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Introduction

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OUTLINE FOR INTRODUCTION:

A)P2Y receptors are a subunit of a catergory of purinergic G-protein-coupled receptors

  1)Cell receptors have specificity for ATP or ADP over adenosine
  2)P2Y12-->platelet activation and thrombus formation
  3)Drugs Candidates - engineered molecules (allosteric regulators) that can inhibit P2Y12 receptors through conformational change and active site inhibition.

B) Plavix, Effient, and Brilinta

  1) Effects on P2Y12

C)ADZ1283 - Binding and Pocket Chemistry D) Differences between P2Y12r with and without ADZ1283

Note: Green Scene still to come

Overall Structure

The is mostly made up of alpha helices, shown in pink. The beta strands are shown in yellow. Polar vs nonpolar:Polar regions are pink. Nonpolar, or hyrophobic, regions are grey.

Binding Interactions

The of P2Y12 is colored in purple, which is the burried site, along with the ligands, which is colored in yellow.

Additional Features

Quiz Question 1

See Also

• 4ntj
• 4pxz
• 4py0
• 1vz1

Credits

Introduction - Adam Murphy

Overall Structure - Cora Ricker

Drug Binding Site - Duy Nguyen

Additional Features - Lauren Timmins

Quiz Question 1 - Aidan Finnerty

References

1. ↑ Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q. Structure of the human P2Y12 receptor in complex with an antithrombotic drug. Nature. 2014 May 1;509(7498):115-8. doi: 10.1038/nature13083. Epub 2014 Mar 23. PMID:24670650 doi:http://dx.doi.org/10.1038/nature13083