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Items: 1 to 20 of 26


Dual-specificity phosphatase 3 deficiency or inhibition limits platelet activation and arterial thrombosis.

Musumeci L, Kuijpers MJ, Gilio K, Hego A, Théâtre E, Maurissen L, Vandereyken M, Diogo CV, Lecut C, Guilmain W, Bobkova EV, Eble JA, Dahl R, Drion P, Rascon J, Mostofi Y, Yuan H, Sergienko E, Chung TD, Thiry M, Senis Y, Moutschen M, Mustelin T, Lancellotti P, Heemskerk JW, Tautz L, Oury C, Rahmouni S.

Circulation. 2015 Feb 17;131(7):656-68. doi: 10.1161/CIRCULATIONAHA.114.010186.


Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.

Bravo Y, Teriete P, Dhanya RP, Dahl R, Lee PS, Kiffer-Moreira T, Ganji SR, Sergienko E, Smith LH, Farquharson C, Millán JL, Cosford ND.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4308-11. doi: 10.1016/j.bmcl.2014.07.013.


Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.

Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND.

J Med Chem. 2014 May 22;57(10):4154-72. doi: 10.1021/jm5000563.


Design, synthesis and bioevaluation of an EphA2 receptor-based targeted delivery system.

Barile E, Wang S, Das SK, Noberini R, Dahl R, Stebbins JL, Pasquale EB, Fisher PB, Pellecchia M.

ChemMedChem. 2014 Jul;9(7):1403-12. doi: 10.1002/cmdc.201400067.


Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes.

Ardecky RJ, Bobkova EV, Kiffer-Moreira T, Brown B, Ganji S, Zou J, Pass I, Narisawa S, Iano FG, Rosenstein C, Cheltsov A, Rascon J, Hedrick M, Gasior C, Forster A, Shi S, Dahl R, Vasile S, Su Y, Sergienko E, Chung TD, Kaunitz J, Hoylaerts MF, Pinkerton AB, Millán JL.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):1000-4. doi: 10.1016/j.bmcl.2013.12.043.


Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.

Sidique S, Dhanya RP, Sheffler DJ, Nickols HH, Yang L, Dahl R, Mangravita-Novo A, Smith LH, D'Souza MS, Semenova S, Conn PJ, Markou A, Cosford ND.

J Med Chem. 2012 Nov 26;55(22):9434-45. doi: 10.1021/jm3005306.


Pharmacological inhibition of PHOSPHO1 suppresses vascular smooth muscle cell calcification.

Kiffer-Moreira T, Yadav MC, Zhu D, Narisawa S, Sheen C, Stec B, Cosford ND, Dahl R, Farquharson C, Hoylaerts MF, Macrae VE, Millán JL.

J Bone Miner Res. 2013 Jan;28(1):81-91. doi: 10.1002/jbmr.1733.


A gatekeeper residue for NEDD8-activating enzyme inhibition by MLN4924.

Toth JI, Yang L, Dahl R, Petroski MD.

Cell Rep. 2012 Apr 19;1(4):309-16. doi: 10.1016/j.celrep.2012.02.006.


Endoplasmic reticulum protein BI-1 regulates Ca²⁺-mediated bioenergetics to promote autophagy.

Sano R, Hou YC, Hedvat M, Correa RG, Shu CW, Krajewska M, Diaz PW, Tamble CM, Quarato G, Gottlieb RA, Yamaguchi M, Nizet V, Dahl R, Thomas DD, Tait SW, Green DR, Fisher PB, Matsuzawa S, Reed JC.

Genes Dev. 2012 May 15;26(10):1041-54. doi: 10.1101/gad.184325.111.


LYP inhibits T-cell activation when dissociated from CSK.

Vang T, Liu WH, Delacroix L, Wu S, Vasile S, Dahl R, Yang L, Musumeci L, Francis D, Landskron J, Tasken K, Tremblay ML, Lie BA, Page R, Mustelin T, Rahmouni S, Rickert RC, Tautz L.

Nat Chem Biol. 2012 Mar 18;8(5):437-46. doi: 10.1038/nchembio.916.


Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth.

Remacle AG, Golubkov VS, Shiryaev SA, Dahl R, Stebbins JL, Chernov AV, Cheltsov AV, Pellecchia M, Strongin AY.

Cancer Res. 2012 May 1;72(9):2339-49. doi: 10.1158/0008-5472.CAN-11-4149.


Novel targeted system to deliver chemotherapeutic drugs to EphA2-expressing cancer cells.

Wang S, Placzek WJ, Stebbins JL, Mitra S, Noberini R, Koolpe M, Zhang Z, Dahl R, Pasquale EB, Pellecchia M.

J Med Chem. 2012 Mar 8;55(5):2427-36. doi: 10.1021/jm201743s.


High-throughput fluorescence polarization assay for chemical library screening against anti-apoptotic Bcl-2 family member Bfl-1.

Zhai D, Godoi P, Sergienko E, Dahl R, Chan X, Brown B, Rascon J, Hurder A, Su Y, Chung TD, Jin C, Diaz P, Reed JC.

J Biomol Screen. 2012 Mar;17(3):350-60. doi: 10.1177/1087057111429372.


Inhibition of hematopoietic protein tyrosine phosphatase augments and prolongs ERK1/2 and p38 activation.

Sergienko E, Xu J, Liu WH, Dahl R, Critton DA, Su Y, Brown BT, Chan X, Yang L, Bobkova EV, Vasile S, Yuan H, Rascon J, Colayco S, Sidique S, Cosford ND, Chung TD, Mustelin T, Page R, Lombroso PJ, Tautz L.

ACS Chem Biol. 2012 Feb 17;7(2):367-77. doi: 10.1021/cb2004274.


Phosphomannose isomerase inhibitors improve N-glycosylation in selected phosphomannomutase-deficient fibroblasts.

Sharma V, Ichikawa M, He P, Scott DA, Bravo Y, Dahl R, Ng BG, Cosford ND, Freeze HH.

J Biol Chem. 2011 Nov 11;286(45):39431-8. doi: 10.1074/jbc.M111.285502. Erratum in: J Biol Chem. 2011 Dec 16;286(50):43588. Scott, David A [added].


Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.

Dahl R, Bravo Y, Sharma V, Ichikawa M, Dhanya RP, Hedrick M, Brown B, Rascon J, Vicchiarelli M, Mangravita-Novo A, Yang L, Stonich D, Su Y, Smith LH, Sergienko E, Freeze HH, Cosford ND.

J Med Chem. 2011 May 26;54(10):3661-8. doi: 10.1021/jm101401a.


Inhibition of the Hematopoietic Protein Tyrosine Phosphatase by Phenoxyacetic Acids.

Bobkova EV, Liu WH, Colayco S, Rascon J, Vasile S, Gasior C, Critton DA, Chan X, Dahl R, Su Y, Sergienko E, Chung TD, Mustelin T, Page R, Tautz L.

ACS Med Chem Lett. 2011 Feb;2(2):113-118.


Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.

De SK, Barile E, Chen V, Stebbins JL, Cellitti JF, Machleidt T, Carlson CB, Yang L, Dahl R, Pellecchia M.

Bioorg Med Chem. 2011 Apr 15;19(8):2582-8. doi: 10.1016/j.bmc.2011.03.017.


An optically pure apogossypolone derivative as potent pan-active inhibitor of anti-apoptotic bcl-2 family proteins.

Wei J, Stebbins JL, Kitada S, Dash R, Zhai D, Placzek WJ, Wu B, Rega MF, Zhang Z, Barile E, Yang L, Dahl R, Fisher PB, Reed JC, Pellecchia M.

Front Oncol. 2011 Sep 30;1:28. doi: 10.3389/fonc.2011.00028.


Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.

Dhanya RP, Sidique S, Sheffler DJ, Nickols HH, Herath A, Yang L, Dahl R, Ardecky R, Semenova S, Markou A, Conn PJ, Cosford ND.

J Med Chem. 2011 Jan 13;54(1):342-53. doi: 10.1021/jm1012165.

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