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Items: 1 to 50 of 83

1.

Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats.

Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Yan W, Merton KP, Schoetens F, Ma JY, Skaptason J, Gao J, Tran DT, Venkatesan H, Rosen MD, Shankley NP, Rabinowitz MH.

Br J Pharmacol. 2015 Aug;172(16):4078-88. doi: 10.1111/bph.13188. Epub 2015 Jun 26.

2.

The cholecystokinin CCK2 receptor antagonist, JNJ-26070109, inhibits gastric acid secretion and prevents omeprazole-induced acid rebound in the rat.

Barrett TD, Lagaud G, Wagaman P, Freedman JM, Yan W, Andries L, Rizzolio MC, Morton MF, Shankley NP.

Br J Pharmacol. 2012 Jul;166(5):1684-93. doi: 10.1111/j.1476-5381.2012.01878.x.

3.

JNJ-26070109 [(R)4-bromo-N-[1-(2,4-difluoro-phenyl)-ethyl]-2-(quinoxaline-5-sulfonylamino)-benzamide]: a novel, potent, and selective cholecystokinin 2 receptor antagonist with good oral bioavailability.

Morton MF, Barrett TD, Freedman J, Li L, Rizzolio MC, Prendergast CE, Wu X, Moreno V, Pyati J, Figueroa K, Cagnon L, Lagaud G, Ver Donck L, Ghoos E, Allison B, Rabinowitz MH, Shankley NP.

J Pharmacol Exp Ther. 2011 Jul;338(1):328-36. doi: 10.1124/jpet.110.178483. Epub 2011 Apr 14.

PMID:
21493750
4.

The scientific legacy of Sir James W. Black.

Page CP, Schaffhausen J, Shankley NP.

Trends Pharmacol Sci. 2011 Apr;32(4):181-2. doi: 10.1016/j.tips.2011.02.009. Epub 2011 Mar 31. No abstract available.

PMID:
21458082
5.

Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor.

Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Haug PV, Yan W, Young A, Hua H, Hart JC, Tran DT, Venkatesan H, Rosen MD, Peltier HM, Sepassi K, Rizzolio MC, Bembenek SD, Mirzadegan T, Rabinowitz MH, Shankley NP.

Mol Pharmacol. 2011 Jun;79(6):910-20. doi: 10.1124/mol.110.070508. Epub 2011 Mar 3.

PMID:
21372172
6.

Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.

Rosen MD, Venkatesan H, Peltier HM, Bembenek SD, Kanelakis KC, Zhao LX, Leonard BE, Hocutt FM, Wu X, Palomino HL, Brondstetter TI, Haugh PV, Cagnon L, Yan W, Liotta LA, Young A, Mirzadegan T, Shankley NP, Barrett TD, Rabinowitz MH.

ACS Med Chem Lett. 2010 Oct 5;1(9):526-9. doi: 10.1021/ml100198y. eCollection 2010 Dec 9.

7.

An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation. 1985.

Black JW, Leff P, Shankley NP, Wood J.

Br J Pharmacol. 2010 Jul;160 Suppl 1:S54-64. doi: 10.1111/j.1476-5381.2010.00855.x. No abstract available.

8.

Functional Characterization of the Canine Heme-Regulated eIF2alpha Kinase: Regulation of Protein Synthesis.

Kanelakis KC, Pyati J, Wagaman PC, Chuang JC, Yang Y, Shankley NP.

Adv Hematol. 2009;2009:251915. doi: 10.1155/2009/251915. Epub 2009 Jun 22.

9.

Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase.

Rosen MD, Woods CR, Goldberg SD, Hack MD, Bounds AD, Yang Y, Wagaman PC, Phuong VK, Ameriks AP, Barrett TD, Kanelakis KC, Chuang JC, Shankley NP, Rabinowitz MH.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6548-51. doi: 10.1016/j.bmcl.2009.10.033. Epub 2009 Oct 13. Erratum in: Bioorg Med Chem Lett. 2010 Jun 15;20(12):3834. Chang, Jui [corrected to Chuang, Jui Chang].

PMID:
19854648
10.

Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: tuning of receptor selectivity and in vivo efficacy.

Pippel M, Boyce K, Venkatesan H, Phuong VK, Yan W, Barrett TD, Lagaud G, Li L, Morton MF, Prendergast C, Wu X, Shankley NP, Rabinowitz MH.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6376-8. doi: 10.1016/j.bmcl.2009.09.065. Epub 2009 Sep 23.

PMID:
19815410
11.

Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.

Pippel M, Allison BD, Phuong VK, Li L, Morton MF, Prendergast C, Wu X, Shankley NP, Rabinowitz MH.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6373-5. doi: 10.1016/j.bmcl.2009.09.064. Epub 2009 Sep 23.

PMID:
19811913
12.

Characterization of a robust enzymatic assay for inhibitors of 2-oxoglutarate-dependent hydroxylases.

Kanelakis KC, Palomino HL, Li L, Wu J, Yan W, Rosen MD, Rizzolio MC, Trivedi M, Morton MF, Yang Y, Venkatesan H, Rabinowitz MH, Shankley NP, Barrett TD.

J Biomol Screen. 2009 Jul;14(6):627-35. doi: 10.1177/1087057109333976. Epub 2009 Jun 4.

PMID:
19498081
13.

Role of CCK and potential utility of CCK1 receptor antagonism in the treatment of pancreatitis induced by biliary tract obstruction.

Barrett TD, Yan W, Freedman JM, Lagaud GJ, Breitenbucher JG, Shankley NP.

Br J Pharmacol. 2008 Apr;153(8):1650-8. doi: 10.1038/bjp.2008.44. Epub 2008 Feb 25.

14.

Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis.

Rosen MD, Hack MD, Allison BD, Phuong VK, Woods CR, Morton MF, Prendergast CE, Barrett TD, Schubert C, Li L, Wu X, Wu J, Freedman JM, Shankley NP, Rabinowitz MH.

Bioorg Med Chem. 2008 Apr 1;16(7):3917-25. doi: 10.1016/j.bmc.2008.01.059. Epub 2008 Feb 5.

PMID:
18289861
15.

Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands.

Woods CR, Hack MD, Allison BD, Phuong VK, Rosen MD, Morton MF, Prendergast CE, Barrett TD, Shankley NP, Rabinowitz MH.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6905-9. Epub 2007 Sep 29.

PMID:
18029172
16.

Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs.

Bhattacharya A, Scott BP, Nasser N, Ao H, Maher MP, Dubin AE, Swanson DM, Shankley NP, Wickenden AD, Chaplan SR.

J Pharmacol Exp Ther. 2007 Nov;323(2):665-74. Epub 2007 Aug 9.

PMID:
17690251
17.

3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide.

Morton MF, Barrett TD, Yan W, Freedman JM, Lagaud G, Prendergast CE, Moreno V, Pyati J, Figueroa K, Li L, Wu X, Rizzolio M, Breitenbucher JG, McClure K, Shankley NP.

J Pharmacol Exp Ther. 2007 Nov;323(2):562-9. Epub 2007 Aug 7.

PMID:
17684117
18.

Obestatin reduces food intake and suppresses body weight gain in rodents.

Lagaud GJ, Young A, Acena A, Morton MF, Barrett TD, Shankley NP.

Biochem Biophys Res Commun. 2007 May 25;357(1):264-9. Epub 2007 Mar 30. Retraction in: Biochem Biophys Res Commun. 2009 Oct 23;388(3):619.

PMID:
17418097
19.
20.

Unexpected relationship between plasma protein binding and the pharmacodynamics of 2-NAP, a CCK1-receptor antagonist.

Gerskowitch VP, Hodge J, Hull RA, Shankley NP, Kalindjian SB, McEwen J, Black JW.

Br J Clin Pharmacol. 2007 May;63(5):618-22. Epub 2006 Oct 17.

21.

Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.

Allison BD, Phuong VK, McAtee LC, Rosen M, Morton M, Prendergast C, Barrett T, Lagaud G, Freedman J, Li L, Wu X, Venkatesan H, Pippel M, Woods C, Rizzolio MC, Hack M, Hoey K, Deng X, King C, Shankley NP, Rabinowitz MH.

J Med Chem. 2006 Oct 19;49(21):6371-90.

PMID:
17034143
22.

Neuromedin U stimulates contraction of human long saphenous vein and gastrointestinal smooth muscle in vitro.

Jones NA, Morton MF, Prendergast CE, Powell GL, Shankley NP, Hollingsworth SJ.

Regul Pept. 2006 Sep 11;136(1-3):109-16. Epub 2006 Jun 19.

PMID:
16782214
23.
24.

Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.

Buck IM, Black JW, Cooke T, Dunstone DJ, Gaffen JD, Griffin EP, Harper EA, Hull RA, Kalindjian SB, Lilley EJ, Linney ID, Low CM, McDonald IM, Pether MJ, Roberts SP, Shankley NP, Shaxted ME, Steel KI, Sykes DA, Tozer MJ, Watt GF, Walker MK, Wright L, Wright PT.

J Med Chem. 2005 Nov 3;48(22):6803-12.

PMID:
16250639
25.

Scaffold hopping with molecular field points: identification of a cholecystokinin-2 (CCK2) receptor pharmacophore and its use in the design of a prototypical series of pyrrole- and imidazole-based CCK2 antagonists.

Low CM, Buck IM, Cooke T, Cushnir JR, Kalindjian SB, Kotecha A, Pether MJ, Shankley NP, Vinter JG, Wright L.

J Med Chem. 2005 Nov 3;48(22):6790-802.

PMID:
16250638
26.

A novel, quantitative bio-assay for cholecystokinin type-1 receptor activity in the anaesthetised rat.

Freedman JM, Barrett TD, Shankley NP.

J Pharmacol Toxicol Methods. 2006 Jul-Aug;54(1):36-41. Epub 2005 Oct 24.

PMID:
16246596
27.

Pharmacological analysis of CCK2 receptors up-regulated using engineered transcription factors.

Morton MF, Liu PQ, Reik A, de la Rosa R, Mendel M, Li XY, Case C, Pabo C, Moreno V, Pyati J, Shankley NP.

Regul Pept. 2005 Jul 15;129(1-3):227-32.

PMID:
15927720
28.

Molecular cloning, expression and pharmacological characterization of the canine cholecystokinin 1 receptor.

Morton MF, Pyati J, Dai H, Li L, Moreno V, Shankley NP.

Br J Pharmacol. 2005 Jun;145(3):374-84.

29.

TNF alpha reduces tachykinin, PGE2-dependent, relaxation of the cultured mouse trachea by increasing the activity of COX-2.

Bachar O, Rose AC, Adner M, Wang X, Prendergast CE, Kempf A, Shankley NP, Cardell LO.

Br J Pharmacol. 2005 Jan;144(2):220-30.

30.

Cell lines for drug discovery: elevating target-protein levels using engineered transcription factors.

Liu PQ, Morton MF, Reik A, de la Rosa R, Mendel MC, Li XY, Case CC, Pabo CO, Moreno V, Kempf A, Pyati J, Shankley NP.

J Biomol Screen. 2004 Feb;9(1):44-51.

PMID:
15006148
31.

Pharmacological comparison of the alternatively spliced short and long CCK2 receptors.

Morton MF, Harper EA, Tavares IA, Shankley NP.

Br J Pharmacol. 2003 Sep;140(1):218-24. Epub 2003 Aug 4.

32.

An assay to evaluate the long-term effects of inflammatory mediators on murine airway smooth muscle: evidence that TNFalpha up-regulates 5-HT(2A)-mediated contraction.

Adner M, Rose AC, Zhang Y, Swärd K, Benson M, Uddman R, Shankley NP, Cardell LO.

Br J Pharmacol. 2002 Dec;137(7):971-82.

33.

Pharmacological evidence for putative CCK(1) receptor heterogeneity in human colon smooth muscle.

Morton MF, Harper EA, Tavares IA, Shankley NP.

Br J Pharmacol. 2002 Jul;136(6):873-82.

34.

Pharmacological characterization of cholecystokinin receptors mediating contraction of human gallbladder and ascending colon.

Morton MF, Welsh NJ, Tavares IA, Shankley NP.

Regul Pept. 2002 Apr 15;105(1):59-64.

PMID:
11853872
35.

Histamine receptor assays.

Shankley NP, Morton MF, Watt GF.

Curr Protoc Pharmacol. 2001 Nov;Chapter 4:Unit4.17. doi: 10.1002/0471141755.ph0417s14.

PMID:
21959758
36.

Comparison of ligand affinity values at the recombinant human H3 receptor and at H3 receptor(s) of human cingulate cortex.

Harper EA, Lovenberg TW, Shankley NP, Black JW.

Inflamm Res. 2001 Apr;50 Suppl 2:S106-7. No abstract available.

PMID:
11411576
37.

Nonpeptide cholecystokinin-2 receptor agonists.

Kalindjian SB, Dunstone DJ, Low CM, Pether MJ, Roberts SP, Tozer MJ, Watt GF, Shankley NP.

J Med Chem. 2001 Apr 12;44(8):1125-33.

PMID:
11312913
38.

Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.

Low CM, Black JW, Broughton HB, Buck IM, Davies JM, Dunstone DJ, Hull RA, Kalindjian SB, McDonald IM, Pether MJ, Shankley NP, Steel KI.

J Med Chem. 2000 Sep 21;43(19):3505-17.

PMID:
11000005
39.

Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.

Linney ID, Buck IM, Harper EA, Kalindjian SB, Pether MJ, Shankley NP, Watt GF, Wright PT.

J Med Chem. 2000 Jun 15;43(12):2362-70.

PMID:
10882362
40.

An improved in vitro bioassay for the study of 5-HT(4) receptors in the human isolated large intestinal circular muscle.

Prins NH, Shankley NP, Welsh NJ, Briejer MR, Lefebvre RA, Akkermans LM, Schuurkes JA.

Br J Pharmacol. 2000 Apr;129(8):1601-8.

42.
44.

From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.

Tozer MJ, Harper EA, Kalindjian SB, Pether MJ, Shankley NP, Watt GF.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1825-30. Erratum in: Bioorg Med Chem Lett 1999 Oct 18;9(20):3061.

PMID:
10406649
45.
46.
47.
48.

Pharmacological classification of adenosine receptors in the sinoatrial and atrioventricular nodes of the guinea-pig.

Meester BJ, Shankley NP, Welsh NJ, Wood J, Meijler FL, Black JW.

Br J Pharmacol. 1998 Jun;124(4):685-92.

49.

International Union of Pharmacology. XIII. Classification of histamine receptors.

Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL.

Pharmacol Rev. 1997 Sep;49(3):253-78. Review. No abstract available.

PMID:
9311023
50.

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