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Items: 21


Beyond Traditional Structure-Based Drug Design: The Role of Iron Complexation, Strain, and Water in the Binding of Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylase 2.

Bembenek SD, Venkatesan H, Peltier HM, Rosen MD, Barrett TD, Kanelakis KC, Palomino HL, Brondstetter TI, Mirzadegan T, Rabinowitz MH.

ACS Omega. 2019 Apr 30;4(4):6703-6708. doi: 10.1021/acsomega.9b00199. Epub 2019 Apr 12.


Glutamatergic stimulation induces GluN2B translation by the nitric oxide-Heme-Regulated eIF2α kinase in cortical neurons.

Ramos-Fernández E, Tajes M, Ill-Raga G, Vargas L, Busquets-García A, Bosch-Morató M, Guivernau B, Valls-Comamala V, Gomis M, Grau C, Fandos C, Rosen MD, Rabinowitz MH, Inestrosa N, Maldonado R, Altafaj X, Ozaita A, Alvarez A, Vicente R, Valverde MA, Muñoz FJ.

Oncotarget. 2016 Sep 13;7(37):58876-58892. doi: 10.18632/oncotarget.11417.


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.


Physiological Control of Nitric Oxide in Neuronal BACE1 Translation by Heme-Regulated eIF2α Kinase HRI Induces Synaptogenesis.

Ill-Raga G, Tajes M, Busquets-García A, Ramos-Fernández E, Vargas LM, Bosch-Morató M, Guivernau B, Valls-Comamala V, Eraso-Pichot A, Guix FX, Fandos C, Rosen MD, Rabinowitz MH, Maldonado R, Alvarez AR, Ozaita A, Muñoz FJ.

Antioxid Redox Signal. 2015 May 20;22(15):1295-307. doi: 10.1089/ars.2014.6080. Epub 2015 Mar 25.


Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.

Rabinowitz MH.

J Med Chem. 2013 Dec 12;56(23):9369-402. doi: 10.1021/jm400386j. Epub 2013 Aug 27. Review.


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.


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.


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.


A one-step synthesis of 2,4-unsubstituted quinoline-3-carboxylic acid esters from o-nitrobenzaldehydes.

Venkatesan H, Hocutt FM, Jones TK, Rabinowitz MH.

J Org Chem. 2010 May 21;75(10):3488-91. doi: 10.1021/jo100392x.


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].


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.


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.


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.


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.


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.


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.


Substrate specificity and novel selective inhibitors of TNF-alpha converting enzyme (TACE) from two-dimensional substrate mapping.

Lambert MH, Blackburn RK, Seaton TD, Kassel DB, Kinder DS, Leesnitzer MA, Bickett DM, Warner JR, Andersen MW, Badiang JG, Cowan DJ, Gaul MD, Petrov KG, Rabinowitz MH, Wiethe RW, Becherer JD, McDougald DL, Musso DL, Andrews RC, Moss ML.

Comb Chem High Throughput Screen. 2005 Jun;8(4):327-39.


Hantzsch synthesis of pyrazolo[1',2':1,2]pyrazolo[3,4-b]pyridines: partial agonists of the calcitonin receptor.

Boros EE, Cowan DJ, Cox RF, Mebrahtu MM, Rabinowitz MH, Thompson JB, Wolfe LA 3rd.

J Org Chem. 2005 Jun 24;70(13):5331-4.


Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Rabinowitz MH, Andrews RC, Becherer JD, Bickett DM, Bubacz DG, Conway JG, Cowan DJ, Gaul M, Glennon K, Lambert MH, Leesnitzer MA, McDougald DL, Moss ML, Musso DL, Rizzolio MC.

J Med Chem. 2001 Nov 22;44(24):4252-67.


N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.

Musso DL, Andersen MW, Andrews RC, Austin R, Beaudet EJ, Becherer JD, Bubacz DG, Bickett DM, Chan JH, Conway JG, Cowan DJ, Gaul MD, Glennon KC, Hedeen KM, Lambert MH, Leesnitzer MA, McDougald DL, Mitchell JL, Moss ML, Rabinowitz MH, Rizzolio MC, Schaller LT, Stanford JB, Tippin T, Warner JR, Whitesell LG, Wiethe RW.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2147-51.


Inhibition of tumor necrosis factor-alpha (TNF-alpha) production and arthritis in the rat by GW3333, a dual inhibitor of TNF-alpha-converting enzyme and matrix metalloproteinases.

Conway JG, Andrews RC, Beaudet B, Bickett DM, Boncek V, Brodie TA, Clark RL, Crumrine RC, Leenitzer MA, McDougald DL, Han B, Hedeen K, Lin P, Milla M, Moss M, Pink H, Rabinowitz MH, Tippin T, Scates PW, Selph J, Stimpson SA, Warner J, Becherer JD.

J Pharmacol Exp Ther. 2001 Sep;298(3):900-8.


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