Structure of the human P2Y12 receptor in complex with an antithrombotic drug

[1]  Hualiang Jiang,et al.  Structure of the CCR5 Chemokine Receptor–HIV Entry Inhibitor Maraviroc Complex , 2013, Science.

[2]  H. Zachrisson,et al.  Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. , 2013, Journal of medicinal chemistry.

[3]  Jonas Boström,et al.  Synthesis, structure-property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y₁₂ receptor. , 2013, European journal of medicinal chemistry.

[4]  Woody Sherman,et al.  Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments , 2013, Journal of Computer-Aided Molecular Design.

[5]  C. Müller,et al.  The platelet P2Y12 receptor under normal and pathological conditions. Assessment with the radiolabeled selective antagonist [3H]PSB-0413 , 2013, Purinergic Signalling.

[6]  R. Stevens,et al.  Structure-function of the G protein-coupled receptor superfamily. , 2013, Annual review of pharmacology and toxicology.

[7]  Michel Bouvier,et al.  Restructuring G-Protein- Coupled Receptor Activation , 2012, Cell.

[8]  Joshua M. Kunken,et al.  Fusion partner toolchest for the stabilization and crystallization of G protein-coupled receptors. , 2012, Structure.

[9]  Clemens Vonrhein,et al.  Exploiting structure similarity in refinement: automated NCS and target-structure restraints in BUSTER , 2012, Acta crystallographica. Section D, Biological crystallography.

[10]  R. Stevens,et al.  Crystal Structure of a Lipid G Protein–Coupled Receptor , 2012, Science.

[11]  M. Lapins,et al.  Identification and analysis of functionally important amino acids in human purinergic 12 receptor using a Saccharomyces cerevisiae expression system , 2012, The FEBS journal.

[12]  S. Rasmussen,et al.  Crystal Structure of the β2Adrenergic Receptor-Gs protein complex , 2011, Nature.

[13]  M. Cattaneo.  Bleeding manifestations of congenital and drug-induced defects of the platelet P2Y12 receptor for adenosine diphosphate , 2011, Thrombosis and Haemostasis.

[14]  M. Cattaneo.  The platelet P2Y₁₂ receptor for adenosine diphosphate: congenital and drug-induced defects. , 2011, Blood.

[15]  B. Ashby,et al.  Mutational analysis of residues important for ligand interaction with the human P2Y(12) receptor. , 2010, European journal of pharmacology.

[16]  K. Jacobson,et al.  P2Y nucleotide receptors: promise of therapeutic applications. , 2010, Drug discovery today.

[17]  S. Husted,et al.  Ticagrelor: The First Reversibly Binding Oral P2Y12 Receptor Antagonist , 2009, Cardiovascular therapeutics.

[18]  Claes Held,et al.  Ticagrelor versus clopidogrel in patients with acute coronary syndromes. , 2009, The New England journal of medicine.

[19]  S. Kunapuli,et al.  Studies on the role of the extracellular cysteines and oligomeric structures of the P2Y12 receptor when interacting with antagonists , 2009, Journal of thrombosis and haemostasis : JTH.

[20]  P. Light,et al.  The Third Intracellular Loop Stabilizes the Inactive State of the Neuropeptide Y1 Receptor* , 2008, Journal of Biological Chemistry.

[21]  I. von Kügelgen,et al.  Interaction of the active metabolite of prasugrel, R‐138727, with cysteine 97 and cysteine 175 of the human P2Y12 receptor , 2008, Journal of thrombosis and haemostasis : JTH.

[22]  Karen N. Allen,et al.  research papers Acta Crystallographica Section D Biological , 2003 .

[23]  Randy J. Read,et al.  Phaser crystallographic software , 2007, Journal of applied crystallography.

[24]  Eric A. Barnard,et al.  International Union of Pharmacology LVIII: Update on the P2Y G Protein-Coupled Nucleotide Receptors: From Molecular Mechanisms and Pathophysiology to Therapy , 2006, Pharmacological Reviews.

[25]  Pascual Ferrara,et al.  The active metabolite of Clopidogrel disrupts P2Y12 receptor oligomers and partitions them out of lipid rafts. , 2006, Proceedings of the National Academy of Sciences of the United States of America.

[26]  J. Jakubowski,et al.  Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (Prasugrel, LY640315), a novel P2Y12 receptor inhibitor , 2005, Thrombosis and Haemostasis.

[27]  M. Cattaneo.  The P2 Receptors and Congenital Platelet Function Defects , 2005, Seminars in thrombosis and hemostasis.

[28]  Fei Long,et al.  REFMAC5 dictionary: organization of prior chemical knowledge and guidelines for its use. , 2004, Acta crystallographica. Section D, Biological crystallography.

[29]  T. Lindahl,et al.  Synergistic action between inhibition of P2Y12/P2Y1 and P2Y12/thrombin in ADP‐ and thrombin‐induced human platelet activation , 2004, British journal of pharmacology.

[30]  Judith Klein-Seetharaman,et al.  Identification of core amino acids stabilizing rhodopsin. , 2004, Proceedings of the National Academy of Sciences of the United States of America.

[31]  T. Schöneberg,et al.  The Structural Evolution of a P2Y-like G-protein-coupled Receptor* , 2003, Journal of Biological Chemistry.

[32]  H. Schiöth,et al.  The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. , 2003, Molecular pharmacology.

[33]  J. Ware,et al.  Molecular bases of defective signal transduction in the platelet P2Y12 receptor of a patient with congenital bleeding , 2003, Proceedings of the National Academy of Sciences of the United States of America.

[34]  G. Burnstock,et al.  Both the ADP receptors P2Y 1 and P2Y 12 , play a role in controlling shape change in human platelets , 2003, Platelets.

[35]  David Julius,et al.  Identification of the platelet ADP receptor targeted by antithrombotic drugs , 2001, Nature.

[36]  V. Cherezov,et al.  Crystallizing membrane proteins using lipidic mesophases , 2009, Nature Protocols.

[37]  Z. Otwinowski,et al.  Processing of X-ray diffraction data collected in oscillation mode. , 1997, Methods in enzymology.

[38]  J. Ballesteros,et al.  [19] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors , 1995 .