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Items: 34

1.

In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.

Vaupel A, Holzer P, Ferretti S, Guagnano V, Kallen J, Mah R, Masuya K, Ruetz S, Rynn C, Schlapbach A, Stachyra T, Stutz S, Todorov M, Jeay S, Furet P.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3404-3408. doi: 10.1016/j.bmcl.2018.08.027. Epub 2018 Aug 26.

PMID:
30217415
2.

Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201.

Jeay S, Ferretti S, Holzer P, Fuchs J, Chapeau EA, Wartmann M, Sterker D, Romanet V, Murakami M, Kerr G, Durand EY, Gaulis S, Cortes-Cros M, Ruetz S, Stachyra TM, Kallen J, Furet P, Würthner J, Guerreiro N, Halilovic E, Jullion A, Kauffmann A, Kuriakose E, Wiesmann M, Jensen MR, Hofmann F, Sellers WR.

Cancer Res. 2018 Nov 1;78(21):6257-6267. doi: 10.1158/0008-5472.CAN-18-0338. Epub 2018 Aug 22.

PMID:
30135191
3.

A Comprehensive Patient-Derived Xenograft Collection Representing the Heterogeneity of Melanoma.

Krepler C, Sproesser K, Brafford P, Beqiri M, Garman B, Xiao M, Shannan B, Watters A, Perego M, Zhang G, Vultur A, Yin X, Liu Q, Anastopoulos IN, Wubbenhorst B, Wilson MA, Xu W, Karakousis G, Feldman M, Xu X, Amaravadi R, Gangadhar TC, Elder DE, Haydu LE, Wargo JA, Davies MA, Lu Y, Mills GB, Frederick DT, Barzily-Rokni M, Flaherty KT, Hoon DS, Guarino M, Bennett JJ, Ryan RW, Petrelli NJ, Shields CL, Terai M, Sato T, Aplin AE, Roesch A, Darr D, Angus S, Kumar R, Halilovic E, Caponigro G, Jeay S, Wuerthner J, Walter A, Ocker M, Boxer MB, Schuchter L, Nathanson KL, Herlyn M.

Cell Rep. 2017 Nov 14;21(7):1953-1967. doi: 10.1016/j.celrep.2017.10.021.

4.

Combined ALK and MDM2 inhibition increases antitumor activity and overcomes resistance in human ALK mutant neuroblastoma cell lines and xenograft models.

Wang HQ, Halilovic E, Li X, Liang J, Cao Y, Rakiec DP, Ruddy DA, Jeay S, Wuerthner JU, Timple N, Kasibhatla S, Li N, Williams JA, Sellers WR, Huang A, Li F.

Elife. 2017 Apr 20;6. pii: e17137. doi: 10.7554/eLife.17137.

5.

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.

6.

The HDM2 (MDM2) Inhibitor NVP-CGM097 Inhibits Tumor Cell Proliferation and Shows Additive Effects with 5-Fluorouracil on the p53-p21-Rb-E2F1 Cascade in the p53wild type Neuroendocrine Tumor Cell Line GOT1.

Reuther C, Heinzle V, Nölting S, Herterich S, Hahner S, Halilovic E, Jeay S, Wuerthner JU, Aristizabal Prada ET, Spöttl G, Maurer J, Auernhammer CJ.

Neuroendocrinology. 2018;106(1):1-19. doi: 10.1159/000453369. Epub 2016 Nov 21.

PMID:
27871087
7.

Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.

Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.

Elife. 2016 Nov 17;5. pii: e19317. doi: 10.7554/eLife.19317. No abstract available.

8.

High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells.

Horn T, Ferretti S, Ebel N, Tam A, Ho S, Harbinski F, Farsidjani A, Zubrowski M, Sellers WR, Schlegel R, Porter D, Morris E, Wuerthner J, Jeay S, Greshock J, Halilovic E, Garraway LA, Caponigro G, Lehár J.

Cancer Res. 2016 Dec 1;76(23):6950-6963. Epub 2016 Sep 22.

9.

Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.

Furet P, Masuya K, Kallen J, Stachyra-Valat T, Ruetz S, Guagnano V, Holzer P, Mah R, Stutz S, Vaupel A, Chène P, Jeay S, Schlapbach A.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-4841. doi: 10.1016/j.bmcl.2016.08.010. Epub 2016 Aug 9.

PMID:
27542305
10.

Dual inhibition of protein kinase C and p53-MDM2 or PKC and mTORC1 are novel efficient therapeutic approaches for uveal melanoma.

Carita G, Frisch-Dit-Leitz E, Dahmani A, Raymondie C, Cassoux N, Piperno-Neumann S, Némati F, Laurent C, De Koning L, Halilovic E, Jeay S, Wylie A, Emery C, Roman-Roman S, Schoumacher M, Decaudin D.

Oncotarget. 2016 Jun 7;7(23):33542-56. doi: 10.18632/oncotarget.9552.

11.

The Public Repository of Xenografts Enables Discovery and Randomized Phase II-like Trials in Mice.

Townsend EC, Murakami MA, Christodoulou A, Christie AL, Köster J, DeSouza TA, Morgan EA, Kallgren SP, Liu H, Wu SC, Plana O, Montero J, Stevenson KE, Rao P, Vadhi R, Andreeff M, Armand P, Ballen KK, Barzaghi-Rinaudo P, Cahill S, Clark RA, Cooke VG, Davids MS, DeAngelo DJ, Dorfman DM, Eaton H, Ebert BL, Etchin J, Firestone B, Fisher DC, Freedman AS, Galinsky IA, Gao H, Garcia JS, Garnache-Ottou F, Graubert TA, Gutierrez A, Halilovic E, Harris MH, Herbert ZT, Horwitz SM, Inghirami G, Intlekofer AM, Ito M, Izraeli S, Jacobsen ED, Jacobson CA, Jeay S, Jeremias I, Kelliher MA, Koch R, Konopleva M, Kopp N, Kornblau SM, Kung AL, Kupper TS, LeBoeuf NR, LaCasce AS, Lees E, Li LS, Look AT, Murakami M, Muschen M, Neuberg D, Ng SY, Odejide OO, Orkin SH, Paquette RR, Place AE, Roderick JE, Ryan JA, Sallan SE, Shoji B, Silverman LB, Soiffer RJ, Steensma DP, Stegmaier K, Stone RM, Tamburini J, Thorner AR, van Hummelen P, Wadleigh M, Wiesmann M, Weng AP, Wuerthner JU, Williams DA, Wollison BM, Lane AA, Letai A, Bertagnolli MM, Ritz J, Brown M, Long H, Aster JC, Shipp MA, Griffin JD, Weinstock DM.

Cancer Cell. 2016 Jul 11;30(1):183. doi: 10.1016/j.ccell.2016.06.008. Epub 2016 Jul 11. No abstract available.

12.

The Public Repository of Xenografts Enables Discovery and Randomized Phase II-like Trials in Mice.

Townsend EC, Murakami MA, Christodoulou A, Christie AL, Köster J, DeSouza TA, Morgan EA, Kallgren SP, Liu H, Wu SC, Plana O, Montero J, Stevenson KE, Rao P, Vadhi R, Andreeff M, Armand P, Ballen KK, Barzaghi-Rinaudo P, Cahill S, Clark RA, Cooke VG, Davids MS, DeAngelo DJ, Dorfman DM, Eaton H, Ebert BL, Etchin J, Firestone B, Fisher DC, Freedman AS, Galinsky IA, Gao H, Garcia JS, Garnache-Ottou F, Graubert TA, Gutierrez A, Halilovic E, Harris MH, Herbert ZT, Horwitz SM, Inghirami G, Intlekofer AM, Ito M, Izraeli S, Jacobsen ED, Jacobson CA, Jeay S, Jeremias I, Kelliher MA, Koch R, Konopleva M, Kopp N, Kornblau SM, Kung AL, Kupper TS, LeBoeuf NR, LaCasce AS, Lees E, Li LS, Look AT, Murakami M, Muschen M, Neuberg D, Ng SY, Odejide OO, Orkin SH, Paquette RR, Place AE, Roderick JE, Ryan JA, Sallan SE, Shoji B, Silverman LB, Soiffer RJ, Steensma DP, Stegmaier K, Stone RM, Tamburini J, Thorner AR, van Hummelen P, Wadleigh M, Wiesmann M, Weng AP, Wuerthner JU, Williams DA, Wollison BM, Lane AA, Letai A, Bertagnolli MM, Ritz J, Brown M, Long H, Aster JC, Shipp MA, Griffin JD, Weinstock DM.

Cancer Cell. 2016 Apr 11;29(4):574-586. doi: 10.1016/j.ccell.2016.03.008. Erratum in: Cancer Cell. 2016 Jul 11;30(1):183.

13.

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Fairhurst RA, Marsilje TH, Stutz S, Boos A, Niklaus M, Chen B, Jiang S, Lu W, Furet P, McCarthy C, Stauffer F, Guagnano V, Vaupel A, Michellys PY, Schnell C, Jeay S.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2057-64. doi: 10.1016/j.bmcl.2016.02.075. Epub 2016 Feb 26.

PMID:
26951753
14.

Inhibition of Wild-Type p53-Expressing AML by the Novel Small Molecule HDM2 Inhibitor CGM097.

Weisberg E, Halilovic E, Cooke VG, Nonami A, Ren T, Sanda T, Simkin I, Yuan J, Antonakos B, Barys L, Ito M, Stone R, Galinsky I, Cowens K, Nelson E, Sattler M, Jeay S, Wuerthner JU, McDonough SM, Wiesmann M, Griffin JD.

Mol Cancer Ther. 2015 Oct;14(10):2249-59. doi: 10.1158/1535-7163.MCT-15-0429. Epub 2015 Jul 23.

15.

Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.

Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F.

J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810. Epub 2015 Aug 5.

PMID:
26181851
16.

Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.

Gessier F, Kallen J, Jacoby E, Chène P, Stachyra-Valat T, Ruetz S, Jeay S, Holzer P, Masuya K, Furet P.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3621-5. doi: 10.1016/j.bmcl.2015.06.058. Epub 2015 Jun 23.

PMID:
26141769
17.

A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.

Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.

Elife. 2015 May 12;4. pii: e06498. doi: 10.7554/eLife.06498. Erratum in: Elife. 2016 Nov 17;5:null.

18.

Dependence of Wilms tumor cells on signaling through insulin-like growth factor 1 in an orthotopic xenograft model targetable by specific receptor inhibition.

Bielen A, Box G, Perryman L, Bjerke L, Popov S, Jamin Y, Jury A, Valenti M, Brandon Ade H, Martins V, Romanet V, Jeay S, Raynaud FI, Hofmann F, Robinson SP, Eccles SA, Jones C.

Proc Natl Acad Sci U S A. 2012 May 15;109(20):E1267-76. doi: 10.1073/pnas.1105034109. Epub 2012 Apr 23.

19.

Enhanced efficacy of IGF1R inhibition in pediatric glioblastoma by combinatorial targeting of PDGFRα/β.

Bielen A, Perryman L, Box GM, Valenti M, de Haven Brandon A, Martins V, Jury A, Popov S, Gowan S, Jeay S, Raynaud FI, Hofmann F, Hargrave D, Eccles SA, Jones C.

Mol Cancer Ther. 2011 Aug;10(8):1407-18. doi: 10.1158/1535-7163.MCT-11-0205. Epub 2011 Jun 9.

20.

ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity.

Munshi N, Jeay S, Li Y, Chen CR, France DS, Ashwell MA, Hill J, Moussa MM, Leggett DS, Li CJ.

Mol Cancer Ther. 2010 Jun;9(6):1544-53. doi: 10.1158/1535-7163.MCT-09-1173. Epub 2010 May 18.

21.

c-Myc represses FOXO3a-mediated transcription of the gene encoding the p27(Kip1) cyclin dependent kinase inhibitor.

Chandramohan V, Mineva ND, Burke B, Jeay S, Wu M, Shen J, Yang W, Hann SR, Sonenshein GE.

J Cell Biochem. 2008 Aug 15;104(6):2091-106. doi: 10.1002/jcb.21765.

PMID:
18393360
22.

The tumor suppressor activity of the lysyl oxidase propeptide reverses the invasive phenotype of Her-2/neu-driven breast cancer.

Min C, Kirsch KH, Zhao Y, Jeay S, Palamakumbura AH, Trackman PC, Sonenshein GE.

Cancer Res. 2007 Feb 1;67(3):1105-12.

23.

The propeptide domain of lysyl oxidase induces phenotypic reversion of ras-transformed cells.

Palamakumbura AH, Jeay S, Guo Y, Pischon N, Sommer P, Sonenshein GE, Trackman PC.

J Biol Chem. 2004 Sep 24;279(39):40593-600. Epub 2004 Jul 23.

24.
25.

B-Myb repressor function is regulated by cyclin A phosphorylation and sequences within the C-terminal domain.

Petrovas C, Jeay S, Lewis RE, Sonenshein GE.

Oncogene. 2003 Apr 3;22(13):2011-20.

PMID:
12673206
26.

New homologous bioassays for human lactogens show that agonism or antagonism of various analogs is a function of assay sensitivity.

Bernichtein S, Jeay S, Vaudry R, Kelly PA, Goffin V.

Endocrine. 2003 Feb-Mar;20(1-2):177-90.

PMID:
12668884
27.

Lysyl oxidase inhibits ras-mediated transformation by preventing activation of NF-kappa B.

Jeay S, Pianetti S, Kagan HM, Sonenshein GE.

Mol Cell Biol. 2003 Apr;23(7):2251-63.

28.

Growth hormone can act as a cytokine controlling survival and proliferation of immune cells: new insights into signaling pathways.

Jeay S, Sonenshein GE, Postel-Vinay MC, Kelly PA, Baixeras E.

Mol Cell Endocrinol. 2002 Feb 25;188(1-2):1-7. Review.

PMID:
11911939
29.

S179D-human PRL, a pseudophosphorylated human PRL analog, is an agonist and not an antagonist.

Bernichtein S, Kinet S, Jeay S, Llovera M, Madern D, Martial JA, Kelly PA, Goffin V.

Endocrinology. 2001 Sep;142(9):3950-63.

31.
32.

Human prolactin (hPRL) antagonists inhibit hPRL-activated signaling pathways involved in breast cancer cell proliferation.

Llovera M, Pichard C, Bernichtein S, Jeay S, Touraine P, Kelly PA, Goffin V.

Oncogene. 2000 Sep 28;19(41):4695-705.

33.

Growth hormone prevents apoptosis through activation of nuclear factor-kappaB in interleukin-3-dependent Ba/F3 cell line.

Jeay S, Sonenshein GE, Postel-Vinay MC, Baixeras E.

Mol Endocrinol. 2000 May;14(5):650-61.

PMID:
10809229
34.

Growth hormone (GH) and prolactin receptors in human peripheral blood mononuclear cells: relation with age and GH-binding protein.

Bresson JL, Jeay S, Gagnerault MC, Kayser C, Beressi N, Wu Z, Kinet S, Dardenne M, Postel-Vinay MC.

Endocrinology. 1999 Jul;140(7):3203-9.

PMID:
10385416

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