This review provides a comprehensive overview of human C5a in the context of its structure and signaling under several pathophysiological conditions, including the current and future therapeutic applications targeting C5a.

Complement activation ultimately leads to the formation of C5a and its interaction with its two receptors, C5aR and C5L2, activating signaling pathways that are important in defending against pathogens and maintaining homeostasis.

Feb 17, 2023 · We solved cryo-electron microscopy (cryo-EM) structures of activated wild-type C5aR1–G i protein bound to each of C5a, the hexapeptidic agonist C5a pep (which has functional bias in terms of...

C5a is a protein fragment released from cleavage of complement component C5 by protease C5-convertase into C5a and C5b fragments.

C5aR2 was not found on the cell surface and its intracellular pool made no contribution to C5a sequestration from the extracellular space. Authors concluded that instead of being the proposed C5a-scavenging receptor, C5aR2 may function in modulating C5a signaling.

Oct 17, 2023 · A series of cryo-EM structures offer insights into how anaphylatoxins C3a and C5a engage complement receptors, illustrating agonist binding modes, pathways of receptor activation, and signaling bias that should facilitate the discovery of ligands and therapeutic candidates targeting these receptors.

C5a binds to at least two seven-transmembrane domain receptors, C5aR (C5R1, CD88) and C5L2 (gpr77), expressed ubiquitously on a wide variety of cells but particularly on the surface of immune cells like macrophages, neutrophils and T cells.

The complement fragment C5a is one of its important effector components and exerts diverse physiological functions through activation of the C5a receptor 1 (C5aR1) and associated downstream G protein and β-arrestin signaling pathways.

May 11, 2023 · The complement receptors C3aR and C5aR1, whose signaling is selectively activated by anaphylatoxins C3a and C5a, are important regulators of both innate and adaptive immune responses.

May 10, 2020 · Complement factor C5a is an integral constituent of the complement cascade critically involved in the innate immune response, and it exerts its functions via two distinct receptors, C5aR1 and C5aR2.