Pam3CSK4 TFA is a trifluoroacetate form of Pam3CSK4. Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2 .
Toll-like receptor 2 (TLR2) recognises bacterial lipopeptides and lipoteichoic acid, and forms heterodimers with TLR1 or TLR6. Pam3CSK4 TFA is a trifluoroacetate form of Pam3CSK4. Pam3CSK4 is a TLR1/2 agonist with an EC50 of 0.47 ng/mL for human TLR1/2. Pam3CSK4 is a TLR1/2 heterodimer recognises triacylated lipopeptides. Human TLR2/1, as expected, responded to Pam3CSK4 with greater potency and efficacy than Pam2CSK4[4]. Pretreatment with Pam3CSK4 enhanced the phagocytic and killing activities against MRSA by the GM-CSF induced neutrophils (GM-CSF neutrophils). Chemotaxis of GM-CSF induced neutrophils was significantly increased after the pretreatment with Pam3CSK4. Furthermore, Pam3CSK4 pretreatment enhanced iNOS, CRAMP, TNF-α, IL-1β, IL-10, and IL-6 expression, p38MAPK and Akt phosphorylation kinases were increased significantly in GM-CSF neutrophils pretreatment with Pam3CSK4 in a dose- and time-dependent manner[5]. Pam3CSK4-treated mice also displayed decreased hippocampus neuronal density, and increased cerebral microglia density. Significantly elevated levels of IL-1β, IL-6, KC, and MCP-1 were detected after the first Pam3CSK4 injection in brain homogenates of PND3 mice. Pam(3)CSK(4) administration did not affect long-term memory function nor the volume of gray or white matter[6].
作用机制
Pam3CSK4 mimics the acylated amino terminus of bacterial LPS, which can activate TLRs[7].
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