Pharmacochemistry of the platelet purinergic receptors.

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Pharmacochemistry of the platelet purinergic receptors. is …
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scholarly articleQ13442814

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P6179Dimensions Publication ID1000828240
P356DOI10.1007/S11302-011-9216-0
P932PMC publication ID3166987
P698PubMed publication ID21484092
P5875ResearchGate publication ID51042845

P50authorStefano CostanziQ37381929
Kenneth A. JacobsonQ37387267
P2093author name stringFrancesca Deflorian
Shilpi Mishra
P2860cites workIdentification of the platelet ADP receptor targeted by antithrombotic drugsQ24290845
Trimeric architecture of homomeric P2X2 and heteromeric P2X1+2 receptor subtypesQ24301398
Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptorQ24612312
International Union of Pharmacology LVIII: update on the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapyQ24629255
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonistQ24654563
Crystal structure of the ATP-gated P2X(4) ion channel in the closed stateQ24657193
The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptorQ24672638
Beta-nicotinamide adenine dinucleotide is an inhibitory neurotransmitter in visceral smooth muscleQ24673894
A novel P2Y(12) adenosine diphosphate receptor antagonist that inhibits platelet aggregation and thrombus formation in rat and dog modelsQ28222823
The adenosine a2b receptor: its role in inflammationQ28303755
Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptorsQ28344116
Antiplatelet action of R-99224, an active metabolite of a novel thienopyridine-type G(i)-linked P2T antagonist, CS-747Q28345809
Selectivity of diadenosine polyphosphates for rat P2X receptor subunitsQ28371849
Second messenger cascade specificity and pharmacological selectivity of the human P2Y1-purinoceptorQ28637757
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonistsQ30435017
Adenosine 5'-O-(1-boranotriphosphate) derivatives as novel P2Y(1) receptor agonists.Q30746442
NF449 is a novel inhibitor of fibroblast growth factor receptor 3 (FGFR3) signaling active in chondrocytes and multiple myeloma cellsQ30982341
Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14).Q31019114
Inhibition of platelet function by administration of MRS2179, a P2Y1 receptor antagonistQ31882653
MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in miceQ33225547
Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregationQ33482579
PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G protein-coupled receptorsQ33507142
Piperazinyl glutamate pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregationQ33530193
Structure-based discovery of A2A adenosine receptor ligandsQ33560239
Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groupsQ33584104
Defective platelet aggregation and increased resistance to thrombosis in purinergic P2Y(1) receptor-null miceQ33903557
Charged residues in the C-terminus of the P2Y1 receptor constitute a basolateral-sorting signalQ33951253
Novel Alexa Fluor-488 labeled antagonist of the A(2A) adenosine receptor: Application to a fluorescence polarization-based receptor binding assayQ33976371
Functionalized congeners of P2Y1 receptor antagonists: 2-alkynyl (N)-methanocarba 2'-deoxyadenosine 3',5'-bisphosphate analogues and conjugation to a polyamidoamine (PAMAM) dendrimer carrierQ34029528
P2Y nucleotide receptors: promise of therapeutic applicationsQ34062142
Mutational analysis of residues important for ligand interaction with the human P2Y(12) receptorQ34169728
Activation of P2Y1 nucleotide receptors induces inhibition of the M-type K+ current in rat hippocampal pyramidal neuronsQ41961727
Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors.Q42085394
Specificity of the ecto-ATPase inhibitor ARL 67156 on human and mouse ectonucleotidasesQ42133085
Inter-subunit disulfide cross-linking in homomeric and heteromeric P2X receptorsQ42166779
Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors.Q42541961
Identification of competitive antagonists of the P2Y1 receptor.Q42552594
Identification of a receptor for ADP on blood platelets by photoaffinity labellingQ42796937
Agonist and antagonist effects of diadenosine tetraphosphate, a platelet dense granule constituent, on platelet P2Y1, P2Y12 and P2X1 receptors.Q42909234
Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonistsQ43027762
A new role for the A2b adenosine receptor in regulating platelet functionQ43183880
Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregationQ43185318
Comparison of ticagrelor and thienopyridine P2Y(12) binding characteristics and antithrombotic and bleeding effects in rat and dog models of thrombosis/hemostasisQ43289595
Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y12 receptorQ43290040
Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y(12)).Q43679810
Activity of diadenosine polyphosphates at P2Y receptors stably expressed in 1321N1 cellsQ43800933
A general approach toward the synthesis of C-nucleoside pyrazolo[1,5-a]-1,3,5-triazines and their 3',5'-bisphosphate C-nucleotide analogues as the first reported in vivo stable P2Y(1)-receptor antagonistsQ44210114
The hypolipidemic drug metabolites nafenopin-CoA and ciprofibroyl-CoA are competitive P2Y1 receptor antagonistsQ44314960
Purification and Functional Reconstitution of the Human P2Y12ReceptorQ44628575
Agonist binding and Gq-stimulating activities of the purified human P2Y1 receptorQ44741503
Synthesis and biological activity of 2-alkylated deoxyadenosine bisphosphate derivatives as P2Y(1) receptor antagonistsQ44803614
Arg333 and Arg334 in the COOH terminus of the human P2Y1 receptor are crucial for Gq couplingQ45127883
Interaction of the active metabolite of prasugrel, R-138727, with cysteine 97 and cysteine 175 of the human P2Y12 receptorQ45140487
Biochemical and functional evidence for heteromeric assembly of P2X1 and P2X4 subunitsQ45247897
Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonistQ45274145
Novel P2Y12 adenosine diphosphate receptor antagonists for inhibition of platelet aggregation (I): in vitro effects on plateletsQ45300057
Ticagrelor binds to human P2Y(12) independently from ADP but antagonizes ADP-induced receptor signaling and platelet aggregation.Q45954831
6-Amino-2-mercapto-3H-pyrimidin-4-one derivatives as new candidates for the antagonism at the P2Y12 receptors.Q45999081
High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.Q46000448
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonistsQ46312937
Effects of 5'-phosphate derivatives of 2-hexynyl adenosine and 2-phenylethynyl adenosine on responses of human platelets mediated by P2Y receptors.Q46436392
P2Y1 receptor antagonists as novel antithrombotic agentsQ46620039
The novel suramin analogue NF864 selectively blocks P2X1 receptors in human platelets with potency in the low nanomolar rangeQ46699751
Acyl derivatives of coenzyme A inhibit platelet function via antagonism at P2Y1 and P2Y12 receptors: a new finding that may influence the design of anti-thrombotic agentsQ46735701
Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptorsQ46743054
Carba-nucleosides as potent antagonists of the adenosine 5'-diphosphate (ADP) purinergic receptor (P2Y12 on human plateletsQ46788165
Pharmacological characterization of recombinant human and rat P2X receptor subtypesQ48911279
Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptorsQ48921231
P2-purinoceptor antagonists: II. Blockade of P2-purinoceptor subtypes and ecto-nucleotidases by compounds related to Evans blue and trypan blue.Q50535582
The suramin analogue NF279 is a novel and potent antagonist selective for the P2X(1) receptor.Q50724270
BF0801, a novel adenine derivative, inhibits platelet activation via phosphodiesterase inhibition and P2Y12 antagonismQ51772011
Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor.Q51812620
Homozygous type I Protein C deficiency in neonatal purpura fulminans with a novel frame-shift deletion of 10 base pairs in exon 8 of PROC gene.Q53625568
Molecular recognition of modified adenine nucleotides by the P2Y(1)-receptor. 1. A synthetic, biochemical, and NMR approach.Q55476249
Detection of P2Y(14) protein in platelets and investigation of the role of P2Y(14) in platelet function in comparison with the EP(3) receptorQ58616257
Identification and biological activity of the active metabolite of clopidogrelQ73322574
Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapyQ77928203
Defining the nucleotide binding sites of P2Y receptors using rhodopsin-based homology modelingQ79177476
Mitochondrial calcium transport is regulated by P2Y1- and P2Y2-like mitochondrial receptorsQ79776887
P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoringQ80468482
Rapid and reversible modulation of platelet function in man by a novel P2Y(12) ADP-receptor antagonist, INS50589Q80677617
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosisQ81161941
Inhibition of receptor/G protein coupling by suramin analogues.Q34388145
Molecular basis for ADP-induced platelet activation. II. The P2Y1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in plateletsQ34453608
Inactivation of the human P2Y12 receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270.Q34530924
Ebselen is a potent non-competitive inhibitor of extracellular nucleoside diphosphokinaseQ34551159
Adenosine receptor antagonists: translating medicinal chemistry and pharmacology into clinical utilityQ34734061
Differential effects of P2-purinoceptor antagonists on phospholipase C- and adenylyl cyclase-coupled P2Y-purinoceptorsQ34792562
Purine and pyrimidine (P2) receptors as drug targetsQ34815266
Structure-activity relationships of suramin and pyridoxal-5'-phosphate derivatives as P2 receptor antagonistsQ34947219
New P2Y12 antagonistsQ34988595
[32P]2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([32P]MRS2500), a novel radioligand for quantification of native P2Y1 receptorsQ35100653
Activation and regulation of purinergic P2X receptor channelsQ35122793
Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonistQ35200801
2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide bindingQ35213075
Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphateQ35606305
Emerging roles for P2X1 receptors in platelet activationQ35809098
Potent agonist action of 2-thioether derivatives of adenine nucleotides at adenylyl cyclase-linked P2Y-purinoceptorsQ35873053
Identification of potent P2Y-purinoceptor agonists that are derivatives of adenosine 5'-monophosphateQ35874099
Comparative studies on the affinities of ATP derivatives for P2x-purinoceptors in rat urinary bladderQ35874677
Purification and Recognition of Recombinant Mouse P2X(1) Receptors Expressed in a Baculovirus SystemQ36058000
Activity of Novel Adenine Nucleotide Derivatives as Agonists and Antagonists at Recombinant Rat P2X ReceptorsQ36086811
Northern Ring Conformation of Methanocarba-Adenosine 5'-Triphosphate Required for Activation of P2X Receptors.Q36108563
2-Substitution of Adenine Nucleotide Analogues Containing a Bicyclo[3.1.0]hexane Ring System Locked in a Northern Conformation: Enhanced Potency as P2Y1 Receptor AntagonistsQ36128578
(N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human plateletsQ36147741
Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognitionQ36183047
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.Q36201452
Modelling the P2Y purinoceptor using rhodopsin as templateQ36251014
The role of amino acids in extracellular loops of the human P2Y1 receptor in surface expression and activation processes.Q36253724
Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog.Q36282943
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.Q36311516
Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.Q36316891
Quantification of recombinant and platelet P2Y(1) receptors utilizing a [(125)I]-labeled high-affinity antagonist 2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([(125)I]MRS2500)Q36626943
Caged agonist of P2Y1 and P2Y12 receptors for light-directed facilitation of platelet aggregation.Q36632204
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonistsQ37122033
Quantification of Gi-mediated inhibition of adenylyl cyclase activity reveals that UDP is a potent agonist of the human P2Y14 receptorQ37444485
Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonistQ37552005
Recent developments in adenosine A2A receptor ligandsQ37565154
New P2Y(12) inhibitorsQ37667399
Elinogrel, a reversible P2Y12 receptor antagonist for the treatment of acute coronary syndrome and prevention of secondary thrombotic events.Q37697100
P2X purinergic receptor ligands: recently patented compoundsQ37703255
Physiological implications of adenosine receptor-mediated platelet aggregationQ37780716
Ectonucleotidases as regulators of purinergic signaling in thrombosis, inflammation, and immunityQ37876541
Transient expression of the recombinant chick brain P2y1 purinoceptor and localization of the corresponding mRNA.Q38468312
ADP ribose is an endogenous ligand for the purinergic P2Y1 receptor.Q39629251
2-MeS-beta,gamma-CCl2-ATP is a potent agent for reducing intraocular pressureQ39722931
A novel insulin secretagogue based on a dinucleoside polyphosphate scaffoldQ39736692
Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffoldQ39741301
Extracellular NAD(+) induces a rise in [Ca(2+)](i) in activated human monocytes via engagement of P2Y(1) and P2Y(11) receptorsQ39800524
Involvement of basic amino acid residues in transmembrane regions 6 and 7 in agonist and antagonist recognition of the human platelet P2Y(12)-receptorQ39937155
Identification of hydrolytically stable and selective P2Y(1) receptor agonists.Q39945033
Rapid resensitization of purinergic receptor function in human platelets.Q39976986
Constitutive and agonist-induced dimerizations of the P2Y1 receptor: relationship to internalization and scaffolding.Q40013918
Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptorQ40018963
Hetero-oligomerization of the P2Y11 receptor with the P2Y1 receptor controls the internalization and ligand selectivity of the P2Y11 receptorQ40083620
Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potencyQ40357842
Identification of a potent inverse agonist at a constitutively active mutant of human P2Y12 receptorQ40360423
Discovery and synthesis of a novel and selective drug-like P2X(1) antagonistQ40415070
Acyclic analogues of adenosine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple pathways of inhibition of platelet aggregation.Q40684082
Structure-activity relationships of dinucleotides: Potent and selective agonists of P2Y receptors.Q40722376
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptorsQ40791305
A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptorsQ40854824
Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.Q40956148
Co-expression of P2X1 and P2X5 receptor subunits reveals a novel ATP-gated ion channel.Q40987897
Contribution of the region Glu181 to Val200 of the extracellular loop of the human P2X1 receptor to agonist binding and gating revealed using cysteine scanning mutagenesis.Q41502656
Heteromultimeric P2X(1/2) receptors show a novel sensitivity to extracellular pHQ41569539
A multiple dose study of prasugrel (CS-747), a novel thienopyridine P2Y12 inhibitor, compared with clopidogrel in healthy humansQ41868121
P433issue3
P304page(s)305-324
P577publication date2011-02-18
P1433published inPurinergic SignallingQ15716545
P1476titlePharmacochemistry of the platelet purinergic receptors
P478volume7

Reverse relations

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