4PXZ


Conserved Protein Domain Family
7tmA_P2Y12

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cd15150: 7tmA_P2Y12 
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P2Y purinoceptor 12, member of the class A family of seven-transmembrane G protein-coupled receptors
The P2Y12 receptor (P2Y12R) is found predominantly on the surface of blood platelets and is activated by adenosine diphosphate (ADP). P2Y12R plays an important role in the regulation of blood clotting and belongs to the G(i) class of the P2Y family of purinergic G protein-coupled receptors. P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-sugars. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5 and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12 and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-sugars (P2Y14).
Statistics
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PSSM-Id: 341326
Aligned: 5 rows
Threshold Bit Score: 421.145
Created: 18-Nov-2008
Updated: 25-Oct-2021
Structure
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Program:
Drawing:
Aligned Rows:
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Conserved site includes 23 residues -Click on image for an interactive view with Cn3D
Feature 1:ligand binding site [chemical binding site]
Evidence:
  • Comment:based on the binding of human P2Y12 receptor to full agonist 2-methylthio-adenosine-5'-diphosphate (2MeSADP, a close analogue of endogenous agonist ADP)
  • Structure:4PXZ: Human P2Y12 receptor binds full agonist 2MeSADP, a close analogue of ADP; contacts at 4A
  • Comment:Small-molecule chemical ligands tend to bind deeper within the receptor core, compared to a peptide ligand neurotensin, which binds towards the extracellular surface of its receptor.

Sequence Alignment
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Format: Row Display: Color Bits: Type Selection:
Feature 1                                                                           #   #   ##  #
4PXZ_A        35 VLFPLLYTVLFFVGLITNGLAMRIFFQIRSKsnFIIFLKNTVISDLLMILTFPFKILSDAklgtGPLRTFVCQVTSVIFY 114
XP_001921964  29 IVFPVLYSILLILGLSLNALAAWVFLRIPSKshFIIYLKNIVVADIIMTLTFPFKILSDAnvasVGIRIFVCRVSSVLFY 108 zebrafish
EMC88215      14 VIFPLLYTILFLVGITMNGLAMWVFFKIPSKsnFIIFLKNTVISDLLMILTFPFKILSDAklvsWVLRGFVCQVTQVVFY 93  domestic pigeon
AAH84665      21 VIFSVLYTVLFIVGVTMNGLAVRVFFQIPSNsnFVIFLKNSVISDCLMIMTFPFKILSDSrlglWKLKGFVCQVTSVIFY 100 African clawed ...
Q9H244        26 VLFPLLYTVLFFVGLITNGLAMRIFFQIRSKsnFIIFLKNTVISDLLMILTFPFKILSDAklgtGPLRTFVCQVTSVIFY 105 human
Feature 1        #  #                                          #  ##  #   #          ##   #      
4PXZ_A       115 FTMYISISFLGLITIDRYQKTTRPFkTSNPKnlLGAKILSVVIWAFMFLLSLPNMILTnrqprdknvKKCSFLKsefglv 194
XP_001921964 109 LTMYISILFFGLISIDRCRKTMWPFvGTNPKrlLHRKLLSGVIWTSLLALSLPNVILTsrpn-igerFKCSDLKtelglq 187 zebrafish
EMC88215      94 FTMYISILFLGLITIDRYQKATSPFrTSTSRslLGAKILSTAIWVSMFALSLPNMILTnkkktpknvKKCALLKsefglv 173 domestic pigeon
AAH84665     101 FTMYISIIFLGLITIDRYLKTVRPFhNSHATnlRRVKIMSTLIWIIMFSISLPNMIFTsktqtpqsvKKCYLLKsdfglv 180 African clawed ...
Q9H244       106 FTMYISISFLGLITIDRYQKTTRPFkTSNPKnlLGAKILSVVIWAFMFLLSLPNMILTnrqprdknvKKCSFLKsefglv 185 human
Feature 1         #  ##  #                                                                       
4PXZ_A       195 WHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYvrtadlednwetlndnlkviekadnaaqvkdaltkmraaaldaqk 274
XP_001921964 188 WHEVVNHICQVIFWGNLIIVIICYTLISRELYKSYartrs---------------------------------------- 227 zebrafish
EMC88215     174 WHEIVNYICQLIFWVNLAVIVVCYILISKELYKSYkrtr----------------------------------------- 212 domestic pigeon
AAH84665     181 WHEIVNFICQFIFWVVFVIIVVCYLLITRKLLQSYkktr----------------------------------------- 219 African clawed ...
Q9H244       186 WHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYvrtr----------------------------------------- 224 human
Feature 1                                                                                        
4PXZ_A       275 atppkledkspdspemkdfrhgfdilvgqiddalklanegkvkeaqaaaeqlkttrnayiqkylrgvgkVPRKKVNVKVF 354
XP_001921964 228 ----------------------------------------------------------------prgtqSKKKHIQVNVF 243 zebrafish
EMC88215     213 -----------------------------------------------------------------ctgkASKKTVNLKVF 227 domestic pigeon
AAH84665     220 -----------------------------------------------------------------sertTSRRKVNIKVF 234 African clawed ...
Q9H244       225 -----------------------------------------------------------------gvgkVPRKKVNVKVF 239 human
Feature 1                        #  #   #                 #                              
4PXZ_A       355 IIIAVFFICFVPFHFARIPYTLSQtrdvfd-ctaentLFYVKESTLWLTSLNACLNPFIYFFLCkSFRNSLI 425
XP_001921964 244 LVLAVFFICFVPFHFARVPYTISQtrallfscpqklfFFKLKESTLWLSSLNSVLDPLIYFFLCkSFRSSLF 315 zebrafish
EMC88215     228 IIIAVFFICFVPFHFTRIPYTLSQtravfe-caaqatLFHVKESTLWLTSLNACLDPFIYFFLCkSFRRSLL 298 domestic pigeon
AAH84665     235 IIIAVFFVCFVPFHFARIPYTLSQtrdvfk-csakmtLFYVKESTLWLSSLNACLDPFIYFFLCrSFRNSLV 305 African clawed frog
Q9H244       240 IIIAVFFICFVPFHFARIPYTLSQtrdvfd-ctaentLFYVKESTLWLTSLNACLDPFIYFFLCkSFRNSLI 310 human

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