Research Brief
What Is Kpv?
Resposta Rapida
Visao Geral KPV (Lys-Pro-Val) e um(a) que ocorre naturalmente tripeptide derivado(a) de the C-terminal fragment (aminoacidos 11–13) of alpha-melanocyte-stimulating hormone (α-MSH), a 13-aminoacido POMC-derived neuropeptide.[1][2] Originally caracterizado(a) por James M. Lipton and Melanie E. Hiltz i...
Visao Geral
KPV (Lys-Pro-Val) e um(a) que ocorre naturalmente tripeptide derivado(a) de the C-terminal fragment (aminoacidos 11–13) of alpha-melanocyte-stimulating hormone (α-MSH), a 13-aminoacido POMC-derived neuropeptide.[1][2]
Originally caracterizado(a) por James M. Lipton and Melanie E. Hiltz in 1989, KPV was identificado(a) como the specific molecular fragment responsavel por the parent hormone's anti-inflamatorio(a) and antipyretic activities — the "active message sequence" que retains immunomodulatory and antimicrobial properties enquanto lacking pigment-inducing activity.[7][8]
A critico(a) mechanistic distinction: KPV does not bind melanocortin receptors (MC1R-MC5R) in mammalian cells, nao increase cAMP, and nao induce melanogenesis. Instead, it enters cells via o(a) PepT1 (SLC15A1) oligopeptide transporter — que is notably upregulou in inflamed colonic tissue — enabling targeted delivery to sites of ativo(a) inflamacao.[3][4]
The FDA placed KPV no(a) Categoria 2 Substancia Farmaceutica a Granels list, citing insufficient human exposure data and potential immunogenicity from peptide-related impurities.[5] No large-scale randomizado controlled trials have been published; human data is limited to patent case studies (psoriasis, contact dermatitis).[9]
Referencias
- Sikiric P, et al. A novo(a) gastric juice peptide, BPC. An overview do(a) stomach-stress-organoprotection hypothesis. Journal of Physiology-Paris. 1993;87(5):313-327.
- Brzoska T, Luger TA, Maaser C, Abels C, Böhm M. Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro e em vivo, and future perspectives. Endocrine Reviews. 2008;29(5):581-602.
- Dalmasso G, Charrier-Hisamuddin L, Nguyen HTT, Yan Y, Sitaraman S, Merlin D. PepT1-Mediated Tripeptide KPV Uptake Reduces Intestinal Inflammation. Gastroenterology. 2008;134(1):166-178.
- Laroui H, Dalmasso G, Nguyen HT, Yan Y, Sitaraman SV, Merlin D. Drug-loaded nanoparticles targeted para o(a) colon with polysaccharide hydrogel reduce colitis in a modelo de camundongo. Gastroenterology. 2010;138:843-853.
- U.S. Food and Drug Administration. Certain Substancia Farmaceutica a Granels for Use in Compounding que May Present Significant Safety Risks. FDA.gov. Updated 2023.
- Xiao B, Xu Z, Viennois E, Zhang Y, Zhang Z, Zhang M, Han MK, Kang Y, Merlin D. Orally Targeted Delivery of Tripeptide KPV via Hyaluronic Acid-Functionalized Nanoparticles Efficiently Alleviates Ulcerative Colitis. Molecular Therapy. 2017;25(7):1628-1640.
- Hiltz ME, Lipton JM. Antiinflammatory activity of a COOH-terminal fragment do(a) neuropeptide alpha-MSH. FASEB Journal. 1989;3:2282-2284.
- Luger TA, Brzoska T. α-MSH related peptides: a novo(a) class of anti-inflamatorio(a) and immunomodulating drugs. Annals do(a) Rheumatic Diseases. 2007;66(Suppl 3):iii52-iii55.
- Lipton JM, Catania AP. Use of KPV tripeptide for dermatological disorders. U.S. Patent No. 6,894,028 B2. 2005.
- Getting SJ, Schiöth HB, Perretti M. Dissection do(a) anti-inflamatorio(a) effect do(a) core and C-terminal (KPV) alpha-melanocyte-stimulating hormone peptides. Journal of Pharmacology and Experimental Therapeutics. 2003;306(2):631-637.
- Kelly JM, Moir AJG, Carlson KE, Haycock JW. Immobilized alpha-melanocyte stimulating hormone 10-13 (GKPV) inibe tumor necrose factor-alpha estimulou NF-kappaB activity. Peptides. 2006;27(3):431-437.
- Land SC. Inhibition of cellular and sistemico(a) inflamacao cues in human bronchial celula epitelials by melanocortin-related peptides. International Journal of Physiology, Pathophysiology and Pharmacology. 2012;4(2):59-73.
- Elliott RJ, Szabo M, Wagner MJ, Kemp EH, MacNeil S, Haycock JW. alpha-Melanocyte-stimulating hormone, MSH 11-13 KPV and adrenocorticotropic hormone signalling in human queratinocito cells. Journal of Investigative Dermatology. 2004;122(4):1010-1019.
- Songok AC, Panta P, Doerrler WT, Macnaughtan MA, Taylor CM. Structural modification do(a) tripeptide KPV by reductive glycoalkylation do(a) lysine residue. PLOS One. 2018;13(6):e0199686.
- Kannengiesser K, Maaser C, Heidemann J, et al. Melanocortin-derived tripeptide KPV has anti-inflamatorio(a) potential in murine models of inflammatory bowel disease. Inflammatory Bowel Diseases. 2008;14(3):324-331.
- Böhm M, Luger T. Are melanocortin peptides future therapeutics for cutaneous cicatrizacao de feridas? Experimental Dermatology. 2019;28:219-224.
- Bonfiglio V, et al. Effects do(a) COOH-terminal tripeptide alpha-MSH(11-13) on corneal epitelial cicatrizacao de feridas: role of nitric oxide. Experimental Eye Research. 2006;83(6):1366-1372.
- Shao W, Chen R, Lin G, Ran K, Zhang Y, Yang J, Xu H. In situ mucoadhesive hydrogel capturing tripeptide KPV: the anti-inflamatorio(a), antibacterial and repairing effect on chemotherapy-induziu oral mucositis. Biomaterials Science. 2022;10:227-242.
- Cutuli M, Cristiani S, Lipton JM, Catania A. Antimicrobial effects of alpha-MSH peptides. Journal of Leukocyte Biology. 2000;67(2):233-239.
- Catania A, et al. Three-dimensional structure do(a) α-MSH-derived candidacidal peptide [Ac-CKPV]2. The Journal of Peptide Research. 2005;66(1):19-26.
- Charnley M, Moir AJG, Douglas CWI, Haycock JW. Anti-microbial action of melanocortin peptides and identification of um(a) novo(a) X-Pro-d/l-Val sequence in Gram-positive and Gram-negative bacteria. Peptides. 2008;29(6):1004-1009.
- Land SC, et al. KPV inibe MMP-9 activity and reduz eotaxin and IL-8 secretion in bronchial celula epitelials. International Journal of Physiology, Pathophysiology and Pharmacology. 2012;4(2):59-73.
- Viennois E, et al. Critical Role of PepT1 in Promoting Colitis-Associated Cancer and Therapeutic Benefits do(a) Anti-inflammatory PepT1-Mediated Tripeptide KPV in a Murine Model. Cellular and Molecular Gastroenterology and Hepatology. 2016;2(3):340-357.
- Wu Y, et al. KPV and RAPA Self-Assembled into Carrier-Free Nanodrugs for Vascular Calcification Therapy. Advanced Healthcare Materials. 2024.
- Catania A, et al. Inhibitory effects of o peptideo (CKPV)2 on endotoxin-induziu host reactions. The Journal of Surgical Research. 2006;131.
- Pawar K, Kolli CS, Rangari NS, Babu RJ. Transdermal Iontophoretic Delivery of Lysine-Proline-Valine (KPV) Peptide Across Microporated Human Skin. Journal of Pharmaceutical Sciences. 2017;106(7):1814-1820.
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