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Items: 1 to 50 of 181

1.

Identification of FAM181A and FAM181B as new interactors with the TEAD transcription factors.

Bokhovchuk F, Mesrouze Y, Delaunay C, Martin T, Villard F, Meyerhofer M, Fontana P, Zimmermann C, Erdmann D, Furet P, Scheufler C, Schmelzle T, Chène P.

Protein Sci. 2019 Nov 7. doi: 10.1002/pro.3775. [Epub ahead of print]

PMID:
31697419
2.

Structure-based design of potent linear peptide inhibitors of the YAP-TEAD protein-protein interaction derived from the YAP omega-loop sequence.

Furet P, Salem B, Mesrouze Y, Schmelzle T, Lewis I, Kallen J, Chène P.

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2316-2319. doi: 10.1016/j.bmcl.2019.06.022. Epub 2019 Jun 18.

PMID:
31235263
3.

Structural States of Hdm2 and HdmX: X-ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes.

Kallen J, Izaac A, Chau S, Wirth E, Schoepfer J, Mah R, Schlapbach A, Stutz S, Vaupel A, Guagnano V, Masuya K, Stachyra TM, Salem B, Chene P, Gessier F, Holzer P, Furet P.

ChemMedChem. 2019 Jul 17;14(14):1305-1314. doi: 10.1002/cmdc.201900201. Epub 2019 May 27.

PMID:
31066983
4.

Molecular and structural characterization of a TEAD mutation at the origin of Sveinsson's chorioretinal atrophy.

Bokhovchuk F, Mesrouze Y, Izaac A, Meyerhofer M, Zimmermann C, Fontana P, Schmelzle T, Erdmann D, Furet P, Kallen J, Chène P.

FEBS J. 2019 Jun;286(12):2381-2398. doi: 10.1111/febs.14817. Epub 2019 Apr 11.

PMID:
30903741
5.

Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.

McNally R, Li Q, Li K, Dekker C, Vangrevelinghe E, Jones M, Chène P, Machauer R, Radimerski T, Eck MJ.

ACS Chem Biol. 2019 Apr 19;14(4):587-593. doi: 10.1021/acschembio.8b00722. Epub 2019 Mar 11.

PMID:
30763067
6.

Adaptation of the bound intrinsically disordered protein YAP to mutations at the YAP:TEAD interface.

Mesrouze Y, Bokhovchuk F, Izaac A, Meyerhofer M, Zimmermann C, Fontana P, Schmelzle T, Erdmann D, Furet P, Kallen J, Chène P.

Protein Sci. 2018 Oct;27(10):1810-1820. doi: 10.1002/pro.3493.

7.

1H, 13C, 15N resonance assignment of human YAP 50-171 fragment.

Feichtinger M, Sára T, Platzer G, Mateos B, Bokhovchuk F, Chène P, Konrat R.

Biomol NMR Assign. 2018 Apr;12(1):179-182. doi: 10.1007/s12104-018-9805-8. Epub 2018 Jan 25.

8.

Effect of the acylation of TEAD4 on its interaction with co-activators YAP and TAZ.

Mesrouze Y, Meyerhofer M, Bokhovchuk F, Fontana P, Zimmermann C, Martin T, Delaunay C, Izaac A, Kallen J, Schmelzle T, Erdmann D, Chène P.

Protein Sci. 2017 Dec;26(12):2399-2409. doi: 10.1002/pro.3312. Epub 2017 Nov 11.

9.

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.

10.

Dissection of the interaction between the intrinsically disordered YAP protein and the transcription factor TEAD.

Mesrouze Y, Bokhovchuk F, Meyerhofer M, Fontana P, Zimmermann C, Martin T, Delaunay C, Erdmann D, Schmelzle T, Chène P.

Elife. 2017 Apr 21;6. pii: e25068. doi: 10.7554/eLife.25068.

11.

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
12.

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
13.

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
14.

Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials.

Fritsch C, Huang A, Chatenay-Rivauday C, Schnell C, Reddy A, Liu M, Kauffmann A, Guthy D, Erdmann D, De Pover A, Furet P, Gao H, Ferretti S, Wang Y, Trappe J, Brachmann SM, Maira SM, Wilson C, Boehm M, Garcia-Echeverria C, Chene P, Wiesmann M, Cozens R, Lehar J, Schlegel R, Caravatti G, Hofmann F, Sellers WR.

Mol Cancer Ther. 2014 May;13(5):1117-29. doi: 10.1158/1535-7163.MCT-13-0865. Epub 2014 Mar 7.

15.

The surprising features of the TEAD4-Vgll1 protein-protein interaction.

Mesrouze Y, Hau JC, Erdmann D, Zimmermann C, Fontana P, Schmelzle T, Chène P.

Chembiochem. 2014 Mar 3;15(4):537-42. doi: 10.1002/cbic.201300715. Epub 2014 Feb 6.

PMID:
24504694
16.

The TEAD4-YAP/TAZ protein-protein interaction: expected similarities and unexpected differences.

Hau JC, Erdmann D, Mesrouze Y, Furet P, Fontana P, Zimmermann C, Schmelzle T, Hofmann F, Chène P.

Chembiochem. 2013 Jul 8;14(10):1218-25. doi: 10.1002/cbic.201300163. Epub 2013 Jun 18.

PMID:
23780915
17.

M2 isoform of pyruvate kinase is dispensable for tumor maintenance and growth.

Cortés-Cros M, Hemmerlin C, Ferretti S, Zhang J, Gounarides JS, Yin H, Muller A, Haberkorn A, Chene P, Sellers WR, Hofmann F.

Proc Natl Acad Sci U S A. 2013 Jan 8;110(2):489-94. doi: 10.1073/pnas.1212780110. Epub 2012 Dec 24.

18.

The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.

Furet P, Chène P, De Pover A, Valat TS, Lisztwan JH, Kallen J, Masuya K.

Bioorg Med Chem Lett. 2012 May 15;22(10):3498-502. doi: 10.1016/j.bmcl.2012.03.083. Epub 2012 Mar 30.

PMID:
22507962
19.

Can biochemistry drive drug discovery beyond simple potency measurements?

Chène P.

Drug Discov Today. 2012 Apr;17(7-8):388-95. doi: 10.1016/j.drudis.2012.01.022. Epub 2012 Feb 3. Review.

PMID:
22326379
20.

Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.

Maira SM, Pecchi S, Huang A, Burger M, Knapp M, Sterker D, Schnell C, Guthy D, Nagel T, Wiesmann M, Brachmann S, Fritsch C, Dorsch M, Chène P, Shoemaker K, De Pover A, Menezes D, Martiny-Baron G, Fabbro D, Wilson CJ, Schlegel R, Hofmann F, García-Echeverría C, Sellers WR, Voliva CF.

Mol Cancer Ther. 2012 Feb;11(2):317-28. doi: 10.1158/1535-7163.MCT-11-0474. Epub 2011 Dec 21.

21.

Factors influencing the inhibition of protein kinases.

Brockhoff M, Hau JC, Fontana P, Zimmermann C, Pover AD, Erdmann D, Chène P.

J Enzyme Inhib Med Chem. 2012 Apr;27(2):194-200. doi: 10.3109/14756366.2011.583922. Epub 2011 Jun 3.

PMID:
21635207
22.

Leveraging the contribution of thermodynamics in drug discovery with the help of fluorescence-based thermal shift assays.

Hau JC, Fontana P, Zimmermann C, De Pover A, Erdmann D, Chène P.

J Biomol Screen. 2011 Jun;16(5):552-6. doi: 10.1177/1087057111399573. Epub 2011 Mar 25.

PMID:
21441415
23.

"4D Biology for health and disease" workshop report.

Abrahams JP, Apweiler R, Balling R, Bertero MG, Bujnicki JM, Chayen NE, Chène P, Corthals GL, Dyląg T, Förster F, Heck AJ, Henderson PJ, Herwig R, Jehenson P, Kokalj SJ, Laue E, Legrain P, Martens L, Migliorini C, Musacchio A, Podobnik M, Schertler GF, Schreiber G, Sixma TK, Smit AB, Stuart D, Svergun DI, Taussig MJ.

N Biotechnol. 2011 Jul;28(4):291-3. doi: 10.1016/j.nbt.2010.10.003. Epub 2010 Oct 15.

PMID:
20951846
24.

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.

25.

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.

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
28.

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
29.

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
30.

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.

31.

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity.

Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K, Fabbro D, Gabriel D, Simonen M, Murphy L, Finan P, Sellers W, García-Echeverría C.

Mol Cancer Ther. 2008 Jul;7(7):1851-63. doi: 10.1158/1535-7163.MCT-08-0017. Epub 2008 Jul 7.

32.

Challenges in design of biochemical assays for the identification of small molecules to target multiple conformations of protein kinases.

Chène P.

Drug Discov Today. 2008 Jun;13(11-12):522-9. doi: 10.1016/j.drudis.2008.03.023. Epub 2008 May 5. Review.

PMID:
18549979
33.

Signalling profile and antitumour activity of the novel Hsp90 inhibitor NVP-AUY922 in multiple myeloma.

Stühmer T, Zöllinger A, Siegmund D, Chatterjee M, Grella E, Knop S, Kortüm M, Unzicker C, Jensen MR, Quadt C, Chène P, Schoepfer J, García-Echeverría C, Einsele H, Wajant H, Bargou RC.

Leukemia. 2008 Aug;22(8):1604-12. doi: 10.1038/leu.2008.111. Epub 2008 May 15.

PMID:
18480838
34.

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.

35.

Cellular studies of MrDb (DDX18).

Dubaele S, Chène P.

Oncol Res. 2007;16(12):549-56.

PMID:
18351129
36.

Towards the design of flavivirus helicase/NTPase inhibitors: crystallographic and mutagenesis studies of the dengue virus NS3 helicase catalytic domain.

Xu T, Sampath A, Chao A, Wen D, Nanao M, Luo D, Chene P, Vasudevan SG, Lescar J.

Novartis Found Symp. 2006;277:87-97; discussion 97-101, 251-3.

PMID:
17319156
37.

Biochemical study of recombinant PcrA from Staphylococcus aureus for the development of screening assays.

Dubaele S, Martin C, Bohn J, Chène P.

J Biochem Mol Biol. 2007 Jan 31;40(1):7-14.

PMID:
17244476
38.

Drugs targeting protein-protein interactions.

Chène P.

ChemMedChem. 2006 Apr;1(4):400-11. Review.

PMID:
16892375
39.

The effect of hypoxia on the expression of 150 kDa oxygen-regulated protein (ORP 150) in HeLa cells.

Cechowska-Pasko M, Bankowski E, Chene P.

Cell Physiol Biochem. 2006;17(1-2):89-96. Epub 2006 Feb 7.

40.

Study of the ATP-binding site of helicase IV from Escherichia coli.

Dubaele S, Lourdel C, Chène P.

Biochem Biophys Res Commun. 2006 Mar 17;341(3):828-36. Epub 2006 Jan 23.

PMID:
16442499
41.

Inhibition of DNA helicases with DNA-competitive inhibitors.

Dubaele S, Jahnke W, Schoepfer J, Fuchs J, Chène P.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):923-7. Epub 2005 Nov 21.

PMID:
16300943
42.

Glucose effect on the expression of 150 kDa oxygen-regulated protein in HeLa cells.

Cechowska-Pasko M, Bańkowski E, Chene P.

Biochem Biophys Res Commun. 2005 Nov 25;337(3):992-7. Epub 2005 Oct 3.

PMID:
16216220
43.

Structure of the Dengue virus helicase/nucleoside triphosphatase catalytic domain at a resolution of 2.4 A.

Xu T, Sampath A, Chao A, Wen D, Nanao M, Chene P, Vasudevan SG, Lescar J.

J Virol. 2005 Aug;79(16):10278-88.

44.
45.

Inhibition of the p53-hdm2 interaction with low molecular weight compounds.

Chène P.

Cell Cycle. 2004 Apr;3(4):460-1. Epub 2004 Apr 1.

PMID:
14976429
46.
47.

The ATPases: a new family for a family-based drug design approach.

Chène P.

Expert Opin Ther Targets. 2003 Jun;7(3):453-61. Review.

PMID:
12783580
48.

Targeting p53 in cancer.

Chène P.

Curr Med Chem Anticancer Agents. 2001 Aug;1(2):151-61. Review.

PMID:
12678764
49.

Inhibiting the p53-MDM2 interaction: an important target for cancer therapy.

Chène P.

Nat Rev Cancer. 2003 Feb;3(2):102-9. Review.

PMID:
12563309
50.

Study of the cytotoxic effect of a peptidic inhibitor of the p53-hdm2 interaction in tumor cells.

Chène P, Fuchs J, Carena I, Furet P, García-Echeverría C.

FEBS Lett. 2002 Oct 9;529(2-3):293-7.

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