Drug intelligence / Profile preview

Gap19

Development stage
Preclinical
Lead developer
Ghent University
Modality
Peptides
Administration
Intravenous, Intraperitoneal
01

Overview

Gap19 is a synthetic nonapeptide (sequence: KQIEIKKFK) derived from the cytoplasmic loop (CL) of Connexin-43 (Cx43). It acts as a highly selective blocker of Cx43 hemichannels by interfering with the intramolecular interaction between the CL and the C-terminal domain, which is necessary for hemichannel opening. Importantly, Gap19 does not inhibit Cx43 gap junctional communication at concentrations that block hemichannels. It has been extensively studied in preclinical models for its cardioprotective effects against ischemia/reperfusion injury and arrhythmias, particularly in the context of Duchenne Muscular Dystrophy (DMD) and myocardial infarction. It also shows potential in neuroprotection by limiting hemichannel-mediated glutamate release and neuroinflammation.

Other names
Cx43 hemichannel blocker Gap19Cx-43 hemichannel blocker Gap19Cx 43 hemichannel blocker Gap19Gap 19Gap19Gap-19
02

Targets

GJA1 (Connexin43 Hemichannel)

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