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)

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].

TAT-CIRP, a trans-activating (Tat) cold-inducible RNA-binding protein-derived peptide, functions as an inhibitor of myeloid differentiation protein 2 (MD2). It has demonstrated significant neuroprotective effects against ischemic and hemorrhagic stroke in mouse models [1].