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Items: 1 to 50 of 687

1.

Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines to develop functionalized ligands to target adenosine receptors: fluorescent ligands as an example.

Federico S, Margiotta E, Paoletta S, Kachler S, Klotz KN, Jacobson KA, Pastorin G, Moro S, Spalluto G.

Medchemcomm. 2019 Feb 18;10(7):1094-1108. doi: 10.1039/c9md00014c. eCollection 2019 Jul 1.

PMID:
31391881
2.

Evidence for the Interaction of A3 Adenosine Receptor Agonists at the Drug-Binding Site(s) of Human P-glycoprotein (ABCB1).

Abel B, Tosh DK, Durell SR, Murakami M, Vahedi S, Jacobson KA, Ambudkar SV.

Mol Pharmacol. 2019 Aug;96(2):180-192. doi: 10.1124/mol.118.115295. Epub 2019 May 24.

3.

Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor.

Lu Y, Qin S, Zhang B, Dai A, Cai X, Ma M, Gao ZG, Yang D, Stevens RC, Jacobson KA, Wang MW, Shui W.

Anal Chem. 2019 Jul 2;91(13):8162-8169. doi: 10.1021/acs.analchem.9b00477. Epub 2019 Jun 12.

PMID:
31094506
4.

Deficiency of adenosine deaminase 2 triggers adenosine-mediated NETosis and TNF production in patients with DADA2.

Carmona-Rivera C, Khaznadar SS, Shwin KW, Irizarry-Caro JA, O'Neil LJ, Liu Y, Jacobson KA, Ombrello AK, Stone DL, Tsai WL, Kastner DL, Aksentijevich I, Kaplan MJ, Grayson PC.

Blood. 2019 Jul 25;134(4):395-406. doi: 10.1182/blood.2018892752. Epub 2019 Apr 23.

PMID:
31015188
5.

Adenosine A3 receptor activation inhibits pronociceptive N-type Ca2+ currents and cell excitability in dorsal root ganglion neurons.

Coppi E, Cherchi F, Fusco I, Failli P, Vona A, Dettori I, Gaviano L, Lucarini E, Jacobson KA, Tosh DK, Salvemini D, Ghelardini C, Pedata F, Di Cesare Mannelli L, Pugliese AM.

Pain. 2019 May;160(5):1103-1118. doi: 10.1097/j.pain.0000000000001488.

PMID:
31008816
6.

Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development.

Jacobson KA, Tosh DK, Jain S, Gao ZG.

Front Cell Neurosci. 2019 Mar 28;13:124. doi: 10.3389/fncel.2019.00124. eCollection 2019. Review.

7.

Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors.

Junker A, Renn C, Dobelmann C, Namasivayam V, Jain S, Losenkova K, Irjala H, Duca S, Balasubramanian R, Chakraborty S, Börgel F, Zimmermann H, Yegutkin GG, Müller CE, Jacobson KA.

J Med Chem. 2019 Apr 11;62(7):3677-3695. doi: 10.1021/acs.jmedchem.9b00164. Epub 2019 Mar 21.

PMID:
30895781
8.

Physiology and effects of nucleosides in mice lacking all four adenosine receptors.

Xiao C, Liu N, Jacobson KA, Gavrilova O, Reitman ML.

PLoS Biol. 2019 Mar 1;17(3):e3000161. doi: 10.1371/journal.pbio.3000161. eCollection 2019 Mar.

9.

Structure Activity Relationship of 4-Amino-2-thiopyrimidine Derivatives as Platelet Aggregation Inhibitors.

Cacciari B, Crepaldi P, Cheng CY, Bossi E, Spalluto G, Federico S, Jacobson KA, Cattaneo M.

Med Chem. 2019 Feb 8. doi: 10.2174/1573406415666190208124534. [Epub ahead of print]

PMID:
30734681
10.

Editorial: Purinergic Pharmacology.

Ciruela F, Jacobson KA.

Front Pharmacol. 2019 Jan 23;10:21. doi: 10.3389/fphar.2019.00021. eCollection 2019. No abstract available.

11.

Design and in Vivo Characterization of A1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series.

Tosh DK, Rao H, Bitant A, Salmaso V, Mannes P, Lieberman DI, Vaughan KL, Mattison JA, Rothwell AC, Auchampach JA, Ciancetta A, Liu N, Cui Z, Gao ZG, Reitman ML, Gavrilova O, Jacobson KA.

J Med Chem. 2019 Feb 14;62(3):1502-1522. doi: 10.1021/acs.jmedchem.8b01662. Epub 2019 Jan 3.

PMID:
30605331
12.

Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A3 adenosine receptor antagonists.

Yu J, Mannes P, Jung YH, Ciancetta A, Bitant A, Lieberman DI, Khaznadar S, Auchampach JA, Gao ZG, Jacobson KA.

Medchemcomm. 2018 Oct 18;9(11):1920-1932. doi: 10.1039/c8md00317c. eCollection 2018 Nov 1.

PMID:
30568760
13.

Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists.

Tosh DK, Ciancetta A, Mannes P, Warnick E, Janowsky A, Eshleman AJ, Gizewski E, Brust TF, Bohn LM, Auchampach JA, Gao ZG, Jacobson KA.

ACS Omega. 2018 Oct 31;3(10):12658-12678. doi: 10.1021/acsomega.8b01237. Epub 2018 Oct 4.

14.

Preclinical Evaluation of the First Adenosine A1 Receptor Partial Agonist Radioligand for Positron Emission Tomography Imaging.

Guo M, Gao ZG, Tyler R, Stodden T, Li Y, Ramsey J, Zhao WJ, Wang GJ, Wiers CE, Fowler JS, Rice KC, Jacobson KA, Kim SW, Volkow ND.

J Med Chem. 2018 Nov 21;61(22):9966-9975. doi: 10.1021/acs.jmedchem.8b01009. Epub 2018 Nov 13.

PMID:
30359014
15.

Probing structure-activity relationship in β-arrestin2 recruitment of diversely substituted adenosine derivatives.

Storme J, Tosh DK, Gao ZG, Jacobson KA, Stove CP.

Biochem Pharmacol. 2018 Dec;158:103-113. doi: 10.1016/j.bcp.2018.10.003. Epub 2018 Oct 4.

PMID:
30292756
16.

Author Correction: Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors.

Liu X, Gao ZG, Wu Y, Stevens RC, Jacobson KA, Zhao S.

Sci Rep. 2018 Jul 24;8(1):11380. doi: 10.1038/s41598-018-29406-6.

17.

Activation of basal forebrain purinergic P2 receptors promotes wakefulness in mice.

Yang C, Larin A, McKenna JT, Jacobson KA, Winston S, Strecker RE, Kalinchuk A, Basheer R, Brown RE.

Sci Rep. 2018 Jul 16;8(1):10730. doi: 10.1038/s41598-018-29103-4.

18.

Thermostabilization and purification of the human dopamine transporter (hDAT) in an inhibitor and allosteric ligand bound conformation.

Navratna V, Tosh DK, Jacobson KA, Gouaux E.

PLoS One. 2018 Jul 2;13(7):e0200085. doi: 10.1371/journal.pone.0200085. eCollection 2018.

19.

Extrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A2A Adenosine Receptor.

Eddy MT, Gao ZG, Mannes P, Patel N, Jacobson KA, Katritch V, Stevens RC, Wüthrich K.

J Am Chem Soc. 2018 Jul 5;140(26):8228-8235. doi: 10.1021/jacs.8b03805. Epub 2018 Jun 20.

20.

Remote control of movement disorders using a photoactive adenosine A2A receptor antagonist.

Taura J, Nolen EG, Cabré G, Hernando J, Squarcialupi L, López-Cano M, Jacobson KA, Fernández-Dueñas V, Ciruela F.

J Control Release. 2018 Aug 10;283:135-142. doi: 10.1016/j.jconrel.2018.05.033. Epub 2018 May 31.

21.

Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors.

Liu X, Gao ZG, Wu Y, Stevens RC, Jacobson KA, Zhao S.

Sci Rep. 2018 May 24;8(1):8084. doi: 10.1038/s41598-018-26577-0. Erratum in: Sci Rep. 2018 Jul 24;8(1):11380.

22.

Structure-Guided Modification of Heterocyclic Antagonists of the P2Y14 Receptor.

Yu J, Ciancetta A, Dudas S, Duca S, Lottermoser J, Jacobson KA.

J Med Chem. 2018 Jun 14;61(11):4860-4882. doi: 10.1021/acs.jmedchem.8b00168. Epub 2018 May 16.

23.

Activation of adenosine A2A or A2B receptors causes hypothermia in mice.

Carlin JL, Jain S, Duroux R, Suresh RR, Xiao C, Auchampach JA, Jacobson KA, Gavrilova O, Reitman ML.

Neuropharmacology. 2018 Sep 1;139:268-278. doi: 10.1016/j.neuropharm.2018.02.035. Epub 2018 Mar 13.

PMID:
29548686
24.

Pyrimidine Nucleotides Containing a (S)-Methanocarba Ring as P2Y6 Receptor Agonists.

Toti KS, Jain S, Ciancetta A, Balasubramanian R, Chakraborty S, Surujdin R, Shi ZD, Jacobson KA.

Medchemcomm. 2017 Oct 1;8(10):1897-1908. doi: 10.1039/C7MD00397H. Epub 2017 Sep 6.

25.

Chemotherapy-induced pain is promoted by enhanced spinal adenosine kinase levels through astrocyte-dependent mechanisms.

Wahlman C, Doyle TM, Little JW, Luongo L, Janes K, Chen Z, Esposito E, Tosh DK, Cuzzocrea S, Jacobson KA, Salvemini D.

Pain. 2018 Jun;159(6):1025-1034. doi: 10.1097/j.pain.0000000000001177.

26.

Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling.

White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC.

Structure. 2018 Feb 6;26(2):259-269.e5. doi: 10.1016/j.str.2017.12.013. Epub 2018 Jan 27.

27.

Purinergic Signaling in Mast Cell Degranulation and Asthma.

Gao ZG, Jacobson KA.

Front Pharmacol. 2017 Dec 22;8:947. doi: 10.3389/fphar.2017.00947. eCollection 2017. Review.

28.

A binding kinetics study of human adenosine A3 receptor agonists.

Xia L, Kyrizaki A, Tosh DK, van Duijl TT, Roorda JC, Jacobson KA, IJzerman AP, Heitman LH.

Biochem Pharmacol. 2018 Jul;153:248-259. doi: 10.1016/j.bcp.2017.12.026. Epub 2018 Jan 3.

29.

Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor.

Eddy MT, Lee MY, Gao ZG, White KL, Didenko T, Horst R, Audet M, Stanczak P, McClary KM, Han GW, Jacobson KA, Stevens RC, Wüthrich K.

Cell. 2018 Jan 11;172(1-2):68-80.e12. doi: 10.1016/j.cell.2017.12.004. Epub 2017 Dec 28.

30.

Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners.

Duroux R, Ciancetta A, Mannes P, Yu J, Boyapati S, Gizewski E, Yous S, Ciruela F, Auchampach JA, Gao ZG, Jacobson KA.

Medchemcomm. 2017 Aug 1;8(8):1659-1667. doi: 10.1039/C7MD00247E. Epub 2017 Jun 22.

31.

On the G protein-coupling selectivity of the native A2B adenosine receptor.

Gao ZG, Inoue A, Jacobson KA.

Biochem Pharmacol. 2018 May;151:201-213. doi: 10.1016/j.bcp.2017.12.003. Epub 2017 Dec 7.

32.

Breakthrough in GPCR Crystallography and Its Impact on Computer-Aided Drug Design.

Ciancetta A, Jacobson KA.

Methods Mol Biol. 2018;1705:45-72. doi: 10.1007/978-1-4939-7465-8_3.

33.

Demystifying P2Y1 Receptor Ligand Recognition through Docking and Molecular Dynamics Analyses.

Ciancetta A, O'Connor RD, Paoletta S, Jacobson KA.

J Chem Inf Model. 2017 Dec 26;57(12):3104-3123. doi: 10.1021/acs.jcim.7b00528. Epub 2017 Nov 28.

34.

Species differences and mechanism of action of A3 adenosine receptor allosteric modulators.

Du L, Gao ZG, Paoletta S, Wan TC, Gizewski ET, Barbour S, van Veldhoven JPD, IJzerman AP, Jacobson KA, Auchampach JA.

Purinergic Signal. 2018 Mar;14(1):59-71. doi: 10.1007/s11302-017-9592-1. Epub 2017 Nov 23.

35.

Purinergic drug targets for gastrointestinal disorders.

Burnstock G, Jacobson KA, Christofi FL.

Curr Opin Pharmacol. 2017 Dec;37:131-141. doi: 10.1016/j.coph.2017.10.011. Epub 2017 Nov 14. Review.

36.

Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor.

Gao ZG, Jacobson KA.

Mol Pharmacol. 2017 Nov;92(5):613-626. doi: 10.1124/mol.117.109660. Epub 2017 Sep 1.

37.

Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential.

Yu J, Ahn S, Kim HJ, Lee M, Ahn S, Kim J, Jin SH, Lee E, Kim G, Cheong JH, Jacobson KA, Jeong LS, Noh M.

J Med Chem. 2017 Sep 14;60(17):7459-7475. doi: 10.1021/acs.jmedchem.7b00805. Epub 2017 Aug 28.

38.

Polypharmacology of conformationally locked methanocarba nucleosides.

Jacobson KA, Tosh DK, Toti KS, Ciancetta A.

Drug Discov Today. 2017 Dec;22(12):1782-1791. doi: 10.1016/j.drudis.2017.07.013. Epub 2017 Aug 3. Review.

39.

Fragment optimization for GPCRs by molecular dynamics free energy calculations: Probing druggable subpockets of the A 2A adenosine receptor binding site.

Matricon P, Ranganathan A, Warnick E, Gao ZG, Rudling A, Lambertucci C, Marucci G, Ezzati A, Jaiteh M, Dal Ben D, Jacobson KA, Carlsson J.

Sci Rep. 2017 Jul 25;7(1):6398. doi: 10.1038/s41598-017-04905-0.

40.

A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy.

Jacobson KA, Merighi S, Varani K, Borea PA, Baraldi S, Aghazadeh Tabrizi M, Romagnoli R, Baraldi PG, Ciancetta A, Tosh DK, Gao ZG, Gessi S.

Med Res Rev. 2018 Jul;38(4):1031-1072. doi: 10.1002/med.21456. Epub 2017 Jul 6. Review.

41.

Highly selective A3 adenosine receptor agonists relieve chronic neuropathic pain.

Salvemini D, Jacobson KA.

Expert Opin Ther Pat. 2017 Aug;27(8):967. doi: 10.1080/13543776.2017.1341018. Epub 2017 Jun 20. No abstract available.

42.

Exploring the Role of N6-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice ∇.

Petrelli R, Scortichini M, Kachler S, Boccella S, Cerchia C, Torquati I, Del Bello F, Salvemini D, Novellino E, Luongo L, Maione S, Jacobson KA, Lavecchia A, Klotz KN, Cappellacci L.

J Med Chem. 2017 May 25;60(10):4327-4341. doi: 10.1021/acs.jmedchem.7b00291. Epub 2017 May 5.

43.

N6-Substituted 5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation.

Yu J, Zhao LX, Park J, Lee HW, Sahu PK, Cui M, Moss SM, Hammes E, Warnick E, Gao ZG, Noh M, Choi S, Ahn HC, Choi J, Jacobson KA, Jeong LS.

J Med Chem. 2017 Apr 27;60(8):3422-3437. doi: 10.1021/acs.jmedchem.7b00241. Epub 2017 Apr 19.

44.

Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.

Tosh DK, Janowsky A, Eshleman AJ, Warnick E, Gao ZG, Chen Z, Gizewski E, Auchampach JA, Salvemini D, Jacobson KA.

J Med Chem. 2017 Apr 13;60(7):3109-3123. doi: 10.1021/acs.jmedchem.7b00141. Epub 2017 Mar 20.

45.

Structural Probing and Molecular Modeling of the A₃ Adenosine Receptor: A Focus on Agonist Binding.

Ciancetta A, Jacobson KA.

Molecules. 2017 Mar 11;22(3). pii: E449. doi: 10.3390/molecules22030449. Review.

46.

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists.

Tosh DK, Ciancetta A, Warnick E, Crane S, Gao ZG, Jacobson KA.

J Med Chem. 2016 Dec 22;59(24):11006-11026. doi: 10.1021/acs.jmedchem.6b01183. Epub 2016 Dec 9.

47.

Hypothermia in mouse is caused by adenosine A1 and A3 receptor agonists and AMP via three distinct mechanisms.

Carlin JL, Jain S, Gizewski E, Wan TC, Tosh DK, Xiao C, Auchampach JA, Jacobson KA, Gavrilova O, Reitman ML.

Neuropharmacology. 2017 Mar 1;114:101-113. doi: 10.1016/j.neuropharm.2016.11.026. Epub 2016 Nov 30.

48.

Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists.

Rodríguez D, Chakraborty S, Warnick E, Crane S, Gao ZG, O'Connor R, Jacobson KA, Carlsson J.

ACS Chem Biol. 2016 Oct 21;11(10):2763-2772. Epub 2016 Aug 22.

49.

Ocular Purine Receptors as Drug Targets in the Eye.

Jacobson KA, Civan MM.

J Ocul Pharmacol Ther. 2016 Oct;32(8):534-547. Epub 2016 Aug 30. Review.

50.

Inherited dysfunctional platelet P2Y12 receptor mutations associated with bleeding disorders.

Lecchi A, Femia EA, Paoletta S, Dupuis A, Ohlmann P, Gachet C, Jacobson KA, Machura K, Podda GM, Zieger B, Cattaneo M.

Hamostaseologie. 2016 Nov 7;36(4):279-283. Epub 2016 Aug 4. Review.

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