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Pharmacological inhibitor of DNA-PK, M3814, potentiates radiotherapy and regresses human tumors in mouse models.

Zenke FT, Zimmermann A, Sirrenberg C, Dahmen H, Kirkin V, Pehl U, Grombacher T, Wilm C, Fuchss T, Amendt C, Vassilev LT, Blaukat A.

Mol Cancer Ther. 2020 Mar 27. pii: molcanther.0734.2019. doi: 10.1158/1535-7163.MCT-19-0734. [Epub ahead of print]


DNA-PK Inhibitor, M3814, as a New Combination Partner of Mylotarg in the Treatment of Acute Myeloid Leukemia.

Carr MI, Zimmermann A, Chiu LY, Zenke FT, Blaukat A, Vassilev LT.

Front Oncol. 2020 Feb 13;10:127. doi: 10.3389/fonc.2020.00127. eCollection 2020.


Prediction of active human dose: learnings from 20 years of Merck KGaA experience, illustrated by case studies.

Peters SA, Petersson C, Blaukat A, Halle JP, Dolgos H.

Drug Discov Today. 2020 Jan 22. pii: S1359-6446(20)30028-3. doi: 10.1016/j.drudis.2020.01.002. [Epub ahead of print] Review.


Therapeutic Implications of p53 Status on Cancer Cell Fate Following Exposure to Ionizing Radiation and the DNA-PK Inhibitor M3814.

Sun Q, Guo Y, Liu X, Czauderna F, Carr MI, Zenke FT, Blaukat A, Vassilev LT.

Mol Cancer Res. 2019 Dec;17(12):2457-2468. doi: 10.1158/1541-7786.MCR-19-0362. Epub 2019 Sep 24.


Identification of a MET-eIF4G1 translational regulation axis that controls HIF-1α levels under hypoxia.

Glück AA, Orlando E, Leiser D, Poliaková M, Nisa L, Quintin A, Gavini J, Stroka DM, Berezowska S, Bubendorf L, Blaukat A, Aebersold DM, Medová M, Zimmer Y.

Oncogene. 2018 Jul;37(30):4181-4196. doi: 10.1038/s41388-018-0256-6. Epub 2018 May 2.


Overcoming hypoxia-induced tumor radioresistance in non-small cell lung cancer by targeting DNA-dependent protein kinase in combination with carbon ion irradiation.

Klein C, Dokic I, Mairani A, Mein S, Brons S, Häring P, Haberer T, Jäkel O, Zimmermann A, Zenke F, Blaukat A, Debus J, Abdollahi A.

Radiat Oncol. 2017 Dec 29;12(1):208. doi: 10.1186/s13014-017-0939-0.


The selective c-Met inhibitor tepotinib can overcome epidermal growth factor receptor inhibitor resistance mediated by aberrant c-Met activation in NSCLC models.

Friese-Hamim M, Bladt F, Locatelli G, Stammberger U, Blaukat A.

Am J Cancer Res. 2017 Apr 1;7(4):962-972. eCollection 2017.


Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases.

Clarke PA, Ortiz-Ruiz MJ, TePoele R, Adeniji-Popoola O, Box G, Court W, Czasch S, El Bawab S, Esdar C, Ewan K, Gowan S, De Haven Brandon A, Hewitt P, Hobbs SM, Kaufmann W, Mallinger A, Raynaud F, Roe T, Rohdich F, Schiemann K, Simon S, Schneider R, Valenti M, Weigt S, Blagg J, Blaukat A, Dale TC, Eccles SA, Hecht S, Urbahns K, Workman P, Wienke D.

Elife. 2016 Dec 9;5. pii: e20722. doi: 10.7554/eLife.20722.


Depletion of FOXM1 via MET Targeting Underlies Establishment of a DNA Damage-Induced Senescence Program in Gastric Cancer.

Francica P, Nisa L, Aebersold DM, Langer R, Bladt F, Blaukat A, Stroka D, Martínez MR, Zimmer Y, Medová M.

Clin Cancer Res. 2016 Nov 1;22(21):5322-5336. Epub 2016 May 16.


A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D, Schwarz D, Schneider K, Stubbs M, Ewan K, Fraser E, TePoele R, Court W, Box G, Valenti M, de Haven Brandon A, Gowan S, Rohdich F, Raynaud F, Schneider R, Poeschke O, Blaukat A, Workman P, Schiemann K, Eccles SA, Wienke D, Blagg J.

Nat Chem Biol. 2015 Dec;11(12):973-980. doi: 10.1038/nchembio.1952. Epub 2015 Oct 26.


Impact of p53 Status on Radiosensitization of Tumor Cells by MET Inhibition-Associated Checkpoint Abrogation.

Mikami K, Medová M, Nisa L, Francica P, Glück AA, Tschan MP, Blaukat A, Bladt F, Aebersold DM, Zimmer Y.

Mol Cancer Res. 2015 Dec;13(12):1544-53. doi: 10.1158/1541-7786.MCR-15-0022. Epub 2015 Sep 10.


KRAS and HRAS mutations confer resistance to MET targeting in preclinical models of MET-expressing tumor cells.

Leiser D, Medová M, Mikami K, Nisa L, Stroka D, Blaukat A, Bladt F, Aebersold DM, Zimmer Y.

Mol Oncol. 2015 Aug;9(7):1434-46. doi: 10.1016/j.molonc.2015.04.001. Epub 2015 Apr 14.


Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.

Dorsch D, Schadt O, Stieber F, Meyring M, Grädler U, Bladt F, Friese-Hamim M, Knühl C, Pehl U, Blaukat A.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1597-602. doi: 10.1016/j.bmcl.2015.02.002. Epub 2015 Feb 16.


The c-Met Inhibitor MSC2156119J Effectively Inhibits Tumor Growth in Liver Cancer Models.

Bladt F, Friese-Hamim M, Ihling C, Wilm C, Blaukat A.

Cancers (Basel). 2014 Aug 19;6(3):1736-52. doi: 10.3390/cancers6031736.


The novel ATP-competitive inhibitor of the MET hepatocyte growth factor receptor EMD1214063 displays inhibitory activity against selected MET-mutated variants.

Medová M, Pochon B, Streit B, Blank-Liss W, Francica P, Stroka D, Keogh A, Aebersold DM, Blaukat A, Bladt F, Zimmer Y.

Mol Cancer Ther. 2013 Nov;12(11):2415-24. doi: 10.1158/1535-7163.MCT-13-0151. Epub 2013 Sep 23.


EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors.

Bladt F, Faden B, Friese-Hamim M, Knuehl C, Wilm C, Fittschen C, Grädler U, Meyring M, Dorsch D, Jaehrling F, Pehl U, Stieber F, Schadt O, Blaukat A.

Clin Cancer Res. 2013 Jun 1;19(11):2941-51. doi: 10.1158/1078-0432.CCR-12-3247. Epub 2013 Apr 3.


Protective autophagy is involved in resistance towards MET inhibitors in human gastric adenocarcinoma cells.

Humbert M, Medová M, Aebersold DM, Blaukat A, Bladt F, Fey MF, Zimmer Y, Tschan MP.

Biochem Biophys Res Commun. 2013 Feb 8;431(2):264-9. doi: 10.1016/j.bbrc.2012.12.120. Epub 2013 Jan 9.


Nephrocystin-4 regulates Pyk2-induced tyrosine phosphorylation of nephrocystin-1 to control targeting to monocilia.

Liebau MC, Höpker K, Müller RU, Schmedding I, Zank S, Schairer B, Fabretti F, Höhne M, Bartram MP, Dafinger C, Hackl M, Burst V, Habbig S, Zentgraf H, Blaukat A, Walz G, Benzing T, Schermer B.

J Biol Chem. 2011 Apr 22;286(16):14237-45. doi: 10.1074/jbc.M110.165464. Epub 2011 Feb 28.


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.


Peptide mimotopes recognized by antibodies cetuximab and matuzumab induce a functionally equivalent anti-EGFR immune response.

Hartmann C, Müller N, Blaukat A, Koch J, Benhar I, Wels WS.

Oncogene. 2010 Aug 12;29(32):4517-27. doi: 10.1038/onc.2010.195. Epub 2010 May 31.


The C-terminal tail of CRTH2 is a key molecular determinant that constrains Galphai and downstream signaling cascade activation.

Schröder R, Merten N, Mathiesen JM, Martini L, Kruljac-Letunic A, Krop F, Blaukat A, Fang Y, Tran E, Ulven T, Drewke C, Whistler J, Pardo L, Gomeza J, Kostenis E.

J Biol Chem. 2009 Jan 9;284(2):1324-36. doi: 10.1074/jbc.M806867200. Epub 2008 Nov 14.


Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization.

Schmiedel J, Blaukat A, Li S, Knöchel T, Ferguson KM.

Cancer Cell. 2008 Apr;13(4):365-73. doi: 10.1016/j.ccr.2008.02.019.


Phosphorylation and regulation of a G protein-coupled receptor by protein kinase CK2.

Torrecilla I, Spragg EJ, Poulin B, McWilliams PJ, Mistry SC, Blaukat A, Tobin AB.

J Cell Biol. 2007 Apr 9;177(1):127-37. Epub 2007 Apr 2.


EGFR kinase domain mutations - functional impact and relevance for lung cancer therapy.

Irmer D, Funk JO, Blaukat A.

Oncogene. 2007 Aug 23;26(39):5693-701. Epub 2007 Mar 12. Review.


Phosphorylation by casein kinase 2 induces PACS-1 binding of nephrocystin and targeting to cilia.

Schermer B, Höpker K, Omran H, Ghenoiu C, Fliegauf M, Fekete A, Horvath J, Köttgen M, Hackl M, Zschiedrich S, Huber TB, Kramer-Zucker A, Zentgraf H, Blaukat A, Walz G, Benzing T.

EMBO J. 2005 Dec 21;24(24):4415-24. Epub 2005 Nov 24.


Mutation of tyrosine in the conserved NPXXY sequence leads to constitutive phosphorylation and internalization, but not signaling, of the human B2 bradykinin receptor.

Kalatskaya I, Schüssler S, Blaukat A, Müller-Esterl W, Jochum M, Proud D, Faussner A.

J Biol Chem. 2004 Jul 23;279(30):31268-76. Epub 2004 May 25.


Comparative analysis of functional assays for characterization of agonist ligands at G protein-coupled receptors.

Niedernberg A, Tunaru S, Blaukat A, Harris B, Kostenis E.

J Biomol Screen. 2003 Oct;8(5):500-10.


The tyrosine kinase Pyk2 regulates Arf1 activity by phosphorylation and inhibition of the Arf-GTPase-activating protein ASAP1.

Kruljac-Letunic A, Moelleken J, Kallin A, Wieland F, Blaukat A.

J Biol Chem. 2003 Aug 8;278(32):29560-70. Epub 2003 May 27.


Downregulation of bradykinin B2 receptor in human fibroblasts during prolonged agonist exposure.

Blaukat A, Micke P, Kalatskaya I, Faussner A, Müller-Esterl W.

Am J Physiol Heart Circ Physiol. 2003 Jun;284(6):H1909-16.


Sphingosine 1-phosphate and dioleoylphosphatidic acid are low affinity agonists for the orphan receptor GPR63.

Niedernberg A, Tunaru S, Blaukat A, Ardati A, Kostenis E.

Cell Signal. 2003 Apr;15(4):435-46.


Regulated and constitutive activation of specific signalling pathways by the human S1P5 receptor.

Niedernberg A, Blaukat A, Schöneberg T, Kostenis E.

Br J Pharmacol. 2003 Feb;138(3):481-93.


PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect.

Tunaru S, Kero J, Schaub A, Wufka C, Blaukat A, Pfeffer K, Offermanns S.

Nat Med. 2003 Mar;9(3):352-5. Epub 2003 Feb 3.


Structure and signalling pathways of kinin receptors.

Blaukat A.

Andrologia. 2003 Feb;35(1):17-23. Review.


Characterization of c-kit expression in small cell lung cancer: prognostic and therapeutic implications.

Micke P, Basrai M, Faldum A, Bittinger F, Rönnstrand L, Blaukat A, Beeh KM, Oesch F, Fischer B, Buhl R, Hengstler JG.

Clin Cancer Res. 2003 Jan;9(1):188-94.


Mechanisms for 2-methoxyestradiol-induced apoptosis of prostate cancer cells.

Bu S, Blaukat A, Fu X, Heldin NE, Landström M.

FEBS Lett. 2002 Nov 6;531(2):141-51.


Palmitoylation of the human bradykinin B2 receptor influences ligand efficacy.

Pizard A, Blaukat A, Michineau S, Dikic I, Müller-Esterl W, Alhenc-Gelas F, Rajerison RM.

Biochemistry. 2001 Dec 25;40(51):15743-51.


Determination of bradykinin B2 receptor in vivo phosphorylation sites and their role in receptor function.

Blaukat A, Pizard A, Breit A, Wernstedt C, Alhenc-Gelas F, Muller-Esterl W, Dikic I.

J Biol Chem. 2001 Nov 2;276(44):40431-40. Epub 2001 Aug 21.


Pyk2 and FAK regulate neurite outgrowth induced by growth factors and integrins.

Ivankovic-Dikic I, Grönroos E, Blaukat A, Barth BU, Dikic I.

Nat Cell Biol. 2000 Sep;2(9):574-81.


Protein tyrosine kinase-mediated pathways in G protein-coupled receptor signaling.

Dikic I, Blaukat A.

Cell Biochem Biophys. 1999;30(3):369-87. Review.


Activation of mitogen-activated protein kinase by the bradykinin B2 receptor is independent of receptor phosphorylation and phosphorylation-triggered internalization.

Blaukat A, Pizard A, Rajerison RM, Alhenc-Gelas F, Müller-Esterl W, Dikic I.

FEBS Lett. 1999 May 28;451(3):337-41.


Adaptor proteins Grb2 and Crk couple Pyk2 with activation of specific mitogen-activated protein kinase cascades.

Blaukat A, Ivankovic-Dikic I, Grönroos E, Dolfi F, Tokiwa G, Vuori K, Dikic I.

J Biol Chem. 1999 May 21;274(21):14893-901.


Bradykinin-induced internalization of the human B2 receptor requires phosphorylation of three serine and two threonine residues at its carboxyl tail.

Pizard A, Blaukat A, Müller-Esterl W, Alhenc-Gelas F, Rajerison RM.

J Biol Chem. 1999 Apr 30;274(18):12738-47.


Overexpression and functional characterization of kinin receptors reveal subtype-specific phosphorylation.

Blaukat A, Herzer K, Schroeder C, Bachmann M, Nash N, Müller-Esterl W.

Biochemistry. 1999 Jan 26;38(4):1300-9.


ACE inhibitor potentiation of bradykinin-induced venoconstriction.

Hecker M, Blaukat A, Bara AT, Müller-Esterl W, Busse R.

Br J Pharmacol. 1997 Aug;121(7):1475-81.


Inhibition of B2 receptor internalization delays its dephosphorylation.

Blaukat A, Müller-Esterl W.

Immunopharmacology. 1997 Jun;36(2-3):115-9. No abstract available.


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