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Items: 25

1.

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.

Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P.

J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7.

PMID:
30137981
2.

Discovery and Characterization of Allosteric WNK Kinase Inhibitors.

Yamada K, Zhang JH, Xie X, Reinhardt J, Xie AQ, LaSala D, Kohls D, Yowe D, Burdick D, Yoshisue H, Wakai H, Schmidt I, Gunawan J, Yasoshima K, Yue QK, Kato M, Mogi M, Idamakanti N, Kreder N, Drueckes P, Pandey P, Kawanami T, Huang W, Yagi YI, Deng Z, Park HM.

ACS Chem Biol. 2016 Dec 16;11(12):3338-3346. Epub 2016 Oct 19.

PMID:
27712055
3.

Protein Kinase Selectivity Profiling Using Microfluid Mobility Shift Assays.

Drueckes P.

Methods Mol Biol. 2016;1439:143-57. doi: 10.1007/978-1-4939-3673-1_9.

PMID:
27316993
4.

Type II Inhibitors Targeting CDK2.

Alexander LT, Möbitz H, Drueckes P, Savitsky P, Fedorov O, Elkins JM, Deane CM, Cowan-Jacob SW, Knapp S.

ACS Chem Biol. 2015 Sep 18;10(9):2116-25. doi: 10.1021/acschembio.5b00398. Epub 2015 Jul 20.

PMID:
26158339
5.

Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers.

Garcia PD, Langowski JL, Wang Y, Chen M, Castillo J, Fanton C, Ison M, Zavorotinskaya T, Dai Y, Lu J, Niu XH, Basham S, Chan J, Yu J, Doyle M, Feucht P, Warne R, Narberes J, Tsang T, Fritsch C, Kauffmann A, Pfister E, Drueckes P, Trappe J, Wilson C, Han W, Lan J, Nishiguchi G, Lindvall M, Bellamacina C, Aycinena JA, Zang R, Holash J, Burger MT.

Clin Cancer Res. 2014 Apr 1;20(7):1834-45. doi: 10.1158/1078-0432.CCR-13-2062. Epub 2014 Jan 28.

6.

The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study.

Chapelat J, Berst F, Marzinzik AL, Moebitz H, Drueckes P, Trappe J, Fabbro D, Seebach D.

Eur J Med Chem. 2012 Nov;57:1-9. doi: 10.1016/j.ejmech.2012.08.038. Epub 2012 Sep 4.

PMID:
23041456
7.

Substrate profiling of IGF-1R and InsR: identification of a potent pentamer substrate.

Chapelat J, Berst F, Marzinzik AL, Moebitz H, Drueckes P, Fabbro D, Trappe J, Seebach D.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7030-3. doi: 10.1016/j.bmcl.2011.09.101. Epub 2011 Sep 29.

PMID:
22004721
8.

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H, Wartmann M, Berghausen J, Drueckes P, Zimmerlin A, Bussiere D, Murray J, Graus Porta D.

J Med Chem. 2011 Oct 27;54(20):7066-83. doi: 10.1021/jm2006222. Epub 2011 Sep 21.

PMID:
21936542
9.

A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.

Tiedt R, Degenkolbe E, Furet P, Appleton BA, Wagner S, Schoepfer J, Buck E, Ruddy DA, Monahan JE, Jones MD, Blank J, Haasen D, Drueckes P, Wartmann M, McCarthy C, Sellers WR, Hofmann F.

Cancer Res. 2011 Aug 1;71(15):5255-64. doi: 10.1158/0008-5472.CAN-10-4433. Epub 2011 Jun 22.

10.

Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277.

Liniger M, Neuhaus C, Hofmann T, Fransioli-Ignazio L, Jordi M, Drueckes P, Trappe J, Fabbro D, Altmann KH.

ACS Med Chem Lett. 2010 Oct 20;2(1):22-7. doi: 10.1021/ml1001807. eCollection 2011 Jan 13.

11.

A fluorescence lifetime-based assay for abelson kinase.

Pritz S, Meder G, Doering K, Drueckes P, Woelcke J, Mayr LM, Hassiepen U.

J Biomol Screen. 2011 Jan;16(1):65-72. doi: 10.1177/1087057110385817. Epub 2010 Dec 8.

PMID:
21148014
12.

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.

Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T.

Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29.

13.

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Pissot-Soldermann C, Gerspacher M, Furet P, Gaul C, Holzer P, McCarthy C, Radimerski T, Regnier CH, Baffert F, Drueckes P, Tavares GA, Vangrevelinghe E, Blasco F, Ottaviani G, Ossola F, Scesa J, Reetz J.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2609-13. doi: 10.1016/j.bmcl.2010.02.056. Epub 2010 Feb 19.

PMID:
20231096
14.

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Gerspacher M, Furet P, Pissot-Soldermann C, Gaul C, Holzer P, Vangrevelinghe E, Lang M, Erdmann D, Radimerski T, Regnier CH, Chene P, De Pover A, Hofmann F, Baffert F, Buhl T, Aichholz R, Blasco F, Endres R, Trappe J, Drueckes P.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21.

PMID:
20138510
15.

Extended kinase profile and properties of the protein kinase inhibitor nilotinib.

Manley PW, Drueckes P, Fendrich G, Furet P, Liebetanz J, Martiny-Baron G, Mestan J, Trappe J, Wartmann M, Fabbro D.

Biochim Biophys Acta. 2010 Mar;1804(3):445-53. doi: 10.1016/j.bbapap.2009.11.008. Epub 2009 Nov 14.

PMID:
19922818
16.

Affinity classification of kinase inhibitors by mass spectrometric methods and validation using standard IC(50) measurements.

Jecklin MC, Touboul D, Jain R, Toole EN, Tallarico J, Drueckes P, Ramage P, Zenobi R.

Anal Chem. 2009 Jan 1;81(1):408-19. doi: 10.1021/ac801782c.

PMID:
19067573
17.

Characterization of compound 584, an Abl kinase inhibitor with lasting effects.

Puttini M, Redaelli S, Moretti L, Brussolo S, Gunby RH, Mologni L, Marchesi E, Cleris L, Donella-Deana A, Drueckes P, Sala E, Lucchini V, Kubbutat M, Formelli F, Zambon A, Scapozza L, Gambacorti-Passerini C.

Haematologica. 2008 May;93(5):653-61. doi: 10.3324/haematol.12212. Epub 2008 Mar 26.

18.

Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases.

Bettayeb K, Tirado OM, Marionneau-Lambot S, Ferandin Y, Lozach O, Morris JC, Mateo-Lozano S, Drueckes P, Schächtele C, Kubbutat MH, Liger F, Marquet B, Joseph B, Echalier A, Endicott JA, Notario V, Meijer L.

Cancer Res. 2007 Sep 1;67(17):8325-34.

19.

A cGMP-dependent protein kinase assay for high throughput screening based on time-resolved fluorescence resonance energy transfer.

Bader B, Butt E, Palmetshofer A, Walter U, Jarchau T, Drueckes P.

J Biomol Screen. 2001 Aug;6(4):255-64.

PMID:
11689125
20.

Expression of the casein kinase 2 subunits in Chinese hamster ovary and 3T3 L1 cells provides information on the role of the enzyme in cell proliferation and the cell cycle.

Li D, Dobrowolska G, Aicher LD, Chen M, Wright JH, Drueckes P, Dunphy EL, Munar ES, Krebs EG.

J Biol Chem. 1999 Nov 12;274(46):32988-96.

21.

A role for the SHP-2 tyrosine phosphatase in nerve growth-induced PC12 cell differentiation.

Wright JH, Drueckes P, Bartoe J, Zhao Z, Shen SH, Krebs EG.

Mol Biol Cell. 1997 Aug;8(8):1575-85.

22.

Activation of E350A mutant maltodextrin phosphorylase by exogenously added acetate.

Drueckes P, Schinzel R.

Protein Eng. 1996 Aug;9(8):701-5.

PMID:
8875647
23.

Mutational analysis of the oligosaccharide recognition site at the active site of Escherichia coli maltodextrin phosphorylase.

Drueckes P, Boeck B, Palm D, Schinzel R.

Biochemistry. 1996 May 28;35(21):6727-34.

PMID:
8639623
24.

Photometric microtiter assay of inorganic phosphate in the presence of acid-labile organic phosphates.

Drueckes P, Schinzel R, Palm D.

Anal Biochem. 1995 Sep 1;230(1):173-7.

PMID:
8585615
25.

The phosphate recognition site of Escherichia coli maltodextrin phosphorylase.

Schinzel R, Drueckes P.

FEBS Lett. 1991 Jul 29;286(1-2):125-8.

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