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Items: 1 to 50 of 287

1.

A membrane-associated, fluorogenic reporter for mammalian phospholipase C isozymes.

Huang W, Wang X, Endo-Streeter S, Barrett M, Waybright J, Wohlfeld C, Hajicek N, Harden TK, Sondek J, Zhang Q.

J Biol Chem. 2018 Feb 2;293(5):1728-1735. doi: 10.1074/jbc.RA117.000926. Epub 2017 Dec 20.

2.

Potent and Selective Peptide-based Inhibition of the G Protein Gαq.

Charpentier TH, Waldo GL, Lowery-Gionta EG, Krajewski K, Strahl BD, Kash TL, Harden TK, Sondek J.

J Biol Chem. 2016 Dec 2;291(49):25608-25616. Epub 2016 Oct 14.

3.

UDP-glucose promotes neutrophil recruitment in the lung.

Sesma JI, Weitzer CD, Livraghi-Butrico A, Dang H, Donaldson S, Alexis NE, Jacobson KA, Harden TK, Lazarowski ER.

Purinergic Signal. 2016 Dec;12(4):627-635. Epub 2016 Jul 15.

4.

Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.

Junker A, Balasubramanian R, Ciancetta A, Uliassi E, Kiselev E, Martiriggiano C, Trujillo K, Mtchedlidze G, Birdwell L, Brown KA, Harden TK, Jacobson KA.

J Med Chem. 2016 Jul 14;59(13):6149-68. doi: 10.1021/acs.jmedchem.6b00044. Epub 2016 Jun 22.

5.

The experimental power of FR900359 to study Gq-regulated biological processes.

Schrage R, Schmitz AL, Gaffal E, Annala S, Kehraus S, Wenzel D, Büllesbach KM, Bald T, Inoue A, Shinjo Y, Galandrin S, Shridhar N, Hesse M, Grundmann M, Merten N, Charpentier TH, Martz M, Butcher AJ, Slodczyk T, Armando S, Effern M, Namkung Y, Jenkins L, Horn V, Stößel A, Dargatz H, Tietze D, Imhof D, Galés C, Drewke C, Müller CE, Hölzel M, Milligan G, Tobin AB, Gomeza J, Dohlman HG, Sondek J, Harden TK, Bouvier M, Laporte SA, Aoki J, Fleischmann BK, Mohr K, König GM, Tüting T, Kostenis E.

Nat Commun. 2015 Dec 14;6:10156. doi: 10.1038/ncomms10156.

6.

Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor.

Kiselev E, Balasubramanian R, Uliassi E, Brown KA, Trujillo K, Katritch V, Hammes E, Stevens RC, Harden TK, Jacobson KA.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4733-4739. doi: 10.1016/j.bmcl.2015.08.021. Epub 2015 Aug 10.

7.

The First 50 Years of Molecular Pharmacology.

Brown JH, Catterall WA, Conn PJ, Cull-Candy SG, Dingledine R, Harden TK, Insel PA, Milligan G, Traynelis SF.

Mol Pharmacol. 2015 Jul;88(1):139-40. doi: 10.1124/mol.115.099564. Epub 2015 May 5. Review.

PMID:
25943115
8.

UDP-Sugars as Extracellular Signaling Molecules: Cellular and Physiologic Consequences of P2Y14 Receptor Activation.

Lazarowski ER, Harden TK.

Mol Pharmacol. 2015 Jul;88(1):151-60. doi: 10.1124/mol.115.098756. Epub 2015 Mar 31. Review.

9.

Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes.

Kiselev E, Barrett MO, Katritch V, Paoletta S, Weitzer CD, Brown KA, Hammes E, Yin AL, Zhao Q, Stevens RC, Harden TK, Jacobson KA.

ACS Chem Biol. 2014 Dec 19;9(12):2833-42. doi: 10.1021/cb500614p. Epub 2014 Oct 20.

10.

Membrane-induced allosteric control of phospholipase C-β isozymes.

Charpentier TH, Waldo GL, Barrett MO, Huang W, Zhang Q, Harden TK, Sondek J.

J Biol Chem. 2014 Oct 24;289(43):29545-57. doi: 10.1074/jbc.M114.586784. Epub 2014 Sep 5.

11.

A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformation.

Schmitz AL, Schrage R, Gaffal E, Charpentier TH, Wiest J, Hiltensperger G, Morschel J, Hennen S, Häußler D, Horn V, Wenzel D, Grundmann M, Büllesbach KM, Schröder R, Brewitz HH, Schmidt J, Gomeza J, Galés C, Fleischmann BK, Tüting T, Imhof D, Tietze D, Gütschow M, Holzgrabe U, Sondek J, Harden TK, Mohr K, Kostenis E.

Chem Biol. 2014 Jul 17;21(7):890-902. doi: 10.1016/j.chembiol.2014.06.003.

12.

Synthesis of extended uridine phosphonates derived from an allosteric P2Y2 receptor ligand.

Song L, Risseeuw MD, Karalic I, Barrett MO, Brown KA, Harden TK, Van Calenbergh S.

Molecules. 2014 Apr 4;19(4):4313-25. doi: 10.3390/molecules19044313.

13.

4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors.

Jayasekara PS, Barrett MO, Ball CB, Brown KA, Hammes E, Balasubramanian R, Harden TK, Jacobson KA.

J Med Chem. 2014 May 8;57(9):3874-83. doi: 10.1021/jm500367e. Epub 2014 Apr 18.

14.

Enigmatic GPCR finds a stimulating drug.

Harden TK.

Sci Signal. 2013 Oct 22;6(298):pe34. doi: 10.1126/scisignal.2004755.

PMID:
24150253
15.

Is GPR17 a P2Y/leukotriene receptor? examination of uracil nucleotides, nucleotide sugars, and cysteinyl leukotrienes as agonists of GPR17.

Qi AD, Harden TK, Nicholas RA.

J Pharmacol Exp Ther. 2013 Oct;347(1):38-46. doi: 10.1124/jpet.113.207647. Epub 2013 Aug 1.

16.

Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes.

Hajicek N, Charpentier TH, Rush JR, Harden TK, Sondek J.

Biochemistry. 2013 Jul 16;52(28):4810-9. doi: 10.1021/bi400433b. Epub 2013 Jul 9.

17.

A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils.

Barrett MO, Sesma JI, Ball CB, Jayasekara PS, Jacobson KA, Lazarowski ER, Harden TK.

Mol Pharmacol. 2013 Jul;84(1):41-9. doi: 10.1124/mol.113.085654. Epub 2013 Apr 16.

18.

Small molecule inhibitors of phospholipase C from a novel high-throughput screen.

Huang W, Barrett M, Hajicek N, Hicks S, Harden TK, Sondek J, Zhang Q.

J Biol Chem. 2013 Feb 22;288(8):5840-8. doi: 10.1074/jbc.M112.422501. Epub 2013 Jan 7.

19.

G protein-coupled receptor-mediated activation of p110β by Gβγ is required for cellular transformation and invasiveness.

Dbouk HA, Vadas O, Shymanets A, Burke JE, Salamon RS, Khalil BD, Barrett MO, Waldo GL, Surve C, Hsueh C, Perisic O, Harteneck C, Shepherd PR, Harden TK, Smrcka AV, Taussig R, Bresnick AR, Nürnberg B, Williams RL, Backer JM.

Sci Signal. 2012 Dec 4;5(253):ra89. doi: 10.1126/scisignal.2003264.

20.

Fluorescent phosphatidylinositol 4,5-bisphosphate derivatives with modified 6-hydroxy group as novel substrates for phospholipase C.

Wang X, Barrett M, Sondek J, Harden TK, Zhang Q.

Biochemistry. 2012 Jul 3;51(26):5300-6. Epub 2012 Jun 22.

21.

The UDP-sugar-sensing P2Y(14) receptor promotes Rho-mediated signaling and chemotaxis in human neutrophils.

Sesma JI, Kreda SM, Steinckwich-Besancon N, Dang H, García-Mata R, Harden TK, Lazarowski ER.

Am J Physiol Cell Physiol. 2012 Sep 1;303(5):C490-8. doi: 10.1152/ajpcell.00138.2012. Epub 2012 Jun 6.

22.

The phospholipase C isozymes and their regulation.

Gresset A, Sondek J, Harden TK.

Subcell Biochem. 2012;58:61-94. doi: 10.1007/978-94-007-3012-0_3. Review.

23.

A PLCβ/PI3Kγ-GSK3 signaling pathway regulates cofilin phosphatase slingshot2 and neutrophil polarization and chemotaxis.

Tang W, Zhang Y, Xu W, Harden TK, Sondek J, Sun L, Li L, Wu D.

Dev Cell. 2011 Dec 13;21(6):1038-50. doi: 10.1016/j.devcel.2011.10.023.

24.

Mechanism of activation and inactivation of Gq/phospholipase C-β signaling nodes.

Harden TK, Waldo GL, Hicks SN, Sondek J.

Chem Rev. 2011 Oct 12;111(10):6120-9. doi: 10.1021/cr200209p. No abstract available.

25.

Acireductone dioxygenase 1 (ARD1) is an effector of the heterotrimeric G protein beta subunit in Arabidopsis.

Friedman EJ, Wang HX, Jiang K, Perovic I, Deshpande A, Pochapsky TC, Temple BR, Hicks SN, Harden TK, Jones AM.

J Biol Chem. 2011 Aug 26;286(34):30107-18. doi: 10.1074/jbc.M111.227256. Epub 2011 Jun 28.

26.

Molecular pharmacology, physiology, and structure of the P2Y receptors.

von Kügelgen I, Harden TK.

Adv Pharmacol. 2011;61:373-415. doi: 10.1016/B978-0-12-385526-8.00012-6. Review.

PMID:
21586365
27.

Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor.

Maruoka H, Jayasekara MP, Barrett MO, Franklin DA, de Castro S, Kim N, Costanzi S, Harden TK, Jacobson KA.

J Med Chem. 2011 Jun 23;54(12):4018-33. doi: 10.1021/jm101591j. Epub 2011 May 20.

28.

Ser352 and Ser354 in the carboxyl terminus of the human P2Y(1) receptor are required for agonist-promoted phosphorylation and internalization in MDCK cells.

Qi AD, Houston-Cohen D, Naruszewicz I, Harden TK, Nicholas RA.

Br J Pharmacol. 2011 Mar;162(6):1304-13. doi: 10.1111/j.1476-5381.2010.01135.x.

29.

Kinetic scaffolding mediated by a phospholipase C-beta and Gq signaling complex.

Waldo GL, Ricks TK, Hicks SN, Cheever ML, Kawano T, Tsuboi K, Wang X, Montell C, Kozasa T, Sondek J, Harden TK.

Science. 2010 Nov 12;330(6006):974-80. doi: 10.1126/science.1193438. Epub 2010 Oct 21.

30.

Mechanism of phosphorylation-induced activation of phospholipase C-gamma isozymes.

Gresset A, Hicks SN, Harden TK, Sondek J.

J Biol Chem. 2010 Nov 12;285(46):35836-47. doi: 10.1074/jbc.M110.166512. Epub 2010 Aug 31.

31.

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.

32.

Charged residues in the C-terminus of the P2Y1 receptor constitute a basolateral-sorting signal.

Wolff SC, Qi AD, Harden TK, Nicholas RA.

J Cell Sci. 2010 Jul 15;123(Pt 14):2512-20. doi: 10.1242/jcs.060723.

33.

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.

34.

Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications.

Maruoka H, Barrett MO, Ko H, Tosh DK, Melman A, Burianek LE, Balasubramanian R, Berk B, Costanzi S, Harden TK, Jacobson KA.

J Med Chem. 2010 Jun 10;53(11):4488-501. doi: 10.1021/jm100287t.

35.

Signalling and pharmacological properties of the P2Y receptor.

Harden TK, Sesma JI, Fricks IP, Lazarowski ER.

Acta Physiol (Oxf). 2010 Jun;199(2):149-60. doi: 10.1111/j.1748-1716.2010.02116.x. Epub 2010 Mar 24. Review.

36.

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.

37.

Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups.

Das A, Ko H, Burianek LE, Barrett MO, Harden TK, Jacobson KA.

J Med Chem. 2010 Jan 14;53(1):471-80. doi: 10.1021/jm901432g.

38.

Quantification of Gi-mediated inhibition of adenylyl cyclase activity reveals that UDP is a potent agonist of the human P2Y14 receptor.

Carter RL, Fricks IP, Barrett MO, Burianek LE, Zhou Y, Ko H, Das A, Jacobson KA, Lazarowski ER, Harden TK.

Mol Pharmacol. 2009 Dec;76(6):1341-8. doi: 10.1124/mol.109.058578. Epub 2009 Sep 16.

39.

Nucleotides released by apoptotic cells act as a find-me signal to promote phagocytic clearance.

Elliott MR, Chekeni FB, Trampont PC, Lazarowski ER, Kadl A, Walk SF, Park D, Woodson RI, Ostankovich M, Sharma P, Lysiak JJ, Harden TK, Leitinger N, Ravichandran KS.

Nature. 2009 Sep 10;461(7261):282-6. doi: 10.1038/nature08296.

40.

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.

41.

Molecular recognition in the P2Y(14) receptor: Probing the structurally permissive terminal sugar moiety of uridine-5'-diphosphoglucose.

Ko H, Das A, Carter RL, Fricks IP, Zhou Y, Ivanov AA, Melman A, Joshi BV, Kovác P, Hajduch J, Kirk KL, Harden TK, Jacobson KA.

Bioorg Med Chem. 2009 Jul 15;17(14):5298-311. doi: 10.1016/j.bmc.2009.05.024. Epub 2009 May 15.

42.

Gi-dependent cell signaling responses of the human P2Y14 receptor in model cell systems.

Fricks IP, Carter RL, Lazarowski ER, Harden TK.

J Pharmacol Exp Ther. 2009 Jul;330(1):162-8. doi: 10.1124/jpet.109.150730. Epub 2009 Apr 1.

43.

Aberrant receptor internalization and enhanced FRS2-dependent signaling contribute to the transforming activity of the fibroblast growth factor receptor 2 IIIb C3 isoform.

Cha JY, Maddileti S, Mitin N, Harden TK, Der CJ.

J Biol Chem. 2009 Mar 6;284(10):6227-40. doi: 10.1074/jbc.M803998200. Epub 2008 Dec 22.

44.

Phospholipase C isozymes as effectors of Ras superfamily GTPases.

Harden TK, Hicks SN, Sondek J.

J Lipid Res. 2009 Apr;50 Suppl:S243-8. doi: 10.1194/jlr.R800045-JLR200. Epub 2008 Nov 24.

45.

Dual activation of phospholipase C-epsilon by Rho and Ras GTPases.

Seifert JP, Zhou Y, Hicks SN, Sondek J, Harden TK.

J Biol Chem. 2008 Oct 31;283(44):29690-8. doi: 10.1074/jbc.M805038200. Epub 2008 Sep 2.

46.

General and versatile autoinhibition of PLC isozymes.

Hicks SN, Jezyk MR, Gershburg S, Seifert JP, Harden TK, Sondek J.

Mol Cell. 2008 Aug 8;31(3):383-94. doi: 10.1016/j.molcel.2008.06.018.

47.

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.

48.

Development of selective agonists and antagonists of P2Y receptors.

Jacobson KA, Ivanov AA, de Castro S, Harden TK, Ko H.

Purinergic Signal. 2009 Mar;5(1):75-89. doi: 10.1007/s11302-008-9106-2. Epub 2008 Jul 4.

49.

Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.

Ko H, Carter RL, Cosyn L, Petrelli R, de Castro S, Besada P, Zhou Y, Cappellacci L, Franchetti P, Grifantini M, Van Calenbergh S, Harden TK, Jacobson KA.

Bioorg Med Chem. 2008 Jun 15;16(12):6319-32. doi: 10.1016/j.bmc.2008.05.013. Epub 2008 May 9.

50.

Ligand and structure-based methodologies for the prediction of the activity of G protein-coupled receptor ligands.

Costanzi S, Tikhonova IG, Harden TK, Jacobson KA.

J Comput Aided Mol Des. 2009 Nov;23(11):747-54. doi: 10.1007/s10822-008-9218-3. Epub 2008 May 16.

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