Target intelligence / Profile preview

C5a anaphylatoxin chemotactic receptor 1 (C5AR1)

Target
C5AR1
Molecular classification
G protein-coupled receptor
01

Overview

C5a anaphylatoxin chemotactic receptor 1 (C5AR1), also known as CD88, is a G protein-coupled receptor (GPCR) that serves as the primary receptor for complement component 5a (C5a), a potent pro-inflammatory peptide generated during activation of the complement system. It plays a central role in mediating immune and inflammatory responses. Activation leads to chemotaxis, cytokine release and modulation of cellular processes. Dysregulation is implicated in various diseases.

Other names
CD88C5aRC5R1
02

Mechanism of action

Agonists stimulate C5AR1, activating G proteins and downstream signaling pathways (e.g., calcium mobilization, ERK1/2 phosphorylation). Antagonists block C5a binding and subsequent receptor activation.

03

Biological functions

Immune cell chemotaxisInflammatory response modulationSignal transduction
04

Disease associations

SepsisAsthmaCancer progression/metastasisNeuropathic painObesityCardiac regeneration
05

Safety considerations

Overactivation can lead to excessive inflammation and tissue damage.Targeted inhibition may compromise protective immunity.
06

Interacting drugs

Paclitaxel

2 more in the full profile.

07

Biomarkers

C5AR1 expression levels in cancer cells (e.g., non-small cell lung cancer)

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