Related Experiment Video
Updated: Aug 16, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Development of C5a receptor antagonists
A K Wong1, S M Taylor, D P Fairlie
1Centre for Drug Design and Development, Department of Physiology and Pharmacology, University of Queensland, Brisbane, Queensland 4072, Australia. ddawong@mailbox.uq.oz.au
Abstract:
During host defense, the human complement system of plasma proteins initiates inflammatory and cellular immune responses to stimuli such as infectious organisms, chemical and physical injury, radiation and neoplasia. Elevated levels of one of these plasma proteins C5a, a 74 amino acid peptidic anaphylatoxin which is one of the most potent pro-inflammatory agents, correlate with the initiation and development of many inflammatory diseases. New agents which prevent binding of C5a to its G-protein-coupled receptors can inhibit the pro-inflammatory actions of C5a and thus be potentially used to treat chronic inflammatory disorders driven by complement activation and C5a production. In recent years significant progress has been made towards the development of potent antagonists of human C5a receptors and clinically useful compounds can reasonably be expected within the next few years.
Related Concept Videos
Antiasthma Drugs: Leukotriene Modifiers
Leukotriene modifiers work through two distinct mechanisms:
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
Antiasthma Drugs: Muscarinic Receptor Antagonists
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
GPCR Desensitization
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
