a-2-binding peptide

A2-Binding peptide has involved in the assembly of MHC Class I molecules.

PKA inhibitor fragment (6-22) amide Acetate is a synthetic peptide which selectively inhibits PKA activity by binding to its substrate site (IC50 < 2 nM).

Tat-NR2BAA is an inactive control peptide of Tat-NR2B9c. It shares a similar sequence with Tat-NR2B9c, but possesses a double-point mutation in the COOH terminal tSXV motif. This mutation renders Tat-NR2BAA unable to bind PSD-95. Tat-NR2B9c, on the other hand, is a membrane-permeable peptide that interferes with PSD-95 NMDAR binding. This interference leads to the decoupling of NR2B- and or NR2A-type NMDARs from PSD-95[1][2].

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

TLQP-21 TFA, a VGF-derived peptide with endocrine and extraendocrine properties, acts as a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM), activating C3aR1 to increase intracellular Ca2+ levels, and is used in research on nociception regulation and other relevant physiological functions[1][2].

BMSpep-57, a potent macrocyclic peptide inhibitor, competitively disrupts the PD-1 PD-L1 interaction, demonstrating a significant inhibitory concentration (IC50) of 7.68 nM. It exhibits binding affinity towards PD-L1 with dissociation constants (Kd) of 19 nM and 19.88 nM in MicroScale Thermophoresis (MST) and Surface Plasmon Resonance (SPR) assays, respectively. This compound enhances T cell functionality by promoting Interleukin-2 (IL-2) production within Peripheral Blood Mononuclear Cells (PBMCs).

Tyrosinase-related Protein 2 (TRP-2) (181-188) is a peptide derived from TRP-2, specifically corresponding to residues 180-188, and it is the primary epitope within TRP-2 recognized by anti-B16 CTLs. Additionally, it conforms to the binding motif of the MHC class I H2-Kb.

Phytochelatin 2, a short plant peptide, serves as an essential metal-binding compound. Phytochelatins are a diverse group of plant compounds that play a crucial role in chelating metals, safeguarding against metal toxicity, and maintaining metal homeostasis.

Bivalirudin TFA, a synthetic 20-residue peptide, serves as a reversible inhibitor of thrombin. Its IC50 value highlights its target specificity in vitro, where, combined with Eptifibatide (8 mg mL) at a low concentration (70 ng mL), it significantly reduces platelet aggregation induced by thrombin (0.2 U mL) by approximately 90% [1]. The compound demonstrates no effect on thrombin generation assay (TGA) parameters up to 10 μmol L [2]. Additionally, it facilitates the binding of MPO to BAEC, leading to functional alterations such as increased NO consumption and enhanced MPO-mediated redox modifications [3]. In vivo studies reveal its efficacy in preventing the rise of antiheparin PF4 antibody IgG levels in rats, with significant findings from the toxicokinetic assessment signaling its safety profile at tested doses, although higher doses resulted in fatalities [4][5]. In clinical trials, its antithrombotic effects were explored, comparing it with alternatives like Ticagrelor and Clopidogrel in a Phase 4 study.

Nonapeptide-1 (Melanostatine-5) acetate salt is a peptide hormone that functions as a selective and competitive antagonist of the melanocortin 1 receptor (MC1R) with a binding affinity (K i) of 40 nM. It effectively inhibits α-MSH-induced increases in intracellular cyclic AMP (cAMP) and melanosome dispersion in melanocytes, with inhibitory concentrations (IC 50) of 2.5 nM and 11 nM, respectively. By inhibiting melanin synthesis, Nonapeptide-1 acetate salt is used in research related to skin pigmentation, adrenal gland steroid production regulation, and skin cancer [1] [2] [3].

GRGDSPK TFA (EMD 56574 TFA) is a peptide containing the Arg-Gly-Asp (RGD) sequence, serving as a competitive and reversible inhibitor of integrin-fibronectin binding. This compound is utilized in research to elucidate integrins' involvement in bone formation and resorption [1] [2].

M1145 TFA, a chimeric peptide, acts as a selective agonist for the galanin receptor type 2 (GAL2), demonstrating a binding affinity (K i) of 6.55 nM. It exhibits significantly greater selectivity for GAL2, with over 90-fold and 76-fold higher affinity compared to GAL1 (K i = 587 nM) and GalR3 (K i = 497 nM), respectively. Additionally, M1145 TFA enhances galanin signal transduction mechanisms [1].

Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective non-competitive inhibitor of TrkB, effectively impeding BDNF-triggered TrkB activity without altering BDNF binding affinity, with an IC50 of 0.30 nM. It crosses the blood-brain barrier, demonstrating analgesic and anxiolytic-like behavioral effects [1] [2] [3].

IKKγ NBD Inhibitory Peptide TFA is a specific NF-κB inhibitor that hinders the interaction between the IKKγ NEMO-binding domain (NBD) and IKKα and IKKβ, effectively preventing TNF-α-induced NF-κB activation. It has been demonstrated to significantly suppress inflammation and improve neurological deficits induced by cerebral ischemia [1] [2] [3].

hFSH-β-(33-53) TFA, a thiol-containing peptide representing the second follicle-stimulating hormone receptor (FSHR) binding domain, acts as an FSHR antagonist, preventing FSH from binding to its receptor and partially promoting estradiol synthesis in Sertoli cells [1] [2] [3].

(Pro3) GIP, human ((Pro3) Gastric Inhibitory Peptide, human) is a stable and specific full agonist for the human GIP receptor (hGIPR) with a high binding affinity (K i K d values of 0.90 nM), demonstrating efficacy in targeting hGIPR, and is thus suitable for obesity-related diabetes research [1] [2].

Peptide E, a potent kappa opiate receptor agonist, exhibits opiate receptor binding activity with an IC50 value of 0.39 μM, making it valuable for central nervous system research [1] [2].

Protein Kinase C (19-35) Peptide, acting as a PKC pseudosubstrate inhibitor region, can potentially inhibit PKC activity by blocking the substrate-binding site within the kinase domain, thereby inactivating the cytoplasmic form of PKC [1] [2].

Hepatitis B Virus Receptor Binding Fragment (hepatitis B peptide 4980), a synthetic peptide analog, specifically binds to Hep G2 cells and is a potential immunogen expected to induce protective antibodies through the attachment blockade pathway of virus neutralization [1] [2].

ErbB-2-binding peptide (HER2-binding peptide), a tumor-targeting peptide, shows significant potential for cancer research applications [1].

Methionylserine (H-MET-SER-OH), a dipeptide composed of methionine and serine, demonstrates effective binding and translocation through the intestinal di tri-peptide transporter 1 (hPEPT1), possessing a K_m value of 0.2 mM. It also exhibits inhibition of ACE enzyme activity, rendering it useful in hypertension research [1] [2].

PNC-28 acetate, a peptide derived from the mdm-2-binding domain (residues 17–26) of the p53 protein featuring a penetratin sequence for membrane crossing, is utilized in pancreatic cancer research [1] [2].

TfR-T12 TFA, a transferrin receptor (TfR)-binding peptide capable of crossing the blood-brain barrier (BBB), exhibits nanomolar (nM) binding affinity [1] [2].

Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide and synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin on Caco-2 cells [1].