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Items: 42

1.

N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.

Schlapbach A, Revesz L, Pissot Soldermann C, Zoller T, Régnier CH, Bornancin F, Radimerski T, Blank J, Schuffenhauer A, Renatus M, Erbel P, Melkko S, Heng R, Simic O, Endres R, Wartmann M, Quancard J.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2153-2158. doi: 10.1016/j.bmcl.2018.05.017. Epub 2018 May 9.

PMID:
29759726
2.

Ex vivo drug response profiling detects recurrent sensitivity patterns in drug-resistant acute lymphoblastic leukemia.

Frismantas V, Dobay MP, Rinaldi A, Tchinda J, Dunn SH, Kunz J, Richter-Pechanska P, Marovca B, Pail O, Jenni S, Diaz-Flores E, Chang BH, Brown TJ, Collins RH, Uhrig S, Balasubramanian GP, Bandapalli OR, Higi S, Eugster S, Voegeli P, Delorenzi M, Cario G, Loh ML, Schrappe M, Stanulla M, Kulozik AE, Muckenthaler MU, Saha V, Irving JA, Meisel R, Radimerski T, Von Stackelberg A, Eckert C, Tyner JW, Horvath P, Bornhauser BC, Bourquin JP.

Blood. 2017 Mar 16;129(11):e26-e37. doi: 10.1182/blood-2016-09-738070. Epub 2017 Jan 25.

3.

JAK2 exon 12 mutant mice display isolated erythrocytosis and changes in iron metabolism favoring increased erythropoiesis.

Grisouard J, Li S, Kubovcakova L, Rao TN, Meyer SC, Lundberg P, Hao-Shen H, Romanet V, Murakami M, Radimerski T, Dirnhofer S, Skoda RC.

Blood. 2016 Aug 11;128(6):839-51. doi: 10.1182/blood-2015-12-689216. Epub 2016 Jun 10.

4.

HSP90 inhibition leads to degradation of the TYK2 kinase and apoptotic cell death in T-cell acute lymphoblastic leukemia.

Akahane K, Sanda T, Mansour MR, Radimerski T, DeAngelo DJ, Weinstock DM, Look AT.

Leukemia. 2016 Jan;30(1):219-28. doi: 10.1038/leu.2015.222. Epub 2015 Aug 12.

5.

Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.

Wu SC, Li LS, Kopp N, Montero J, Chapuy B, Yoda A, Christie AL, Liu H, Christodoulou A, van Bodegom D, van der Zwet J, Layer JV, Tivey T, Lane AA, Ryan JA, Ng SY, DeAngelo DJ, Stone RM, Steensma D, Wadleigh M, Harris M, Mandon E, Ebel N, Andraos R, Romanet V, Dölemeyer A, Sterker D, Zender M, Rodig SJ, Murakami M, Hofmann F, Kuo F, Eck MJ, Silverman LB, Sallan SE, Letai A, Baffert F, Vangrevelinghe E, Radimerski T, Gaul C, Weinstock DM.

Cancer Cell. 2015 Jul 13;28(1):29-41. doi: 10.1016/j.ccell.2015.06.005.

6.

CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms.

Meyer SC, Keller MD, Chiu S, Koppikar P, Guryanova OA, Rapaport F, Xu K, Manova K, Pankov D, O'Reilly RJ, Kleppe M, McKenney AS, Shih AH, Shank K, Ahn J, Papalexi E, Spitzer B, Socci N, Viale A, Mandon E, Ebel N, Andraos R, Rubert J, Dammassa E, Romanet V, Dölemeyer A, Zender M, Heinlein M, Rampal R, Weinberg RS, Hoffman R, Sellers WR, Hofmann F, Murakami M, Baffert F, Gaul C, Radimerski T, Levine RL.

Cancer Cell. 2015 Jul 13;28(1):15-28. doi: 10.1016/j.ccell.2015.06.006.

7.

JAK-STAT pathway activation in malignant and nonmalignant cells contributes to MPN pathogenesis and therapeutic response.

Kleppe M, Kwak M, Koppikar P, Riester M, Keller M, Bastian L, Hricik T, Bhagwat N, McKenney AS, Papalexi E, Abdel-Wahab O, Rampal R, Marubayashi S, Chen JJ, Romanet V, Fridman JS, Bromberg J, Teruya-Feldstein J, Murakami M, Radimerski T, Michor F, Fan R, Levine RL.

Cancer Discov. 2015 Mar;5(3):316-31. doi: 10.1158/2159-8290.CD-14-0736. Epub 2015 Jan 8.

8.

The identification and characterization of a STAT5 gene signature in hematologic malignancies.

Sonkin D, Palmer M, Rong X, Horrigan K, Regnier CH, Fanton C, Holash J, Pinzon-Ortiz M, Squires M, Sirulnik A, Radimerski T, Schlegel R, Morrissey M, Cao ZA.

Cancer Biomark. 2015;15(1):79-87. doi: 10.3233/CBM-140434.

PMID:
25524945
9.

Effects of Jak2 type 1 inhibitors NVP-BSK805 and NVP-BVB808 on Jak2 mutation-positive and Bcr-Abl-positive cell lines.

Ringel F, Kaeda J, Schwarz M, Oberender C, Grille P, Dörken B, Marque F, Manley PW, Radimerski T, le Coutre P.

Acta Haematol. 2014;132(1):75-86. doi: 10.1159/000356784. Epub 2014 Jan 31.

PMID:
24504330
10.

Targeting PI3K, HER2 and the IL-8/JAK2 axis in metastatic breast cancer: Which combination makes the whole greater than the sum of its parts?

Britschgi A, Radimerski T, Bentires-Alj M.

Drug Resist Updat. 2013 Jul-Nov;16(3-5):68-72. doi: 10.1016/j.drup.2013.10.001. Epub 2013 Oct 10. Review.

PMID:
24169539
11.

JAK1/2 and Pan-deacetylase inhibitor combination therapy yields improved efficacy in preclinical mouse models of JAK2V617F-driven disease.

Evrot E, Ebel N, Romanet V, Roelli C, Andraos R, Qian Z, Dölemeyer A, Dammassa E, Sterker D, Cozens R, Hofmann F, Murakami M, Baffert F, Radimerski T.

Clin Cancer Res. 2013 Nov 15;19(22):6230-41. doi: 10.1158/1078-0432.CCR-13-0905. Epub 2013 Sep 30.

12.

Differential effects of hydroxyurea and INC424 on mutant allele burden and myeloproliferative phenotype in a JAK2-V617F polycythemia vera mouse model.

Kubovcakova L, Lundberg P, Grisouard J, Hao-Shen H, Romanet V, Andraos R, Murakami M, Dirnhofer S, Wagner KU, Radimerski T, Skoda RC.

Blood. 2013 Feb 14;121(7):1188-99. doi: 10.1182/blood-2012-03-415646. Epub 2012 Dec 20.

13.

JAK2/STAT5 inhibition circumvents resistance to PI3K/mTOR blockade: a rationale for cotargeting these pathways in metastatic breast cancer.

Britschgi A, Andraos R, Brinkhaus H, Klebba I, Romanet V, Müller U, Murakami M, Radimerski T, Bentires-Alj M.

Cancer Cell. 2012 Dec 11;22(6):796-811. doi: 10.1016/j.ccr.2012.10.023.

14.

Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.

Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H, Bhagwat N, Koppikar P, Goel A, Wyder L, Tavares G, Baffert F, Pissot-Soldermann C, Manley PW, Gaul C, Voshol H, Levine RL, Sellers WR, Hofmann F, Radimerski T.

Cancer Discov. 2012 Jun;2(6):512-523. doi: 10.1158/2159-8290.CD-11-0324. Epub 2012 May 3.

15.

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.

16.

Metformin counters both lipolytic/inflammatory agents-decreased hormone sensitive lipase phosphorylation at Ser-554 and -induced lipolysis in human adipocytes.

Grisouard J, Timper K, Bouillet E, Radimerski T, Dembinski K, Frey DM, Peterli R, Zulewski H, Keller U, Müller B, Christ-Crain M.

Arch Physiol Biochem. 2011 Oct;117(4):209-14. doi: 10.3109/13813455.2010.550925. Epub 2011 Feb 22.

PMID:
21338323
17.

Bim and Mcl-1 exert key roles in regulating JAK2V617F cell survival.

Rubert J, Qian Z, Andraos R, Guthy DA, Radimerski T.

BMC Cancer. 2011 Jan 19;11:24. doi: 10.1186/1471-2407-11-24.

18.

Glucose-dependent insulinotropic polypeptide (GIP) induces calcitonin gene-related peptide (CGRP)-I and procalcitonin (Pro-CT) production in human adipocytes.

Timper K, Grisouard J, Radimerski T, Dembinski K, Peterli R, Häring A, Frey DM, Zulewski H, Keller U, Müller B, Christ-Crain M.

J Clin Endocrinol Metab. 2011 Feb;96(2):E297-303. doi: 10.1210/jc.2010-1324. Epub 2010 Nov 24.

PMID:
21106708
19.

Both inflammatory and classical lipolytic pathways are involved in lipopolysaccharide-induced lipolysis in human adipocytes.

Grisouard J, Bouillet E, Timper K, Radimerski T, Dembinski K, Frey DM, Peterli R, Zulewski H, Keller U, Müller B, Christ-Crain M.

Innate Immun. 2012 Feb;18(1):25-34. doi: 10.1177/1753425910386632. Epub 2010 Nov 18.

PMID:
21088047
20.

Mechanisms of metformin action on glucose transport and metabolism in human adipocytes.

Grisouard J, Timper K, Radimerski TM, Frey DM, Peterli R, Kola B, Korbonits M, Herrmann P, Krähenbühl S, Zulewski H, Keller U, Müller B, Christ-Crain M.

Biochem Pharmacol. 2010 Dec 1;80(11):1736-45. doi: 10.1016/j.bcp.2010.08.021. Epub 2010 Sep 8.

PMID:
20816671
21.

Role of calcium in lipopolysaccharide-induced calcitonin gene expression in human adipocytes.

Radimerski TM, Grisouard J, Timper K, Zulewski H, Christ-Crain M, Keller U, Müller B.

Innate Immun. 2011 Aug;17(4):403-13. doi: 10.1177/1753425910377100. Epub 2010 Aug 3.

PMID:
20682585
22.

Insulin resistance and increased lipolysis in bone marrow derived adipocytes stimulated with agonists of Toll-like receptors.

Franchini M, Monnais E, Seboek D, Radimerski T, Zini E, Kaufmann K, Lutz T, Reusch C, Ackermann M, Muller B, Linscheid P.

Horm Metab Res. 2010 Sep;42(10):703-9. doi: 10.1055/s-0030-1261872. Epub 2010 Jul 5.

23.

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.

24.

The nuclear receptor DHR3 modulates dS6 kinase-dependent growth in Drosophila.

Montagne J, Lecerf C, Parvy JP, Bennion JM, Radimerski T, Ruhf ML, Zilbermann F, Vouilloz N, Stocker H, Hafen E, Kozma SC, Thomas G.

PLoS Genet. 2010 May 6;6(5):e1000937. doi: 10.1371/journal.pgen.1000937.

25.

Metformin induces glucose uptake in human preadipocyte-derived adipocytes from various fat depots.

Fischer M, Timper K, Radimerski T, Dembinski K, Frey DM, Zulewski H, Keller U, Müller B, Christ-Crain M, Grisouard J.

Diabetes Obes Metab. 2010 Apr;12(4):356-9. doi: 10.1111/j.1463-1326.2009.01169.x.

PMID:
20380657
26.

Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800.

Massey AJ, Schoepfer J, Brough PA, Brueggen J, Chène P, Drysdale MJ, Pfaar U, Radimerski T, Ruetz S, Schweitzer A, Wood M, Garcia-Echeverria C, Jensen MR.

Mol Cancer Ther. 2010 Apr;9(4):906-19. doi: 10.1158/1535-7163.MCT-10-0055. Epub 2010 Apr 6.

27.

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
28.

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
29.

Procalcitonin levels predict clinical course and progression-free survival in patients with medullary thyroid cancer.

Walter MA, Meier C, Radimerski T, Iten F, Kränzlin M, Müller-Brand J, de Groot JW, Kema IP, Links TP, Müller B.

Cancer. 2010 Jan 1;116(1):31-40. doi: 10.1002/cncr.24738.

30.

Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.

Brough PA, Barril X, Borgognoni J, Chene P, Davies NG, Davis B, Drysdale MJ, Dymock B, Eccles SA, Garcia-Echeverria C, Fromont C, Hayes A, Hubbard RE, Jordan AM, Jensen MR, Massey A, Merrett A, Padfield A, Parsons R, Radimerski T, Raynaud FI, Robertson A, Roughley SD, Schoepfer J, Simmonite H, Sharp SY, Surgenor A, Valenti M, Walls S, Webb P, Wood M, Workman P, Wright L.

J Med Chem. 2009 Aug 13;52(15):4794-809. doi: 10.1021/jm900357y.

PMID:
19610616
31.

Discovery of a new class of catalytic topoisomerase II inhibitors targeting the ATP-binding site by structure based design. Part I.

Furet P, Schoepfer J, Radimerski T, Chène P.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4014-7. doi: 10.1016/j.bmcl.2009.06.034. Epub 2009 Jun 13.

PMID:
19560355
32.

Catalytic inhibition of topoisomerase II by a novel rationally designed ATP-competitive purine analogue.

Chène P, Rudloff J, Schoepfer J, Furet P, Meier P, Qian Z, Schlaeppi JM, Schmitz R, Radimerski T.

BMC Chem Biol. 2009 Jan 7;9:1. doi: 10.1186/1472-6769-9-1.

33.

NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models.

Jensen MR, Schoepfer J, Radimerski T, Massey A, Guy CT, Brueggen J, Quadt C, Buckler A, Cozens R, Drysdale MJ, Garcia-Echeverria C, Chène P.

Breast Cancer Res. 2008;10(2):R33. doi: 10.1186/bcr1996. Epub 2008 Apr 22.

34.

A nutrient sensor mechanism controls Drosophila growth.

Colombani J, Raisin S, Pantalacci S, Radimerski T, Montagne J, Léopold P.

Cell. 2003 Sep 19;114(6):739-49.

35.

The Drosophila forkhead transcription factor FOXO mediates the reduction in cell number associated with reduced insulin signaling.

Jünger MA, Rintelen F, Stocker H, Wasserman JD, Végh M, Radimerski T, Greenberg ME, Hafen E.

J Biol. 2003;2(3):20. Epub 2003 Aug 7.

36.

Rheb is an essential regulator of S6K in controlling cell growth in Drosophila.

Stocker H, Radimerski T, Schindelholz B, Wittwer F, Belawat P, Daram P, Breuer S, Thomas G, Hafen E.

Nat Cell Biol. 2003 Jun;5(6):559-65.

37.

Lethality of Drosophila lacking TSC tumor suppressor function rescued by reducing dS6K signaling.

Radimerski T, Montagne J, Hemmings-Mieszczak M, Thomas G.

Genes Dev. 2002 Oct 15;16(20):2627-32.

38.

Gliogenesis in Drosophila: genome-wide analysis of downstream genes of glial cells missing in the embryonic nervous system.

Egger B, Leemans R, Loop T, Kammermeier L, Fan Y, Radimerski T, Strahm MC, Certa U, Reichert H.

Development. 2002 Jul;129(14):3295-309.

39.

dS6K-regulated cell growth is dPKB/dPI(3)K-independent, but requires dPDK1.

Radimerski T, Montagne J, Rintelen F, Stocker H, van der Kaay J, Downes CP, Hafen E, Thomas G.

Nat Cell Biol. 2002 Mar;4(3):251-5.

40.

Insulin signaling: lessons from the Drosophila tuberous sclerosis complex, a tumor suppressor.

Montagne J, Radimerski T, Thomas G.

Sci STKE. 2001 Oct 23;2001(105):pe36. Review.

PMID:
11675514
41.

Genetic and biochemical characterization of dTOR, the Drosophila homolog of the target of rapamycin.

Oldham S, Montagne J, Radimerski T, Thomas G, Hafen E.

Genes Dev. 2000 Nov 1;14(21):2689-94.

42.

Identification of insulin-induced sites of ribosomal protein S6 phosphorylation in Drosophila melanogaster.

Radimerski T, Mini T, Schneider U, Wettenhall RE, Thomas G, Jenö P.

Biochemistry. 2000 May 16;39(19):5766-74.

PMID:
10801327

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