P2Y purinoceptor 12 - Revision history

Wu3857: /* Reference */

2019-08-19T23:09:13Z

‎Reference

Wu3857: /* Summary */

2019-08-17T15:41:17Z

‎Summary

Wu3857 at 15:39, 17 August 2019

2019-08-17T15:39:29Z

Wu3857: Created page with "{| align="left" | TOC |} {{#invoke:InfoboxforTarget|run|P2Y12, ADPG-R|[https://www.uniprot.org/uniprot/Q9H244 Q9H244]|Homo sapiens|Cys17, Cys270|[http://pfam.xfam.org/..."

2019-08-17T15:37:18Z

Created page with "{| align="left" | __TOC__ |} {{#invoke:InfoboxforTarget|run|P2Y12, ADPG-R|[https://www.uniprot.org/uniprot/Q9H244 Q9H244]|Homo sapiens|Cys17, Cys270|[http://pfam.xfam.org/..."

New page

{| align="left"
| __TOC__
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{{#invoke:InfoboxforTarget|run|P2Y12, ADPG-R|[https://www.uniprot.org/uniprot/Q9H244 Q9H244]|Homo sapiens|Cys17, Cys270|[http://pfam.xfam.org/family/PF00001 7 transmembrane receptor (rhodopsin family)], G-protein coupled receptor 1 family]|[[:Category:P2Y purinoceptor 12|Ligand list]]|G-protein coupled receptor}}

==Summary==

===Protein Function ===
In the field of purinergic signaling, the P2Y12 protein is found mainly but not exclusively on the surface of blood platelets, and is an important regulator in blood clotting. P2Y12 belongs to the Gi class of a group of G protein-coupled (GPCR) purinergic receptors and is a chemoreceptor for adenosine diphosphate (ADP). The P2Y family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor is involved in platelet aggregation, and is a potential target for the treatment of thromboembolisms and other clotting disorders. 
The drugs clopidogrel (Plavix), prasugrel (Efient, Effient) ticagrelor (Brilinta) and cangrelor (Kengreal) bind to this receptor and are marketed as antiplatelet agents. P2Y12 inhibitors do not change the risk of death when given to people who have had a NSTEMI. They do however increase the risk of bleeding and decrease the risk of further cardiovascular problems. Thus their routine use is of questionable value. (From Wikipedia) 
Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Required for normal platelet aggregation and blood coagulation. (From Uniprot) 

===Cys Function & Property===
Cys17 and Cys270 are located at the extracellular regions of P2Y12, and could form disulfide bond 
[[File:563-function.png|center |600px]]
<div align="center">P2Y12 topology (PMID: 30302530)</div> 

* Hydrophobic property:
:[[File:563-hydro.png||600px]]
* SASA：
:Cys17: 26.597 A^2 
:Cys270: 44.767 A^2 

==Protein Sequence==

MQAVDNLTSA PGNTSL'''C'''TRD YKITQVLFPL LYTVLFFVGL ITNGLAMRIF 
FQIRSKSNFI IFLKNTVISD LLMILTFPFK ILSDAKLGTG PLRTFVCQVT 
SVIFYFTMYI SISFLGLITI DRYQKTTRPF KTSNPKNLLG AKILSVVIWA 
FMFLLSLPNM ILTNRQPRDK NVKKCSFLKS EFGLVWHEIV NYICQVIFWI 
NFLIVIVCYT LITKELYRSY VRTRGVGKVP RKKVNVKVFI IIAVFFICFV 
PFHFARIPYT LSQTRDVFD'''C''' TAENTLFYVK ESTLWLTSLN ACLDPFIYFF 
LCKSFRNSLI SMLKCPNSAT SLSQDNRKKE QDGGDPNEET PM 


==Structural Information==
*Known structure with covalent ligand: 
:Unknown 

*Protein structure:
:[[File:563.png|center|800px]]

==Related Pathway==
*[https://www.genome.jp/kegg-bin/show_pathway?ko04611 Platelet activation] 

==Experimental Evidence==
:Cys-directed Mutation

==Reference==
# Ding Z, Kim S, Dorsam R T, et al. '''Inactivation of the human P2Y12 receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270[J].''' Blood, 2003, 101(10): 3908-3914. [https://www.ncbi.nlm.nih.gov/pubmed/?term=12560222 12560222] 

[[Category:Targets|Targets]]
[[Category:Homo sapiens|Homo sapiens]]
[[Category:G-protein coupled receptor|G-protein coupled receptor]]
[[Category:G-protein coupled receptor 1 family|G-protein coupled receptor 1 family]]
[[Category:Platelet activation|Platelet activation]]

@@ Line 13: / Line 13: @@
 ===Cys Function & Property===
 Cys17 and Cys270 are located at the extracellular regions of P2Y12, and could form disulfide bond <br/>
-[[File:563-function.png|center |600px]]
+[[File:563-function.png|center |800px]]
 <div align="center">P2Y12 topology (PMID: 30302530)</div><br/>

@@ Line 48: / Line 48: @@
 ==Reference==
 # Ding Z, Kim S, Dorsam R T, et al. '''Inactivation of the human P2Y<sub>12</sub> receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270[J].''' Blood, 2003, 101(10): 3908-3914. [https://www.ncbi.nlm.nih.gov/pubmed/?term=12560222 12560222]<br/>
-[[Category:Targets|Targets]]
-[[Category:Homo sapiens|Homo sapiens]]
+[[Category:Targets]]
-[[Category:G-protein coupled receptor|G-protein coupled receptor]]
+[[Category:Homo sapiens]]
-[[Category:G-protein coupled receptor 1 family|G-protein coupled receptor 1 family]]
+[[Category:G-protein coupled receptor]]
-[[Category:Platelet activation|Platelet activation]]
+[[Category:G-protein coupled receptor 1 family]]

P2Y purinoceptor 12 - Revision history

Wu3857: /* Reference */

Wu3857: /* Summary */

Wu3857 at 15:39, 17 August 2019

Wu3857: Created page with "{| align="left" | __TOC__ |} {{#invoke:InfoboxforTarget|run|P2Y12, ADPG-R|[https://www.uniprot.org/uniprot/Q9H244 Q9H244]|Homo sapiens|Cys17, Cys270|[http://pfam.xfam.org/..."

Wu3857: Created page with "{| align="left" | TOC |} {{#invoke:InfoboxforTarget|run|P2Y12, ADPG-R|[https://www.uniprot.org/uniprot/Q9H244 Q9H244]|Homo sapiens|Cys17, Cys270|[http://pfam.xfam.org/..."