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Dual action of neurokinin-1 antagonists on Mas-related GPCRs.
It is shown that conventional NK-1R antagonists have off-target activity on the mouse receptor MrgprB2 but not on the homologous human receptor MRGPRX2, and antagonists of MrgPRs may fill the void left by the failure of NK- 1R antagonists.
Cowhage-Evoked Itch Is Mediated by a Novel Cysteine Protease: A Ligand of Protease-Activated Receptors
- V. B. Reddy, Aurel O. Iuga, S. G. Shimada, R. LaMotte, E. Lerner
- BiologyThe Journal of Neuroscience
- 23 April 2008
It is demonstrated that both native and recombinant mucunain evoke the same quality of itch in humans and it is shown that muc unain is a ligand for protease-activated receptors two and four.
Substance P activates Mas‐related G protein–coupled receptors to induce itch
Plant cysteine proteases that evoke itch activate protease‐activated receptors
Background Bromelain, ficin and papain are cysteine proteases from plants that produce itch upon injection into skin. Their mechanism of action has not been considered previously.
Maxadilan, a PAC1 receptor agonist from sand flies
Cathepsin S elicits itch and signals via protease-activated receptors.
- V. B. Reddy, S. G. Shimada, P. Sikand, R. LaMotte, E. Lerner
- BiologyThe Journal of investigative dermatology
- 1 May 2010
Human cathepsin S is focused on because it shares active site sequence homology with mucunain and is selectively up-regulated in human keratinocytes upon stimulation with interferon-gamma, consistent with a possible pruritic role in inflammatory skin disease.
Cathepsin S Signals via PAR2 and Generates a Novel Tethered Ligand Receptor Agonist
It is shown that cathepsin S cleaves near the N-terminus of PAR2 to expose a novel tethered ligand, KVDGTS, which generates downstream signaling events specific to PAR2 but is weaker than SLIGRL.
A single amino acid in MRGPRX2 necessary for binding and activation by pruritogens.
Chrysoptin Is a Potent Glycoprotein IIb/IIIa Fibrinogen Receptor Antagonist Present in Salivary Gland Extracts of the Deerfly*
The results reveal that insect salivary glands are a source of fibrinogen receptor antagonists, and chrysoptin, an inhibitor of ADP-induced platelet aggregation, is a source.
MRGPRX2, atopic dermatitis, and red man syndrome
It is determined that Vancoymycin and staphylococcus-toxin evoke degranulation via interaction with the same receptor, MRGPRX2, on mast cells, and a receptor antagonist inhibits this process.