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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]


FGF401, a first-in-class highly selective and potent FGFR4 inhibitor for the treatment of FGF19-driven hepatocellular cancer.

Weiss A, Adler F, Buhles A, Stamm C, Fairhurst RA, Kiffe M, Sterker D, Centeleghe M, Wartmann M, Kinyamu-Akunda J, Schadt HS, Couttet P, Wolf A, Wang Y, Barzaghi-Rinaudo P, Murakami M, Kauffmann A, Knoepfel T, Buschmann N, Leblanc C, Mah R, Furet P, Blank J, Hofmann F, Sellers WR, Graus Porta D.

Mol Cancer Ther. 2019 Aug 13. pii: molcanther.1291.2018. doi: 10.1158/1535-7163.MCT-18-1291. [Epub ahead of print]


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.


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.


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.


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.


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.


Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy.

Manley PW, Caravatti G, Furet P, Roesel J, Tran P, Wagner T, Wartmann M.

Biochemistry. 2018 Sep 25;57(38):5576-5590. doi: 10.1021/acs.biochem.8b00727. Epub 2018 Sep 13.


Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.

Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P.

J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7.


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.


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.


2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.

Knoepfel T, Furet P, Mah R, Buschmann N, Leblanc C, Ripoche S, Graus-Porta D, Wartmann M, Galuba I, Fairhurst RA.

ACS Med Chem Lett. 2018 Feb 1;9(3):215-220. doi: 10.1021/acsmedchemlett.7b00485. eCollection 2018 Mar 8.


Asparagine and sugars are both required to sustain secondary axis elongation after bud outgrowth in Rosa hybrida.

Le Moigne MA, Guérin V, Furet PM, Billard V, Lebrec A, Spíchal L, Roman H, Citerne S, Morvan-Bertrand A, Limami A, Vian A, Lothier J.

J Plant Physiol. 2018 Mar;222:17-27. doi: 10.1016/j.jplph.2017.12.013. Epub 2017 Dec 26.


Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.

Fairhurst RA, Knoepfel T, Leblanc C, Buschmann N, Gaul C, Blank J, Galuba I, Trappe J, Zou C, Voshol J, Genick C, Brunet-Lefeuvre P, Bitsch F, Graus-Porta D, Furet P.

Medchemcomm. 2017 Jun 8;8(8):1604-1613. doi: 10.1039/c7md00213k. eCollection 2017 Aug 1.


The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.

Wylie AA, Schoepfer J, Jahnke W, Cowan-Jacob SW, Loo A, Furet P, Marzinzik AL, Pelle X, Donovan J, Zhu W, Buonamici S, Hassan AQ, Lombardo F, Iyer V, Palmer M, Berellini G, Dodd S, Thohan S, Bitter H, Branford S, Ross DM, Hughes TP, Petruzzelli L, Vanasse KG, Warmuth M, Hofmann F, Keen NJ, Sellers WR.

Nature. 2017 Mar 30;543(7647):733-737. doi: 10.1038/nature21702. Epub 2017 Mar 22.


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.


Bioorthogonal Probes for the Study of MDM2-p53 Inhibitors in Cells and Development of High-Content Screening Assays for Drug Discovery.

D'Alessandro PL, Buschmann N, Kaufmann M, Furet P, Baysang F, Brunner R, Marzinzik A, Vorherr T, Stachyra TM, Ottl J, Lizos DE, Cobos-Correa A.

Angew Chem Int Ed Engl. 2016 Dec 23;55(52):16026-16030. doi: 10.1002/anie.201608568. Epub 2016 Nov 22.


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 and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.

Hoegenauer K, Soldermann N, Stauffer F, Furet P, Graveleau N, Smith AB, Hebach C, Hollingworth GJ, Lewis I, Gutmann S, Rummel G, Knapp M, Wolf RM, Blanz J, Feifel R, Burkhart C, Zécri F.

ACS Med Chem Lett. 2016 Jun 2;7(8):762-7. doi: 10.1021/acsmedchemlett.6b00119. eCollection 2016 Aug 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.


Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.

Shaw DE, Baig F, Bruce I, Chamoin S, Collingwood SP, Cross S, Dayal S, Drückes P, Furet P, Furminger V, Haggart D, Hussey M, Konstantinova I, Loren JC, Molteni V, Roberts S, Reilly J, Saunders AM, Stringer R, Sviridenko L, Thomas M, Thomson CG, Tomlins C, Wen B, Yeh V, Pearce AC.

J Med Chem. 2016 Sep 8;59(17):7901-14. doi: 10.1021/acs.jmedchem.6b00703. Epub 2016 Aug 19.


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.


Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.

Stauffer F, Cowan-Jacob SW, Scheufler C, Furet P.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2065-7. doi: 10.1016/j.bmcl.2016.02.074. Epub 2016 Feb 26.


Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.

Honda A, Harrington E, Cornella-Taracido I, Furet P, Knapp MS, Glick M, Triantafellow E, Dowdle WE, Wiedershain D, Maniara W, Moore C, Finan PM, Hamann LG, Firestone B, Murphy LO, Keaney EP.

ACS Med Chem Lett. 2015 Nov 13;7(1):72-6. doi: 10.1021/acsmedchemlett.5b00335. eCollection 2016 Jan 14.


A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.

Bold G, Schnell C, Furet P, McSheehy P, Brüggen J, Mestan J, Manley PW, Drückes P, Burglin M, Dürler U, Loretan J, Reuter R, Wartmann M, Theuer A, Bauer-Probst B, Martiny-Baron G, Allegrini P, Goepfert A, Wood J, Littlewood-Evans A.

J Med Chem. 2016 Jan 14;59(1):132-46. doi: 10.1021/acs.jmedchem.5b01582. Epub 2015 Dec 21.


Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Imbach-Weese P, Gerspacher M, Caravatti G, Furet P, Zoller T, Fritsch C, Haasen D, Trappe J, Guthy DA, Arz D, Wirth J.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3569-74. doi: 10.1016/j.bmcl.2015.06.078. Epub 2015 Jun 27.


Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Gerspacher M, Imbach-Weese P, Mah R, Caravatti G, Furet P, Fritsch C, Schnell C, Blanz J, Blasco F, Desrayaud S, Guthy DA, Knapp M, Arz D, Wirth J, Roehn-Carnemolla E, Luu VH.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3575-81. doi: 10.1016/j.bmcl.2015.06.067. Epub 2015 Jun 26.


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 a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.

Gerspacher M, Fairhurst RA, Mah R, Roehn-Carnemolla E, Furet P, Fritsch C, Guthy DA.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3582-4. doi: 10.1016/j.bmcl.2015.06.077. Epub 2015 Jun 30.


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.


Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.

Vaupel A, Bold G, De Pover A, Stachyra-Valat T, Lisztwan JH, Kallen J, Masuya K, Furet P.

Bioorg Med Chem Lett. 2014 May 1;24(9):2110-4. doi: 10.1016/j.bmcl.2014.03.039. Epub 2014 Mar 22. Erratum in: Bioorg Med Chem Lett. 2015 Mar 15;25(6):1356. Hergovich-Lisztwan, Joanna [corrected to Lisztwan, Joanna Hergovich].


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.


Light and nitrogen nutrition regulate apical control in Rosa hybrida L.

Furet PM, Lothier J, Demotes-Mainard S, Travier S, Henry C, Guérin V, Vian A.

J Plant Physiol. 2014 Mar 1;171(5):7-13. doi: 10.1016/j.jplph.2013.10.008. Epub 2013 Dec 11.


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.


Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R, Hamon J, Fabbro D, Caravatti G.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007. Epub 2013 May 14. Erratum in: Bioorg Med Chem Lett. 2013 Aug 15;23(16):4723.


Differential regulation of two sucrose transporters by defoliation and light conditions in perennial ryegrass.

Furet PM, Berthier A, Decau ML, Morvan-Bertrand A, Prud'homme MP, Noiraud-Romy N, Meuriot F.

Plant Physiol Biochem. 2012 Dec;61:88-96. doi: 10.1016/j.plaphy.2012.09.011. Epub 2012 Oct 3.


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.


New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.

Stauffer F, Furet P, Floersheimer A, Lang M.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1860-3. doi: 10.1016/j.bmcl.2012.01.076. Epub 2012 Jan 28.


Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H, Wartmann M, Berghausen J, Drueckes P, Zimmerlin A, Bussiere D, Murray J, Graus Porta D.

J Med Chem. 2011 Oct 27;54(20):7066-83. doi: 10.1021/jm2006222. Epub 2011 Sep 21.


Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison.

Weisberg E, Roesel J, Furet P, Bold G, Imbach P, Flörsheimer A, Caravatti G, Jiang J, Manley P, Ray A, Griffin JD.

Genes Cancer. 2010 Oct;1(10):1021-32. doi: 10.1177/1947601910396505.


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.


The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis.

Martiny-Baron G, Holzer P, Billy E, Schnell C, Brueggen J, Ferretti M, Schmiedeberg N, Wood JM, Furet P, Imbach P.

Angiogenesis. 2010 Sep;13(3):259-67. doi: 10.1007/s10456-010-9183-z. Epub 2010 Aug 29.


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.


New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.

Gommermann N, Buehlmayer P, von Matt A, Breitenstein W, Masuya K, Pirard B, Furet P, Cowan-Jacob SW, Weckbecker G.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3628-31. doi: 10.1016/j.bmcl.2010.04.112. Epub 2010 Apr 29.


Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay.

Jahnke W, Grotzfeld RM, Pellé X, Strauss A, Fendrich G, Cowan-Jacob SW, Cotesta S, Fabbro D, Furet P, Mestan J, Marzinzik AL.

J Am Chem Soc. 2010 May 26;132(20):7043-8. doi: 10.1021/ja101837n.


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.


Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.

Furet P, Gerspacher M, Pissot-Soldermann C.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1858-60. doi: 10.1016/j.bmcl.2010.01.151. Epub 2010 Feb 4.


Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.

Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J.

Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009.


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.


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