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Items: 1 to 20 of 101

1.

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.

PMID:
27742837
2.

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.

3.

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.

4.

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.

5.

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):4733-9. doi: 10.1016/j.bmcl.2015.08.021.

6.

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. Review.

7.

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. Review.

8.

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.

9.

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.

10.

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.

11.

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.

12.

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.

13.

Enigmatic GPCR finds a stimulating drug.

Harden TK.

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

PMID:
24150253
14.

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.

15.

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.

16.

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.

17.

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.

18.

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.

19.
20.

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.

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