximal tubular HK-2 cells and activates them via the C3a receptor.BackgroundSome individual components of complement are synthesized by the kidney.
Pussell, Bruce A. +7 more
core +4 more sources
Activated human T lymphocytes express a functional C3a receptor [PDF]
The Journal of Immunology, 2000 The C3a molecule is an anaphylatoxin of the C system with a wide spectrum of proinflammatory effects predominantly an cells of myeloid origin. In this study we investigated the expression of the high affinity receptor for C3a (C3aR) in human T ...
Werfel, T. +7 more
core +6 more sources
Nature Communications, 2017 Complement C3a is an important protein in innate and adaptive immunity, but its roles in vivo are unclear. Here the authors develop novel chemical agonists and antagonists for the C3a receptor, and show that they modulate mast cell degranulation and ...
Rink-Jan Lohman +13 more
doaj +2 more sources
C3a receptor antagonism as a novel therapeutic target for chronic rhinosinusitis. [PDF]
Mucosal Immunol, 2018 Chronic rhinosinusitis with nasal polyps (CRSwNP) is an inflammatory disease with an unknown etiology. Recent studies have implicated the complement system as a potential modulator of disease immunopathology.
Mulligan JK +11 more
europepmc +2 more sources