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Items: 41


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.


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.


A critical assessment of the synthesis and biological activity of p53/human double minute 2-stapled peptide inhibitors.

Wallbrecher R, Chène P, Ruetz S, Stachyra T, Vorherr T, Brock R.

Br J Pharmacol. 2017 Aug;174(16):2613-2622. doi: 10.1111/bph.13834. Epub 2017 Jul 6.


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.


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.


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.


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.


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.


A double blinded, placebo-controlled pilot study to examine reduction of CD34 +/CD117 +/CD133 + lymphoma progenitor cells and duration of remission induced by neoadjuvant valspodar in dogs with large B-cell lymphoma.

Ito D, Childress M, Mason N, Winter A, O'Brien T, Henson M, Borgatti A, Lewellen M, Krick E, Stewart J, Lahrman S, Rajwa B, Scott MC, Seelig D, Koopmeiners J, Ruetz S, Modiano J.

Version 3. F1000Res. 2015 Feb 11 [revised 2017 Jan 1];4:42. doi: 10.12688/f1000research.6055.3. eCollection 2015.


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.


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.


Quantified tumor t1 is a generic early-response imaging biomarker for chemotherapy reflecting cell viability.

McSheehy PM, Weidensteiner C, Cannet C, Ferretti S, Laurent D, Ruetz S, Stumm M, Allegrini PR.

Clin Cancer Res. 2010 Jan 1;16(1):212-25. doi: 10.1158/1078-0432.CCR-09-0686. Epub 2009 Dec 15.


Cis-stilbene derived furopyranones show potent antiproliferative activity by inducing G2/M arrest.

Fuhrer CA, Grüter E, Ruetz S, Häner R.

ChemMedChem. 2007 Apr;2(4):441-4. No abstract available.


The mTOR inhibitor RAD001 sensitizes tumor cells to DNA-damaged induced apoptosis through inhibition of p21 translation.

Beuvink I, Boulay A, Fumagalli S, Zilbermann F, Ruetz S, O'Reilly T, Natt F, Hall J, Lane HA, Thomas G.

Cell. 2005 Mar 25;120(6):747-59.


The human ubiquitin-conjugating enzyme Cdc34 controls cellular proliferation through regulation of p27Kip1 protein levels.

Butz N, Ruetz S, Natt F, Hall J, Weiler J, Mestan J, Ducarre M, Grossenbacher R, Hauser P, Kempf D, Hofmann F.

Exp Cell Res. 2005 Feb 15;303(2):482-93.


In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase.

García-Echeverría C, Pearson MA, Marti A, Meyer T, Mestan J, Zimmermann J, Gao J, Brueggen J, Capraro HG, Cozens R, Evans DB, Fabbro D, Furet P, Porta DG, Liebetanz J, Martiny-Baron G, Ruetz S, Hofmann F.

Cancer Cell. 2004 Mar;5(3):231-9.


Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors.

Ruetz S, Fabbro D, Zimmermann J, Meyer T, Gray N.

Curr Med Chem Anticancer Agents. 2003 Jan;3(1):1-14. Review.


beta-Homolysine oligomers: a new class of Trojan carriers.

García-Echeverría C, Ruetz S.

Bioorg Med Chem Lett. 2003 Jan 20;13(2):247-51.


Protein kinases as targets for anticancer agents: from inhibitors to useful drugs.

Fabbro D, Ruetz S, Buchdunger E, Cowan-Jacob SW, Fendrich G, Liebetanz J, Mestan J, O'Reilly T, Traxler P, Chaudhuri B, Fretz H, Zimmermann J, Meyer T, Caravatti G, Furet P, Manley PW.

Pharmacol Ther. 2002 Feb-Mar;93(2-3):79-98. Review.


Novel antiangiogenic effects of the bisphosphonate compound zoledronic acid.

Wood J, Bonjean K, Ruetz S, Bellahcène A, Devy L, Foidart JM, Castronovo V, Green JR.

J Pharmacol Exp Ther. 2002 Sep;302(3):1055-61.


PKC412--a protein kinase inhibitor with a broad therapeutic potential.

Fabbro D, Ruetz S, Bodis S, Pruschy M, Csermak K, Man A, Campochiaro P, Wood J, O'Reilly T, Meyer T.

Anticancer Drug Des. 2000 Feb;15(1):17-28.


Functional expression of the multidrug resistance-associated protein in the yeast Saccharomyces cerevisiae.

Ruetz S, Brault M, Kast C, Hemenway C, Heitman J, Grant CE, Cole SP, Deeley RG, Gros P.

J Biol Chem. 1999 Jan 22;274(4):2592. No abstract available.


The pfmdr1 gene of Plasmodium falciparum confers cellular resistance to antimalarial drugs in yeast cells.

Ruetz S, Delling U, Brault M, Schurr E, Gros P.

Proc Natl Acad Sci U S A. 1999 Feb 16;96(4):1810. No abstract available.


Functional interactions between synthetic alkyl phospholipids and the ABC transporters P-glycoprotein, Ste-6, MRP, and Pgh 1.

Ruetz S, Brault M, Dalton W, Gros P.

Biochemistry. 1999 Mar 2;38(9):2860. No abstract available.


Yeast secretory vesicle system for expression and functional characterization of P-glycoproteins.

Ruetz S.

Methods Enzymol. 1998;292:382-96. No abstract available.


Protein kinase C-mediated phosphorylation does not regulate drug transport by the human multidrug resistance P-glycoprotein.

Goodfellow HR, Sardini A, Ruetz S, Callaghan R, Gros P, McNaughton PA, Higgins CF.

J Biol Chem. 1996 Jun 7;271(23):13668-74.


ATP-dependent transport of organic anions in secretory vesicles of Saccharomyces cerevisiae.

St-Pierre MV, Ruetz S, Epstein LF, Gros P, Arias IM.

Proc Natl Acad Sci U S A. 1994 Sep 27;91(20):9476-9.


A mechanism for P-glycoprotein action in multidrug resistance: are we there yet?

Ruetz S, Gros P.

Trends Pharmacol Sci. 1994 Jul;15(7):260-3. Review.


Phosphatidylcholine translocase: a physiological role for the mdr2 gene.

Ruetz S, Gros P.

Cell. 1994 Jul 1;77(7):1071-81.


Functional expression of P-glycoproteins in secretory vesicles.

Ruetz S, Gros P.

J Biol Chem. 1994 Apr 22;269(16):12277-84.


Functional expression of P-glycoprotein encoded by the mouse mdr3 gene in yeast cells.

Ruetz S, Raymond M, Gros P.

Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11588-92.


Functional activation of plasma membrane anion exchangers occurs in a pre-Golgi compartment.

Ruetz S, Lindsey AE, Ward CL, Kopito RR.

J Cell Biol. 1993 Apr;121(1):37-48.


Function and biosynthesis of erythroid and nonerythroid anion exchangers.

Ruetz S, Lindsey AE, Kopito RR.

Soc Gen Physiol Ser. 1993;48:193-200. No abstract available.


Functional reconstitution of the canalicular bile salt transport system of rat liver.

Ruetz S, Hugentobler G, Meier PJ.

Proc Natl Acad Sci U S A. 1988 Aug;85(16):6147-51.


Isolation and characterization of the putative canalicular bile salt transport system of rat liver.

Ruetz S, Fricker G, Hugentobler G, Winterhalter K, Kurz G, Meier PJ.

J Biol Chem. 1987 Aug 15;262(23):11324-30.


Adriamycin as a probe for the transversal distribution of cardiolipin in the inner mitochondrial membrane.

Cheneval D, Müller M, Toni R, Ruetz S, Carafoli E.

J Biol Chem. 1985 Oct 25;260(24):13003-7.

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