Human PROKR2

Figure. Concentration-dependent activation of PROKR2 by prokineticin 2

Reporter cells were transfected with either the expression plasmid for human prokineticin receptor 2 (PROKR2) or the mock plasmid and treated with various concentrations of prokineticin 2. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 25 ng/ml.

prokineticin receptor 2
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
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.


  1. 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.
  2. 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.
  3. 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.
  4. Negri L, Lattanzi R, Giannini E, et al. Biological activities of Bv8 analogues. Br J Pharmacol 2005;146:625-32.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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