Drug intelligence / Profile preview

PI3Kγ blocking peptide

Development stage
Preclinical
Lead developer
University of Turin
Modality
Peptides
Administration
Inhalation
01

Overview

PI3Kγ blocking peptide is an experimental synthetic peptide designed to selectively inhibit the non-catalytic, or scaffolding, functions of Phosphatidylinositol 3-kinase gamma (PI3Kγ). Unlike traditional PI3K inhibitors that target the enzyme's catalytic lipid kinase activity, this peptide disrupts the protein-protein interactions mediated by PI3Kγ, such as its association with phosphodiesterase 4 (PDE4) and protein kinase A (PKA). Developed primarily by researchers at the University of Turin and the University of Cologne, the peptide is used as a tool to study the complex roles of PI3Kγ in cardiovascular and inflammatory diseases. In preclinical models of pulmonary hypertension, blocking the non-catalytic function of PI3Kγ has been shown to exacerbate hypoxia-induced pulmonary vascular resistance by reducing nitric oxide synthase (eNOS) activity, suggesting that PI3Kγ's scaffolding role may be protective in certain vascular contexts.

Other names
PI3Kγ scaffold-disrupting peptidePI3Kγ-mimetic peptidePI3Kγ non-catalytic function inhibitor
02

Targets

Phosphoinositide 3-kinase gamma-A-kinase anchoring protein interfacePRKAR1A (cAMP-dependent protein kinase type I-alpha regulatory subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)

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