Immune regulation, inflammation, cytokine balance
Immunomodulation.
Peptides that have shown immunomodulatory or inflammation-modulating effects in preclinical studies. Includes thymosin derivatives and tuftsin analogs.
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BPC-157
Body Protection Compound 157
BPC-157 is a synthetic pentadecapeptide derived from a partial sequence of a human gastric juice protein. In preclinical studies, interactions with the NO system (nitric oxide signalling pathway) and with the EGR1 and VEGFR2 receptor pathways have been described, which may mediate angiogenic and cytoprotective effects. The precise mechanisms of action in humans have not been conclusively established.
TB-500
Thymosin Beta-4
TB-500 (as a synthetic analog of thymosin beta-4, a naturally occurring peptide) interacts with G-actin and regulates actin polymerisation in cells. Thymosin beta-4 is expressed endogenously in high concentrations in platelets and other cells and is involved in cell migration, proliferation and differentiation. Preclinical studies suggest interactions with angiogenic and inflammation-modulating signalling pathways. The term 'TB-500' is a trade designation for a synthetic fragment analog and is not identical to native thymosin beta-4.
Selank
TP-7
Selank is a synthetic heptapeptide, likewise developed at the Institute of Molecular Genetics of the Russian Academy of Sciences. It is based on the sequence of the endogenous immunomodulator tuftsin (Thr-Lys-Pro-Arg) with a C-terminal Pro-Gly-Pro extension for enzymatic stabilisation. In preclinical studies, anxiolytic effects without sedative properties have been described — compared with benzodiazepines, no GABA-A modulatory mechanism was demonstrated. Possible mechanisms discussed include modulation of the serotonergic system, inhibition of enkephalin degradation, and immunomodulatory effects via tuftsin receptors.
LL-37
Cathelicidin
LL-37 is the only human cathelicidin — a 37-amino-acid peptide produced by proteolytic cleavage from the precursor protein hCAP-18. It acts directly antimicrobially by destabilising bacterial cell membranes (cationic charge + amphipathic helical structure). In addition, LL-37 has immunomodulatory functions: it activates Toll-like receptors (TLR), promotes the chemotaxis of immune cells, stimulates angiogenesis via VEGFR-2 and accelerates wound healing. LL-37 is produced mainly in neutrophils, mast cells and epithelial cells — especially after tissue injury or infection.
Thymosin Alpha-1
Tα1
Thymosin alpha-1 (Tα1) is a 28-amino-acid peptide originally isolated as fraction 5 from the thymus. It is a natural cleavage product of prothymosin alpha and is produced mainly in thymic epithelial cells. Tα1 modulates T-cell maturation and function: it promotes the Th1 response, increases the activity of natural killer cells (NK cells) and stimulates the production of IL-2, interferon-gamma and interferon-alpha. Its molecular site of action includes Toll-like receptors (TLR2 and TLR9) on dendritic cells, which explains its activation of the adaptive immune response.
VIP
Vasoaktives Intestinales Peptid
VIP is a 28-amino-acid neuropeptide of the secretin/glucagon superfamily, produced throughout the nervous system as well as in intestinal, respiratory and immunological tissues. VIP binds the G-protein-coupled receptors VPAC1 and VPAC2, which via cAMP signalling pathways leads to vasodilation, bronchodilation and pronounced immunomodulation. Immunologically, VIP inhibits the production of pro-inflammatory cytokines (TNF-α, IL-6, IL-12) and promotes regulatory T cells (Tregs) as well as anti-inflammatory mediators (IL-10). In the lung and gut, VIP also acts as a neuroprotective and epithelium-protecting mediator.
KPV
Lys-Pro-Val
KPV is a tripeptide (lysine-proline-valine) corresponding to the C-terminal end of α-melanocyte-stimulating hormone (α-MSH). While the full α-MSH (13 amino acids) is strongly pigmenting and binds MC1R/MC3R, the KPV fragment exerts its anti-inflammatory effects via mechanisms that are partly independent of melanocortin receptors. KPV inhibits NF-κB signalling pathways in intestinal epithelial cells and immune cells, reduces the release of pro-inflammatory cytokines (IL-8, TNF-α) and appears able to enter inflammatory cells directly. Owing to its small size (tripeptide), KPV shows good intestinal stability.
ARA 290 (Cibinetid)
ARA 290
ARA 290 (cibinetide) is a short peptide derived from helix B of erythropoietin (EPO). It binds to the so-called innate repair receptor (a complex of the EPO receptor and the β-common receptor subunit) without having the erythropoietic (blood-forming) action of EPO. Tissue-protective and inflammation-modulating effects have been described. The focus is on neuropathic and inflammatory conditions.
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