- Nomenclature
- prokineticin receptor 2
- Available assay modes
- Agonist, Inverse agonist, Antagonist, PAM, NAM
- Panels
- à la carte, Endocrinology/Metabolism, Neurology, Ophthalmology, Dermatology, Musculoskeletal, Urology/Reproduction, Human non-orphan GPCRs
Prokineticin receptors
Prokineticin receptors, PKR1 and PKR2 respond to the cysteine-rich 81-86 amino-acid peptides prokineticin-1 (also known as endocrine gland-derived vascular endothelial growth factor, mambakine) and prokineticin-2 (protein Bv8 homologue). An orthologue of PROK1 from black mamba (Dendroaspis polylepis) venom, mamba intestinal toxin 1 (MIT1, [1]) is a potent, non-selective agonist at prokineticin receptors [2], while Bv8, an orthologue of PROK2 from amphibians (Bombina sp., [3]), is equipotent at recombinant PKR1 and PKR2 [4], and has high potency in macrophage chemotaxis assays, which are lost in PKR1-null mice.References
- Schweitz H, Pacaud P, Diochot S, et al. MIT(1), a black mamba toxin with a new and highly potent activity on intestinal contraction. FEBS Lett 1999;461:183-8.
- Masuda Y, Takatsu Y, Terao Y, et al. Isolation and identification of EG-VEGF/prokineticins as cognate ligands for two orphan G-protein-coupled receptors. Biochem Biophys Res Commun 2002;293:396-402.
- Mollay C, Wechselberger C, Mignogna G, et al. Bv8, a small protein from frog skin and its homologue from snake venom induce hyperalgesia in rats. Eur J Pharmacol 1999;374:189-96.
- Negri L, Lattanzi R, Giannini E, et al. Biological activities of Bv8 analogues. Br J Pharmacol 2005;146:625-32.
