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Items: 17

1.

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.

Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L.

J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15.

PMID:
31368705
2.

A precision therapy against cancers driven by KIT/PDGFRA mutations.

Evans EK, Gardino AK, Kim JL, Hodous BL, Shutes A, Davis A, Zhu XJ, Schmidt-Kittler O, Wilson D, Wilson K, DiPietro L, Zhang Y, Brooijmans N, LaBranche TP, Wozniak A, Gebreyohannes YK, Schöffski P, Heinrich MC, DeAngelo DJ, Miller S, Wolf B, Kohl N, Guzi T, Lydon N, Boral A, Lengauer C.

Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690. doi: 10.1126/scitranslmed.aao1690.

PMID:
29093181
3.

First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.

Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N, Shutes A, Winter C, Lengauer C, Kohl NE, Guzi T.

Cancer Discov. 2015 Apr;5(4):424-37. doi: 10.1158/2159-8290.CD-14-1029. Epub 2015 Mar 16.

4.

SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.

Karra S, Xiao Y, Chen X, Liu-Bujalski L, Huck B, Sutton A, Goutopoulos A, Askew B, Josephson K, Jiang X, Shutes A, Shankar V, Noonan T, Garcia-Berrios G, Dong R, Dhanabal M, Tian H, Wang Z, Clark A, Goodstal S.

Bioorg Med Chem Lett. 2013 May 15;23(10):3081-7. doi: 10.1016/j.bmcl.2013.03.008. Epub 2013 Mar 13.

PMID:
23570792
5.

Allosteric IGF-1R Inhibitors.

Heinrich T, Grädler U, Böttcher H, Blaukat A, Shutes A.

ACS Med Chem Lett. 2010 May 18;1(5):199-203. doi: 10.1021/ml100044h. eCollection 2010 Aug 12.

6.

Capillary microfluidic electrophoretic mobility shift assays: application to enzymatic assays in drug discovery.

Perrin D, Frémaux C, Shutes A.

Expert Opin Drug Discov. 2010 Jan;5(1):51-63. doi: 10.1517/17460440903493431.

PMID:
22823971
7.

Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.

Onesto C, Shutes A, Picard V, Schweighoffer F, Der CJ.

Methods Enzymol. 2008;439:111-29. doi: 10.1016/S0076-6879(07)00409-0.

PMID:
18374160
8.

DLC-1 suppresses non-small cell lung cancer growth and invasion by RhoGAP-dependent and independent mechanisms.

Healy KD, Hodgson L, Kim TY, Shutes A, Maddileti S, Juliano RL, Hahn KM, Harden TK, Bang YJ, Der CJ.

Mol Carcinog. 2008 May;47(5):326-37.

9.

Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.

Shutes A, Onesto C, Picard V, Leblond B, Schweighoffer F, Der CJ.

J Biol Chem. 2007 Dec 7;282(49):35666-78. Epub 2007 Oct 11.

10.

Real-time in vitro measurement of intrinsic and Ras GAP-mediated GTP hydrolysis.

Shutes A, Der CJ.

Methods Enzymol. 2006;407:9-22.

PMID:
16757310
11.

Biochemical analyses of the Wrch atypical Rho family GTPases.

Shutes A, Berzat AC, Chenette EJ, Cox AD, Der CJ.

Methods Enzymol. 2006;406:11-26. Review.

PMID:
16472646
12.

Real-time in vitro measurement of GTP hydrolysis.

Shutes A, Der CJ.

Methods. 2005 Oct;37(2):183-89.

PMID:
16288887
13.

Transforming activity of the Rho family GTPase, Wrch-1, a Wnt-regulated Cdc42 homolog, is dependent on a novel carboxyl-terminal palmitoylation motif.

Berzat AC, Buss JE, Chenette EJ, Weinbaum CA, Shutes A, Der CJ, Minden A, Cox AD.

J Biol Chem. 2005 Sep 23;280(38):33055-65. Epub 2005 Jul 26.

14.

Atypical mechanism of regulation of the Wrch-1 Rho family small GTPase.

Shutes A, Berzat AC, Cox AD, Der CJ.

Curr Biol. 2004 Nov 23;14(22):2052-6.

15.

Established and emerging fluorescence-based assays for G-protein function: heterotrimeric G-protein alpha subunits and regulator of G-protein signaling (RGS) proteins.

Kimple RJ, Jones MB, Shutes A, Yerxa BR, Siderovski DP, Willard FS.

Comb Chem High Throughput Screen. 2003 Jun;6(4):399-407.

PMID:
12769684
16.
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