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Items: 22

1.

Co-inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity.

Basler M, Lindstrom MM, LaStant JJ, Bradshaw JM, Owens TD, Schmidt C, Maurits E, Tsu C, Overkleeft HS, Kirk CJ, Langrish CL, Groettrup M.

EMBO Rep. 2018 Oct 2. pii: e46512. doi: 10.15252/embr.201846512. [Epub ahead of print]

PMID:
30279279
2.

The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance.

Venetsanakos E, Brameld KA, Phan VT, Verner E, Owens TD, Xing Y, Tam D, LaStant J, Leung K, Karr DE, Hill RJ, Gerritsen ME, Goldstein DM, Funk JO, Bradshaw JM.

Mol Cancer Ther. 2017 Dec;16(12):2668-2676. doi: 10.1158/1535-7163.MCT-17-0309. Epub 2017 Oct 4.

PMID:
28978721
3.

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.

Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J, Loughhead DG, Ton T, Karr DE, Gerritsen ME, Goldstein DM, Funk JO.

J Med Chem. 2017 Aug 10;60(15):6516-6527. doi: 10.1021/acs.jmedchem.7b00360. Epub 2017 Jul 25.

PMID:
28665128
4.

Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK).

Lou Y, Lopez F, Jiang Y, Han X, Brotherton C, Billedeau R, Gabriel S, Gleason S, Goldstein DM, Hilgenkamp R, Kocer B, Orzechowski L, Tan J, Wovkulich P, Wen B, Fry D, Di Lello P, Chen L, Zhang FJ, Fretland J, Nangia A, Yang T, Owens TD.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):632-635. doi: 10.1016/j.bmcl.2016.11.092. Epub 2016 Dec 2.

PMID:
28025004
5.

A Small Molecule Inhibitor of ITK and RLK Impairs Th1 Differentiation and Prevents Colitis Disease Progression.

Cho HS, Shin HM, Haberstock-Debic H, Xing Y, Owens TD, Funk JO, Hill RJ, Bradshaw JM, Berg LJ.

J Immunol. 2015 Nov 15;195(10):4822-31. doi: 10.4049/jimmunol.1501828. Epub 2015 Oct 14.

6.

Prolonged and tunable residence time using reversible covalent kinase inhibitors.

Bradshaw JM, McFarland JM, Paavilainen VO, Bisconte A, Tam D, Phan VT, Romanov S, Finkle D, Shu J, Patel V, Ton T, Li X, Loughhead DG, Nunn PA, Karr DE, Gerritsen ME, Funk JO, Owens TD, Verner E, Brameld KA, Hill RJ, Goldstein DM, Taunton J.

Nat Chem Biol. 2015 Jul;11(7):525-31. doi: 10.1038/nchembio.1817. Epub 2015 May 25.

7.

Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.

Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A, Owens TD, Verner E, Brameld KA, Funk JO, Hill RJ, Johnson AJ, Dubovsky JA.

J Biol Chem. 2015 Mar 6;290(10):5960-78. doi: 10.1074/jbc.M114.614891. Epub 2015 Jan 15.

8.

Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.

Lou Y, Sweeney ZK, Kuglstatter A, Davis D, Goldstein DM, Han X, Hong J, Kocer B, Kondru RK, Litman R, McIntosh J, Sarma K, Suh J, Taygerly J, Owens TD.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):367-71. doi: 10.1016/j.bmcl.2014.11.030. Epub 2014 Nov 20.

PMID:
25466710
9.

Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.

Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD.

J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p. Epub 2014 Apr 16.

PMID:
24712864
10.

Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.

Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE Jr, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villaseñor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC.

J Med Chem. 2013 Feb 28;56(4):1677-92. doi: 10.1021/jm301720p. Epub 2013 Feb 12.

PMID:
23350847
11.

Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.

Lou Y, Owens TD, Kuglstatter A, Kondru RK, Goldstein DM.

J Med Chem. 2012 May 24;55(10):4539-50. doi: 10.1021/jm300035p. Epub 2012 Mar 21. Review. No abstract available.

PMID:
22394077
12.

RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents.

Xu D, Kim Y, Postelnek J, Vu MD, Hu DQ, Liao C, Bradshaw M, Hsu J, Zhang J, Pashine A, Srinivasan D, Woods J, Levin A, O'Mahony A, Owens TD, Lou Y, Hill RJ, Narula S, DeMartino J, Fine JS.

J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. doi: 10.1124/jpet.111.187740. Epub 2012 Jan 6.

13.
14.

N-tert-butanesulfinyl imines: versatile intermediates for the asymmetric synthesis of amines.

Ellman JA, Owens TD, Tang TP.

Acc Chem Res. 2002 Nov;35(11):984-95.

PMID:
12437323
16.

Synthesis and crystal structure of a unique and homochiral N,S-bonded N,N'-bis(tert-butanesulfinyl)amidinate rhodium(I) complex.

Souers AJ, Owens TD, Oliver AG, Hollander FJ, Ellman JA.

Inorg Chem. 2001 Sep 24;40(20):5299-301. No abstract available.

PMID:
11559098
17.

Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.

Semple JE, Levy OE, Minami NK, Owens TD, Siev DV.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2305-9.

PMID:
11055344
18.

New synthetic technology for efficient construction of alpha-hydroxy-beta-amino amides via the Passerini reaction.

Semple JE, Owens TD, Nguyen K, Levy OE.

Org Lett. 2000 Sep 7;2(18):2769-72.

PMID:
10964361
20.

Potent and selective thrombin inhibitors featuring hydrophobic, basic P3-P4-aminoalkyllactam moieties.

Semple JE, Rowley DC, Owens TD, Minami NK, Uong TH, Brunck TK.

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3525-30.

PMID:
9934465
21.

Conservation of the Escherichia coli dnaX programmed ribosomal frameshift signal in Salmonella typhimurium.

Blinkova A, Burkart MF, Owens TD, Walker JR.

J Bacteriol. 1997 Jul;179(13):4438-42.

22.

Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.

Semple JE, Rowley DC, Brunck TK, Ha-Uong T, Minami NK, Owens TD, Tamura SY, Goldman EA, Siev DV, Ardecky RJ, Carpenter SH, Ge Y, Richard BM, Nolan TG, Håkanson K, Tulinsky A, Nutt RF, Ripka WC.

J Med Chem. 1996 Nov 8;39(23):4531-6. No abstract available.

PMID:
8917639

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