User:Anat Levit/Sandbox 1
From Proteopedia
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<applet load='FILE_consurf1254065510_pipe.pdb' size='400' frame='true' align='right' caption='Human PROKR1' /> | <applet load='FILE_consurf1254065510_pipe.pdb' size='400' frame='true' align='right' caption='Human PROKR1' /> | ||
| - | PKs exert their biological function through activation of two homologous G-protein coupled receptors (see Wikipedia: [http://en.wikipedia.org/wiki/G_protein_coupled_receptors G protein-coupled receptors]), termed Prokineticin receptor 1 (PROKR1) and Prokineticin receptor 2 (PROKR2). These receptors share <scene name='User:Anat_Levit/Sandbox_1/Pkr_colored_by_homology/ | + | PKs exert their biological function through activation of two homologous G-protein coupled receptors (see Wikipedia: [http://en.wikipedia.org/wiki/G_protein_coupled_receptors G protein-coupled receptors]), termed Prokineticin receptor 1 (PROKR1) and Prokineticin receptor 2 (PROKR2). These receptors share |
| + | <scene name='User:Anat_Levit/Sandbox_1/Pkr_colored_by_homology/4'>85% sequence homology</scene>, which is a high value among known GPCRs. The proteins diverse mainly in their extra and intra-cellular tails. | ||
Revision as of 14:10, 6 October 2009
Prokineticin 1 (PK1) and its close homologue PK2 are two secreted proteins, which belong to the AVIT protein family. They are small related peptides of 80-90 amino acids in length, sharing 10 conserved cysteins, which create a five disulphide-bridged motif (colipase fold) and an identical amino-termini – AVIT. PK's are expressed in a wide array of peripheral tissues, including the steroidogenic glands (such as the ovary, testis and adrenal gland), but also in the gastrointestinal tract, nervous system, bladder, bone marrow and prostate.
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PKs exert their biological function through activation of two homologous G-protein coupled receptors (see Wikipedia: G protein-coupled receptors), termed Prokineticin receptor 1 (PROKR1) and Prokineticin receptor 2 (PROKR2). These receptors share , which is a high value among known GPCRs. The proteins diverse mainly in their extra and intra-cellular tails.
The prokineticin and their receptors are expressed in various tissues, including the cardiovascular, gastrointestinal, immune, reproductive, endocrine and nervous systems. The receptors have been shown to couple to Gq, Gi and Gs, thereafter mediating intracellular calcium mobilization, phosphorylation of p42/p44 MAPK, AKT and cAMP accumulation, respectively. Receptor activation has been shown to mediate proliferation, anti-apoptosis, differentiation and mobilization of target cells.
The prokineticin receptors have been found to be involved in various pathologies involving the cardiovascular, reproductive, endocrine and nervous systems. Notably, PROKR2 has been found to be mutated in Kallmann syndrome with dilated cardiomyopathy, a hypogonadism caused by a deficiency of gonadotropin-releasing hormone (GnRH) (see Wikipedia: Kallmann syndrome). Except for Z123X, which is Y in PROKR1, all other residues mutated in PROKR2 are identical in PROKR1.
