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Items: 24

1.

Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation.

Baltschukat S, Engstler BS, Huang A, Hao HX, Tam A, Wang HQ, Liang J, DiMare MT, Bhang HC, Wang Y, Furet P, Sellers WR, Hofmann F, Schoepfer J, Tiedt R.

Clin Cancer Res. 2019 May 15;25(10):3164-3175. doi: 10.1158/1078-0432.CCR-18-2814. Epub 2019 Jan 23.

PMID:
30674502
2.

The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models.

Kim S, Tiedt R, Loo A, Horn T, Delach S, Kovats S, Haas K, Engstler BS, Cao A, Pinzon-Ortiz M, Mulford I, Acker MG, Chopra R, Brain C, di Tomaso E, Sellers WR, Caponigro G.

Oncotarget. 2018 Oct 16;9(81):35226-35240. doi: 10.18632/oncotarget.26215. eCollection 2018 Oct 16.

3.

Targeting multiple nodes of MLL complexes to improve leukemia therapy.

Dafflon C, Tiedt R, Schwaller J.

Oncotarget. 2017 Oct 7;8(53):90614-90615. doi: 10.18632/oncotarget.21598. eCollection 2017 Oct 31. No abstract available.

4.

Project DRIVE: A Compendium of Cancer Dependencies and Synthetic Lethal Relationships Uncovered by Large-Scale, Deep RNAi Screening.

McDonald ER 3rd, de Weck A, Schlabach MR, Billy E, Mavrakis KJ, Hoffman GR, Belur D, Castelletti D, Frias E, Gampa K, Golji J, Kao I, Li L, Megel P, Perkins TA, Ramadan N, Ruddy DA, Silver SJ, Sovath S, Stump M, Weber O, Widmer R, Yu J, Yu K, Yue Y, Abramowski D, Ackley E, Barrett R, Berger J, Bernard JL, Billig R, Brachmann SM, Buxton F, Caothien R, Caushi JX, Chung FS, Cortés-Cros M, deBeaumont RS, Delaunay C, Desplat A, Duong W, Dwoske DA, Eldridge RS, Farsidjani A, Feng F, Feng J, Flemming D, Forrester W, Galli GG, Gao Z, Gauter F, Gibaja V, Haas K, Hattenberger M, Hood T, Hurov KE, Jagani Z, Jenal M, Johnson JA, Jones MD, Kapoor A, Korn J, Liu J, Liu Q, Liu S, Liu Y, Loo AT, Macchi KJ, Martin T, McAllister G, Meyer A, Mollé S, Pagliarini RA, Phadke T, Repko B, Schouwey T, Shanahan F, Shen Q, Stamm C, Stephan C, Stucke VM, Tiedt R, Varadarajan M, Venkatesan K, Vitari AC, Wallroth M, Weiler J, Zhang J, Mickanin C, Myer VE, Porter JA, Lai A, Bitter H, Lees E, Keen N, Kauffmann A, Stegmeier F, Hofmann F, Schmelzle T, Sellers WR.

Cell. 2017 Jul 27;170(3):577-592.e10. doi: 10.1016/j.cell.2017.07.005.

5.

Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.

Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C.

ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9.

6.

Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf-/- mouse model.

Chapeau EA, Gembarska A, Durand EY, Mandon E, Estadieu C, Romanet V, Wiesmann M, Tiedt R, Lehar J, de Weck A, Rad R, Barys L, Jeay S, Ferretti S, Kauffmann A, Sutter E, Grevot A, Moulin P, Murakami M, Sellers WR, Hofmann F, Jensen MR.

Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3151-3156. doi: 10.1073/pnas.1620262114. Epub 2017 Mar 6.

7.

Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion-Positive Cholangiocarcinoma.

Goyal L, Saha SK, Liu LY, Siravegna G, Leshchiner I, Ahronian LG, Lennerz JK, Vu P, Deshpande V, Kambadakone A, Mussolin B, Reyes S, Henderson L, Sun JE, Van Seventer EE, Gurski JM Jr, Baltschukat S, Schacher-Engstler B, Barys L, Stamm C, Furet P, Ryan DP, Stone JR, Iafrate AJ, Getz G, Porta DG, Tiedt R, Bardelli A, Juric D, Corcoran RB, Bardeesy N, Zhu AX.

Cancer Discov. 2017 Mar;7(3):252-263. doi: 10.1158/2159-8290.CD-16-1000. Epub 2016 Dec 29.

8.

Complementary activities of DOT1L and Menin inhibitors in MLL-rearranged leukemia.

Dafflon C, Craig VJ, Méreau H, Gräsel J, Schacher Engstler B, Hoffman G, Nigsch F, Gaulis S, Barys L, Ito M, Aguadé-Gorgorió J, Bornhauser B, Bourquin JP, Proske A, Stork-Fux C, Murakami M, Sellers WR, Hofmann F, Schwaller J, Tiedt R.

Leukemia. 2017 Jun;31(6):1269-1277. doi: 10.1038/leu.2016.327. Epub 2016 Nov 14.

PMID:
27840424
9.

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.

Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C.

ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11.

10.

Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket.

Scheufler C, Möbitz H, Gaul C, Ragot C, Be C, Fernández C, Beyer KS, Tiedt R, Stauffer F.

ACS Med Chem Lett. 2016 Jun 6;7(8):730-4. doi: 10.1021/acsmedchemlett.6b00168. eCollection 2016 Aug 11.

11.

Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth.

Harbinski F, Craig VJ, Sanghavi S, Jeffery D, Liu L, Sheppard KA, Wagner S, Stamm C, Buness A, Chatenay-Rivauday C, Yao Y, He F, Lu CX, Guagnano V, Metz T, Finan PM, Hofmann F, Sellers WR, Porter JA, Myer VE, Graus-Porta D, Wilson CJ, Buckler A, Tiedt R.

Cancer Discov. 2012 Oct;2(10):948-59. doi: 10.1158/2159-8290.CD-12-0237. Epub 2012 Aug 8.

12.

Structure--activity relationship and mode of action of N-(6-ferrocenyl-2-naphthoyl) dipeptide ethyl esters: novel organometallic anticancer compounds.

Mooney A, Tiedt R, Maghoub T, O'Donovan N, Crown J, White B, Kenny PT.

J Med Chem. 2012 Jun 14;55(11):5455-66. doi: 10.1021/jm3004027. Epub 2012 May 21.

PMID:
22548380
13.

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.

Weigert O, Lane AA, Bird L, Kopp N, Chapuy B, van Bodegom D, Toms AV, Marubayashi S, Christie AL, McKeown M, Paranal RM, Bradner JE, Yoda A, Gaul C, Vangrevelinghe E, Romanet V, Murakami M, Tiedt R, Ebel N, Evrot E, De Pover A, Régnier CH, Erdmann D, Hofmann F, Eck MJ, Sallan SE, Levine RL, Kung AL, Baffert F, Radimerski T, Weinstock DM.

J Exp Med. 2012 Feb 13;209(2):259-73. doi: 10.1084/jem.20111694. Epub 2012 Jan 23.

14.

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.

15.

Pronounced thrombocytosis in transgenic mice expressing reduced levels of Mpl in platelets and terminally differentiated megakaryocytes.

Tiedt R, Coers J, Ziegler S, Wiestner A, Hao-Shen H, Bornmann C, Schenkel J, Karakhanova S, de Sauvage FJ, Jackson CW, Skoda RC.

Blood. 2009 Feb 19;113(8):1768-77. doi: 10.1182/blood-2008-03-146084. Epub 2008 Oct 9.

16.

A de novo splice donor mutation in the thrombopoietin gene causes hereditary thrombocythemia in a Polish family.

Liu K, Kralovics R, Rudzki Z, Grabowska B, Buser AS, Olcaydu D, Gisslinger H, Tiedt R, Frank P, Okoñ K, van der Maas AP, Skoda RC.

Haematologica. 2008 May;93(5):706-14. doi: 10.3324/haematol.11801. Epub 2008 Mar 26.

17.

Ratio of mutant JAK2-V617F to wild-type Jak2 determines the MPD phenotypes in transgenic mice.

Tiedt R, Hao-Shen H, Sobas MA, Looser R, Dirnhofer S, Schwaller J, Skoda RC.

Blood. 2008 Apr 15;111(8):3931-40. Epub 2007 Dec 26.

18.

Talin is required for integrin-mediated platelet function in hemostasis and thrombosis.

Petrich BG, Marchese P, Ruggeri ZM, Spiess S, Weichert RA, Ye F, Tiedt R, Skoda RC, Monkley SJ, Critchley DR, Ginsberg MH.

J Exp Med. 2007 Dec 24;204(13):3103-11. Epub 2007 Dec 17.

19.

Megakaryocyte-restricted MYH9 inactivation dramatically affects hemostasis while preserving platelet aggregation and secretion.

Léon C, Eckly A, Hechler B, Aleil B, Freund M, Ravanat C, Jourdain M, Nonne C, Weber J, Tiedt R, Gratacap MP, Severin S, Cazenave JP, Lanza F, Skoda R, Gachet C.

Blood. 2007 Nov 1;110(9):3183-91. Epub 2007 Jul 30.

20.
21.

Altered gene expression in myeloproliferative disorders correlates with activation of signaling by the V617F mutation of Jak2.

Kralovics R, Teo SS, Buser AS, Brutsche M, Tiedt R, Tichelli A, Passamonti F, Pietra D, Cazzola M, Skoda RC.

Blood. 2005 Nov 15;106(10):3374-6. Epub 2005 Aug 4.

22.

A gain-of-function mutation of JAK2 in myeloproliferative disorders.

Kralovics R, Passamonti F, Buser AS, Teo SS, Tiedt R, Passweg JR, Tichelli A, Cazzola M, Skoda RC.

N Engl J Med. 2005 Apr 28;352(17):1779-90.

23.

Zim17, a novel zinc finger protein essential for protein import into mitochondria.

Burri L, Vascotto K, Fredersdorf S, Tiedt R, Hall MN, Lithgow T.

J Biol Chem. 2004 Nov 26;279(48):50243-9. Epub 2004 Sep 21.

24.

The RING finger protein Siah-1 regulates the level of the transcriptional coactivator OBF-1.

Tiedt R, Bartholdy BA, Matthias G, Newell JW, Matthias P.

EMBO J. 2001 Aug 1;20(15):4143-52.

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