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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.


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 antagonists.

Kim HS, Ohno M, Xu B, Kim HO, Choi Y, Ji XD, Maddileti S, Marquez VE, Harden TK, Jacobson KA.

J Med Chem. 2003 Nov 6;46(23):4974-87.


Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands.

Nandanan E, Jang SY, Moro S, Kim HO, Siddiqui MA, Russ P, Marquez VE, Busson R, Herdewijn P, Harden TK, Boyer JL, Jacobson KA.

J Med Chem. 2000 Mar 9;43(5):829-42.


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.


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.


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.


Development of selective high affinity antagonists, agonists, and radioligands for the P2Y1 receptor.

Houston D, Costanzi S, Jacobson KA, Harden TK.

Comb Chem High Throughput Screen. 2008 Jul;11(6):410-9. Review.


Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors.

Kim HS, Ravi RG, Marquez VE, Maddileti S, Wihlborg AK, Erlinge D, Malmsjö M, Boyer JL, Harden TK, Jacobson KA.

J Med Chem. 2002 Jan 3;45(1):208-18.


Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.

Cattaneo M, Lecchi A, Ohno M, Joshi BV, Besada P, Tchilibon S, Lombardi R, Bischofberger N, Harden TK, Jacobson KA.

Biochem Pharmacol. 2004 Nov 15;68(10):1995-2002.


Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.

Waldo GL, Corbitt J, Boyer JL, Ravi G, Kim HS, Ji XD, Lacy J, Jacobson KA, Harden TK.

Mol Pharmacol. 2002 Nov;62(5):1249-57.


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).

Ohlmann P, de Castro S, Brown GG Jr, Gachet C, Jacobson KA, Harden TK.

Pharmacol Res. 2010 Oct;62(4):344-51. doi: 10.1016/j.phrs.2010.05.007. Epub 2010 Jun 4.


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.


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 mice.

Hechler B, Nonne C, Roh EJ, Cattaneo M, Cazenave JP, Lanza F, Jacobson KA, Gachet C.

J Pharmacol Exp Ther. 2006 Feb;316(2):556-63. Epub 2005 Oct 19.


Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.

Ravi RG, Kim HS, Servos J, Zimmermann H, Lee K, Maddileti S, Boyer JL, Harden TK, Jacobson KA.

J Med Chem. 2002 May 9;45(10):2090-100.


Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors.

Camaioni E, Boyer JL, Mohanram A, Harden TK, Jacobson KA.

J Med Chem. 1998 Jan 15;41(2):183-90.


Nucleotide analogues containing 2-oxa-bicyclo[2.2.1]heptane and l-alpha-threofuranosyl ring systems: interactions with P2Y receptors.

Ohno M, Costanzi S, Kim HS, Kempeneers V, Vastmans K, Herdewijn P, Maddileti S, Gao ZG, Harden TK, Jacobson KA.

Bioorg Med Chem. 2004 Nov 1;12(21):5619-30.


Synthesis and biological activity of 2-alkylated deoxyadenosine bisphosphate derivatives as P2Y(1) receptor antagonists.

Mathieu R, Baurand A, Schmitt M, Gachet C, Bourguignon JJ.

Bioorg Med Chem. 2004 Apr 1;12(7):1769-79.


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.

Chhatriwala M, Ravi RG, Patel RI, Boyer JL, Jacobson KA, Harden TK.

J Pharmacol Exp Ther. 2004 Dec;311(3):1038-43. Epub 2004 Sep 2.

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