Drug intelligence / Profile preview

RGS1 palmitoylation-blocking peptide

Development stage
Preclinical
Modality
Peptides
01

Overview

RGS1 palmitoylation-blocking peptide is a novel therapeutic peptide designed to inhibit the post-translational palmitoylation of **Regulator of G-protein signaling 1 (RGS1)**. In the context of acute kidney injury (AKI), extracellular fatty acids in the injury-associated microenvironment induce RGS1 expression and promote its palmitoylation. Palmitoylated RGS1 interacts with and inhibits **Rac1**, a GTPase essential for actin cytoskeletal remodeling during macrophage efferocytosis (the clearance of apoptotic cells). By blocking this modification, the peptide restores Rac1 activity and macrophage efferocytic capacity, leading to reduced proinflammatory cytokine release and accelerated resolution of inflammation and renal tissue repair. The peptide has demonstrated efficacy in murine models of ischemia/reperfusion (I/R)-induced AKI.

Other names
RGS1 palmitoylation inhibitor peptideRGS-1 palmitoylation inhibitor peptideRGS 1 palmitoylation inhibitor peptideRGS1-blocking peptideRGS-1-blocking peptideRGS 1-blocking peptide
02

Targets

RGS1

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