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Items: 27

1.

Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form.

Nelp MT, Kates PA, Hunt JT, Newitt JA, Balog A, Maley D, Zhu X, Abell L, Allentoff A, Borzilleri R, Lewis HA, Lin Z, Seitz SP, Yan C, Groves JT.

Proc Natl Acad Sci U S A. 2018 Mar 27;115(13):3249-3254. doi: 10.1073/pnas.1719190115. Epub 2018 Mar 12.

2.

Crystal structures of apo and inhibitor-bound TGFβR2 kinase domain: insights into TGFβR isoform selectivity.

Tebben AJ, Ruzanov M, Gao M, Xie D, Kiefer SE, Yan C, Newitt JA, Zhang L, Kim K, Lu H, Kopcho LM, Sheriff S.

Acta Crystallogr D Struct Biol. 2016 May;72(Pt 5):658-74. doi: 10.1107/S2059798316003624. Epub 2016 Apr 26.

PMID:
27139629
3.

Crystal structure of microtubule affinity-regulating kinase 4 catalytic domain in complex with a pyrazolopyrimidine inhibitor.

Sack JS, Gao M, Kiefer SE, Myers JE Jr, Newitt JA, Wu S, Yan C.

Acta Crystallogr F Struct Biol Commun. 2016 Feb;72(Pt 2):129-34. doi: 10.1107/S2053230X15024747. Epub 2016 Jan 22.

4.

Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.

Huang A, Jayaraman L, Fura A, Vite GD, Trainor GL, Gottardis MM, Spires TE, Spires VM, Rizzo CA, Obermeier MT, Elzinga PA, Todderud G, Fan Y, Newitt JA, Beyer SM, Zhu Y, Warrack BM, Goodenough AK, Tebben AJ, Doweyko AM, Gold DL, Balog A.

ACS Med Chem Lett. 2015 Dec 2;7(1):40-5. doi: 10.1021/acsmedchemlett.5b00310. eCollection 2016 Jan 14.

5.

Development of a Model Protein Interaction Pair as a Benchmarking Tool for the Quantitative Analysis of 2-Site Protein-Protein Interactions.

Yamniuk AP, Newitt JA, Doyle ML, Arisaka F, Giannetti AM, Hensley P, Myszka DG, Schwarz FP, Thomson JA, Eisenstein E.

J Biomol Tech. 2015 Dec;26(4):125-41. doi: 10.7171/jbt.15-2604-001. Epub 2015 Oct 29.

6.

Development and Fit-for-Purpose Validation of a Soluble Human Programmed Death-1 Protein Assay.

Ni YG, Yuan X, Newitt JA, Peterson JE, Gleason CR, Haulenbeek J, Santockyte R, Lafont V, Marsilio F, Neely RJ, DeSilva B, Piccoli SP.

AAPS J. 2015 Jul;17(4):976-87. doi: 10.1208/s12248-015-9762-4. Epub 2015 May 1.

7.

Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.

Sivaprakasam P, Han X, Civiello RL, Jacutin-Porte S, Kish K, Pokross M, Lewis HA, Ahmed N, Szapiel N, Newitt JA, Baldwin ET, Xiao H, Krause CM, Park H, Nophsker M, Lippy JS, Burton CR, Langley DR, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63. doi: 10.1016/j.bmcl.2015.03.046. Epub 2015 Mar 24.

PMID:
25845281
8.

Discovery of novel P1 groups for coagulation factor VIIa inhibition using fragment-based screening.

Cheney DL, Bozarth JM, Metzler WJ, Morin PE, Mueller L, Newitt JA, Nirschl AH, Rendina AR, Tamura JK, Wei A, Wen X, Wurtz NR, Seiffert DA, Wexler RR, Priestley ES.

J Med Chem. 2015 Mar 26;58(6):2799-808. doi: 10.1021/jm501982k. Epub 2015 Mar 12.

PMID:
25764119
9.

The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.

Wrobleski ST, Lin S, Dhar TG, Dyckman AJ, Li T, Pitt S, Zhang R, Fan Y, Doweyko AM, Tokarski JS, Kish KF, Kiefer SE, Sack JS, Newitt JA, Witmer MR, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4120-6. doi: 10.1016/j.bmcl.2013.05.047. Epub 2013 May 23.

PMID:
23746475
10.

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.

Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly KM, Shuster DJ, Doweyko AM, Sack JS, Kish K, Kiefer SE, Newitt JA, Zhang H, Marathe PH, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4633-7. doi: 10.1016/j.bmcl.2011.05.091. Epub 2011 May 30.

PMID:
21705217
11.

5-amino-pyrazoles as potent and selective p38α inhibitors.

Das J, Moquin RV, Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Newitt JA, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6886-9. doi: 10.1016/j.bmcl.2010.10.034. Epub 2010 Oct 13.

PMID:
21035336
12.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

Liu C, Lin J, Wrobleski ST, Lin S, Hynes J, Wu H, Dyckman AJ, Li T, Wityak J, Gillooly KM, Pitt S, Shen DR, Zhang RF, McIntyre KW, Salter-Cid L, Shuster DJ, Zhang H, Marathe PH, Doweyko AM, Sack JS, Kiefer SE, Kish KF, Newitt JA, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

J Med Chem. 2010 Sep 23;53(18):6629-39. doi: 10.1021/jm100540x.

PMID:
20804198
13.

Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors.

Lin S, Wrobleski ST, Hynes J Jr, Pitt S, Zhang R, Fan Y, Doweyko AM, Kish KF, Sack JS, Malley MF, Kiefer SE, Newitt JA, McKinnon M, Trzaskos J, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5864-8. doi: 10.1016/j.bmcl.2010.07.102. Epub 2010 Jul 30.

PMID:
20732813
14.

Assessing compound binding to the Eg5 motor domain using a thermal shift assay.

McDonnell PA, Yanchunas J, Newitt JA, Tao L, Kiefer SE, Ortega M, Kut S, Burford N, Goldfarb V, Duke GJ, Shen H, Metzler W, Doyle M, Chen Z, Tarby C, Borzilleri R, Vaccaro W, Gottardis M, Lu S, Crews D, Kim K, Lombardo L, Roussell DL.

Anal Biochem. 2009 Sep 1;392(1):59-69. doi: 10.1016/j.ab.2009.05.044. Epub 2009 Jun 2.

PMID:
19497292
15.

Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects.

Constantine KL, Mueller L, Metzler WJ, McDonnell PA, Todderud G, Goldfarb V, Fan Y, Newitt JA, Kiefer SE, Gao M, Tortolani D, Vaccaro W, Tokarski J.

J Med Chem. 2008 Oct 9;51(19):6225-9. doi: 10.1021/jm800747w. Epub 2008 Sep 5.

PMID:
18771253
16.

Structural basis for the high-affinity binding of pyrrolotriazine inhibitors of p38 MAP kinase.

Sack JS, Kish KF, Pokross M, Xie D, Duke GJ, Tredup JA, Kiefer SE, Newitt JA.

Acta Crystallogr D Biol Crystallogr. 2008 Jul;D64(Pt 7):705-10. doi: 10.1107/S0907444908010032. Epub 2008 Jun 18.

PMID:
18566506
17.

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. doi: 10.1016/j.bmcl.2008.02.031. Epub 2008 Feb 16.

PMID:
18313298
18.

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

Hynes J Jr, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K, Zhang H, Marathe PH, Doweyko AM, Tokarski JS, Sack JS, Pokross M, Kiefer SE, Newitt JA, Barrish JC, Dodd J, Schieven GL, Leftheris K.

J Med Chem. 2008 Jan 10;51(1):4-16. Epub 2007 Dec 12.

PMID:
18072718
19.

The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants.

Tokarski JS, Newitt JA, Chang CY, Cheng JD, Wittekind M, Kiefer SE, Kish K, Lee FY, Borzillerri R, Lombardo LJ, Xie D, Zhang Y, Klei HE.

Cancer Res. 2006 Jun 1;66(11):5790-7.

20.

Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.

Kim KS, Lu S, Cornelius LA, Lombardo LJ, Borzilleri RM, Schroeder GM, Sheng C, Rovnyak G, Crews D, Schmidt RJ, Williams DK, Bhide RS, Traeger SC, McDonnell PA, Mueller L, Sheriff S, Newitt JA, Pudzianowski AT, Yang Z, Wild R, Lee FY, Batorsky R, Ryder JS, Ortega-Nanos M, Shen H, Gottardis M, Roussell DL.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3937-42. Epub 2006 May 30.

PMID:
16730979
21.

Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.

Tarby CM, Kaltenbach RF 3rd, Huynh T, Pudzianowski A, Shen H, Ortega-Nanos M, Sheriff S, Newitt JA, McDonnell PA, Burford N, Fairchild CR, Vaccaro W, Chen Z, Borzilleri RM, Naglich J, Lombardo LJ, Gottardis M, Trainor GL, Roussell DL.

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2095-100. Epub 2006 Feb 3.

PMID:
16458511
24.
25.

A highly conserved nucleotide in the Alu domain of SRP RNA mediates translation arrest through high affinity binding to SRP9/14.

Chang DY, Newitt JA, Hsu K, Bernstein HD, Maraia RJ.

Nucleic Acids Res. 1997 Mar 15;25(6):1117-22.

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