KPV

Research Use Only

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KPV Overview

KPV is a small tripeptide derived from the C-terminus of α-MSH that retains signaling activity while lacking melanotropic effects. Through PepT1-mediated uptake in epithelial and macrophage models, KPV directly accesses intracellular compartments where it modulates NF-κB signaling and reduces expression of key cytokines including TNF-α, IL-1β, IL-6, and IL-8. Research models examine KPV's effects on cytokine signaling cascades, epithelial barrier dynamics through tight junction protein regulation, mucosal modeling in experimental systems, and antimicrobial properties in laboratory settings.

History

The cytokine-modulating properties of the KPV sequence were first identified in the late 1980s through structure-activity studies of α-MSH by Hiltz, Lipton, and colleagues. Systematic truncation experiments demonstrated that this C-terminal tripeptide retained significant immunomodulatory activity despite its minimal size, representing the smallest effective sequence for cytokine-modulating action. Subsequent mechanistic studies by Dalmasso et al. in 2008 elucidated the PepT1-mediated epithelial uptake mechanism, establishing KPV's potential for targeting signaling pathways in experimental mucosal models.

Structure

Molecular Formula: C₁₆H₃₀N₄O₄
Molecular Weight: 342.43 g/mol
CAS: 67727-97-3
PubChem CID: 125672

Research Findings

KPV has been extensively studied in cytokine signaling research, with investigations focusing on NF-κB pathway modulation, epithelial signaling models, barrier dynamics, and immune modulation in various experimental systems. Studies examine both its unique transporter-mediated delivery and potent cytokine-modulating mechanisms.

Key Areas of Research:

• Cytokine: NF-κB, MAPK, suppression
• Epithelial: Mucosal signaling, modeling
• Barrier: Tight junction, permeability, integrity
• Immune: Peptide-receptor, macrophage, T-cell

Together, these investigations demonstrate KPV's multifaceted cytokine-modulating actions through PepT1-mediated uptake and direct intracellular signaling modulation. As a minimal bioactive sequence, KPV provides a research framework for examining peptide-based cytokine mechanisms, epithelial immune signaling, and barrier dynamics in diverse experimental models.

References

Dalmasso, G., et al. (2008). PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. Gastroenterology, 134(1), 166–178.

Brzoska, T., Luger, T.A., Maaser, C., Abels, C., & Böhm, M. (2008). Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro and in vivo, and future perspectives for the treatment of immune-mediated inflammatory diseases. Endocrine Reviews, 29(5), 581–602.

Hiltz, M.E., & Lipton, J.M. (1989). Antiinflammatory activity of a COOH-terminal fragment of the neuropeptide alpha-MSH. FASEB Journal, 3(11), 2282–2284.