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Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates.

Klutz AM, Gao ZG, Lloyd J, Shainberg A, Jacobson KA.

J Nanobiotechnology. 2008 Oct 23;6:12. doi: 10.1186/1477-3155-6-12.


Polyamidoamine (PAMAM) dendrimer conjugates of "clickable" agonists of the A3 adenosine receptor and coactivation of the P2Y14 receptor by a tethered nucleotide.

Tosh DK, Yoo LS, Chinn M, Hong K, Kilbey SM 2nd, Barrett MO, Fricks IP, Harden TK, Gao ZG, Jacobson KA.

Bioconjug Chem. 2010 Feb 17;21(2):372-84. doi: 10.1021/bc900473v.


GPCR ligand dendrimer (GLiDe) conjugates: adenosine receptor interactions of a series of multivalent xanthine antagonists.

Kecskés A, Tosh DK, Wei Q, Gao ZG, Jacobson KA.

Bioconjug Chem. 2011 Jun 15;22(6):1115-27. doi: 10.1021/bc1005812. Epub 2011 May 12.


Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts.

Wan TC, Tosh DK, Du L, Gizewski ET, Jacobson KA, Auchampach JA.

BMC Pharmacol. 2011 Oct 31;11:11. doi: 10.1186/1471-2210-11-11.


Application of the functionalized congener approach to dendrimer-based signaling agents acting through A(2A) adenosine receptors.

Kim Y, Klutz AM, Hechler B, Gao ZG, Gachet C, Jacobson KA.

Purinergic Signal. 2009 Mar;5(1):39-50. doi: 10.1007/s11302-008-9113-3. Epub 2008 Jul 4.


PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G protein-coupled receptors.

Kim Y, Hechler B, Gao ZG, Gachet C, Jacobson KA.

Bioconjug Chem. 2009 Oct 21;20(10):1888-98. doi: 10.1021/bc9001689. Epub 2009 Sep 28.


Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.

Baraldi PG, Cacciari B, Pineda de Las Infantas MJ, Romagnoli R, Spalluto G, Volpini R, Costanzi S, Vittori S, Cristalli G, Melman N, Park KS, Ji XD, Jacobson KA.

J Med Chem. 1998 Aug 13;41(17):3174-85.


Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition.

Tosh DK, Phan K, Deflorian F, Wei Q, Yoo LS, Gao ZG, Jacobson KA.

Bioconjug Chem. 2012 Feb 15;23(2):232-47. doi: 10.1021/bc200526c. Epub 2012 Jan 11.


Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists.

Das A, Sanjayan GJ, Kecskés M, Yoo L, Gao ZG, Jacobson KA.

J Nanobiotechnology. 2010 May 17;8:11. doi: 10.1186/1477-3155-8-11.


Functionalized congeners of P2Y1 receptor antagonists: 2-alkynyl (N)-methanocarba 2'-deoxyadenosine 3',5'-bisphosphate analogues and conjugation to a polyamidoamine (PAMAM) dendrimer carrier.

de Castro S, Maruoka H, Hong K, Kilbey SM 2nd, Costanzi S, Hechler B, Brown GG Jr, Gachet C, Harden TK, Jacobson KA.

Bioconjug Chem. 2010 Jul 21;21(7):1190-205. doi: 10.1021/bc900569u.


Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.

Klotz KN, Hessling J, Hegler J, Owman C, Kull B, Fredholm BB, Lohse MJ.

Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):1-9.


Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.

Li AH, Moro S, Forsyth N, Melman N, Ji XD, Jacobson KA.

J Med Chem. 1999 Feb 25;42(4):706-21.


Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.

Gallo-Rodriguez C, Ji XD, Melman N, Siegman BD, Sanders LH, Orlina J, Fischer B, Pu Q, Olah ME, van Galen PJ, et al.

J Med Chem. 1994 Mar 4;37(5):636-46.


Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic myocardial injury.

Tracey WR, Magee WP, Oleynek JJ, Hill RJ, Smith AH, Flynn DM, Knight DR.

Am J Physiol Heart Circ Physiol. 2003 Dec;285(6):H2780-7. Epub 2003 Aug 14.


Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.

Kim YC, de Zwart M, Chang L, Moro S, von Frijtag Drabbe Künzel JK, Melman N, IJzerman AP, Jacobson KA.

J Med Chem. 1998 Jul 16;41(15):2835-45.


Enhanced potency of nucleotide-dendrimer conjugates as agonists of the P2Y14 receptor: multivalent effect in G protein-coupled receptor recognition.

Das A, Zhou Y, Ivanov AA, Carter RL, Harden TK, Jacobson KA.

Bioconjug Chem. 2009 Aug 19;20(8):1650-9. doi: 10.1021/bc900206g. Epub 2009 Jul 2.


5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.

Da Settimo F, Primofiore G, Taliani S, Marini AM, La Motta C, Simorini F, Salerno S, Sergianni V, Tuccinardi T, Martinelli A, Cosimelli B, Greco G, Novellino E, Ciampi O, Trincavelli ML, Martini C.

J Med Chem. 2007 Nov 15;50(23):5676-84. Epub 2007 Oct 10.


Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.

Tosh DK, Chinn M, Ivanov AA, Klutz AM, Gao ZG, Jacobson KA.

J Med Chem. 2009 Dec 10;52(23):7580-92. doi: 10.1021/jm900426g.


2-Substituted N-ethylcarboxamidoadenosine derivatives as high-affinity agonists at human A3 adenosine receptors.

Klotz KN, Camaioni E, Volpini R, Kachler S, Vittori S, Cristalli G.

Naunyn Schmiedebergs Arch Pharmacol. 1999 Aug;360(2):103-8.


Molecular cloning and characterization of an adenosine receptor: the A3 adenosine receptor.

Zhou QY, Li C, Olah ME, Johnson RA, Stiles GL, Civelli O.

Proc Natl Acad Sci U S A. 1992 Aug 15;89(16):7432-6.

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