Inhibitors
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Inhibitors

Introduction Nociceptin/orphanin FQ (N/OFQ) modulates various biological functions, including nociception, via selective stimulation of the N/OFQ peptide receptor (NOP). UFP-101 is a novel NOP ligand designed to bind [Nphe1] chemically in the same molecule, eliminating potency and the [Arg14, Lys15] substitution increases ligand potency and duration of action in vivo.

Introduction ICl 154,129 is a new compound that shows selectivity as an antagonist of [Leu5]enkephalin and [D-AIa2, D-Leu5]enkephalin at opiate receptors in the mouse vas deferens preparation. The recent finding shows that ICI 154,129 is active in rats in a novel model of delta receptor activation.

Introduction In the respiratory tract, there are tachykinin P (SP) and neurokinin A (NKA) in capsaicin-sensitive primary afferent neurons. Bradykinin has various effects such as bronchoconstriction, mucus secretion, and plasma spillover.

Introduction Tandem P-domain weak inward rectifying K+ (TWIK)-related K+ channel 1 (TREK-1) and TWIK-related acid-sensitive K+ channel 3 (TASK-3) have been proposed to be related to depression. TREK-1 and TASK-3 antagonists are thought as the new potential treatments for depression.

Introduction The voltage-gated Kv1.3 channel in effector memory T cells serves as a new therapeutic target for multiple sclerosis. The molecular weight of ADWX-1 is 4072.8 Da and the ADWX-1 peptide blocked Kv1.

Introduction Orexin A (OXA) and orexin B (OXB) are hypothalamic neuropeptides discovered in 1998, which bind to two G-protein coupled receptors (GPCRs), namely orexin receptor 1 (OX1) and orexin receptor 2 (OX2).

Introduction The peptide st-Ht31 P, A-kinase anchoring protein (AKAP) inhibitor, has the negative control for st-Ht31. In DRG sensory neurons, the st-Ht31 P attenuated forskolin-stimulated translocation of the protein kinase A (PKA) catalytic subunit to the plasma membrane.

Introduction The sodium channel subtypes NaV1.2 and NaV1.6 are the two major forms of excitatory pyramidal neurons in the cerebral cortex, with local specificity that can be combined with the initiation and spread of action potentials (APs).

Introduction Guangxitoxin 1E is a KV2.1 and KV2.2 specific channel blocker (IC50 values are 1-3 nM). The experimental results showed that it enhances glucose-stimulated insulin secretion from human islets in vitro, but not from islet cells lacking the KV2.

Introduction  ClC-2 chloride channels are voltage-gated ion channels that are expressed in neuronal and epithelial cells where they are critical mediators for the passive diffusion of Cl across the plasma membrane.

Introduction The serine/threonine kinase Pim-1 plays an important role in cell cycle progression and apoptosis inhibition, resulting in prostate tumorigenesis. Therefore, Pim-1 inhibition has been expected to be an attractive target for developing new anti-cancer drugs.

Introduction Acid-sensitive ion channels (ASICs) are a class of proton-gated ion channels belonging to the Degenerin/Epithelial sodium channel family (Deg/ENaC) with four encoded genes: ASIC1, ASIC2, ASIC3, ASIC4.

Introduction PMX-53, a chemically synthesized peptide material, is a potent C5a antagonist in human neutrophils and macrophages in vitro, aiming to protect rodents from a number of experimental inflammatory diseases.

Introduction Pep2m, a peptide inhibitor of GluA2 subunit binding to NSF, reduces α-amino- 3-hydroxy-5-methyl-isoxazolepropionate (AMPA) currents.Pharmacologic actionBy infusion into cultured hippocampal neurons of a blocking peptide (pep2m), the disruption of N-ethylmaleimide-sensitive fusion protein– (NSF–) GluR2 interaction causes a rapid decrease in the frequency without change in the amplitude of AMPA receptor–mediated miniature excitatory postsynaptic currents (mEPSCs).

Introduction Galanin-(2–13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide (M871) is a novel peptide antagonist selectively recognizing the galanin receptor type 2. Galanin (GAL) and its three receptors have been linked to a wide variety of physiological processes and are distributed in both the central and peripheral nervous systems.

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