Delving into the Latest Updates on F2Pal16 pepducins with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms-

Target

FPR2

Action

modulators

Mechanism

FPR2 modulators(N-formyl peptide receptor 2 modulators)

Therapeutic Areas

Infectious Diseases

Active Indication-

Inactive Indication

Bacterial Infections

Originator Organization

University of Gothenburg

Active Organization-

Inactive Organization

University of Gothenburg

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Pepducins containing a fatty acid linked to an amino acid sequence derived from cytosolic parts of a G-protein-coupled receptor (GPCR) constitute a new group of lipopeptide tools in GPCR studies. Pepducins corresponding to the third intracellular loop of formyl peptide receptor 2 (FPR2) activate human neutrophils, and we show here that, in addition, these allosteric modulators of receptor activity also kill bacteria. The functional dualism of FPR2 pepducins could potentially be explored as a novel class of antibacterial drugs with immunomodulatory properties.

24 Sep 2010·FEBS lettersQ3 · BIOLOGY

Activation of human monocytes by a formyl peptide receptor 2‐derived pepducin

Q3 · BIOLOGY

Article

Author: Joon Seong Park ; Jae Woong Shim ; Ha Young Lee ; Jae Young Kwon ; Hak Jung Kim ; Sang Doo Kim ; Jong-Min Kim ; Yoe-Sik Bae ; Suk-Hwan Baek

We synthesized and investigated the effect of formyl peptide receptor 2 (FPR2)‐derived pepducins in human monocytes. The FPR2‐based cell‐penetrating lipopeptide, “pepducin” (F2pal‐16), stimulated intracellular calcium increase in human monocytes via pertussis toxin (PTX)‐sensitive G‐protein and phospholipase C (PLC) activity. From a functional aspect, we showed that F2pal‐16 stimulated monocyte chemotaxis. F2pal‐16 also stimulated the generation of superoxide anion in human monocytes. Moreover, F2pal‐16 dramatically increased the production of several kinds of pro‐inflammatory cytokines (CXCL8, CCL2, IL‐1β and TNF‐α) in human monocytes via NF‐κB activation. Since FPR2 plays an important role in immune responses, F2pal‐16 can serve as a useful reagent for the study of FPR2‐mediated immune modulation.

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Preclinical	Sweden	University of Gothenburg	26 Feb 2014

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