F2Pal16 pepducins(F2Pal16 pepducins) - 药物靶点：FPR2_专利_临床

概要

基本信息

药物类型

合成多肽

别名-

靶点

FPR2

作用方式

调节剂

作用机制

FPR2调节剂(N-formyl peptide receptor 2 modulators)

治疗领域

感染

在研适应症-

非在研适应症

细菌感染

原研机构

University of Gothenburg

在研机构-

非在研机构

University of Gothenburg

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 F2Pal16 pepducins 相关的临床结果

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100 项与 F2Pal16 pepducins 相关的转化医学

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100 项与 F2Pal16 pepducins 相关的专利（医药）

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2

项与 F2Pal16 pepducins 相关的文献（医药）

2014-05-01·Antimicrobial agents and chemotherapy2区 · 医学

Antibacterial Activity of Pepducins, Allosterical Modulators of Formyl Peptide Receptor Signaling

2区 · 医学

Article

作者: Gabl, Michael ; Oprea, Tudor I. ; Boulay, Francois ; Jönsson, Bodil ; Winther, Malene ; Bylund, Johan ; Dahlgren, Claes ; Forsman, Huamei

ABSTRACT:

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.

2010-09-24·FEBS letters3区 · 生物学

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

3区 · 生物学

Article

作者: Joon Seong Park ; Jae Woong Shim ; Ha Young Lee ; Hak Jung Kim ; Jae Young Kwon ; 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.

100 项与 F2Pal16 pepducins 相关的药物交易

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