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Items: 16

1.

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 May 8. doi: 10.1002/cmdc.201900201. [Epub ahead of print]

PMID:
31066983
2.

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
3.

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Caravatti G, Guagnano V, Aichholz R, Blanz J, Blasco F, Wipfli P, Fritsch C, Maira SM, Schnell C, Seiler FH.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4729-4734. doi: 10.1016/j.bmcl.2016.08.041. Epub 2016 Aug 17.

PMID:
27575470
4.

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
5.

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
6.

Fibroblast growth factor receptors as novel therapeutic targets in SNF5-deleted malignant rhabdoid tumors.

Wöhrle S, Weiss A, Ito M, Kauffmann A, Murakami M, Jagani Z, Thuery A, Bauer-Probst B, Reimann F, Stamm C, Pornon A, Romanet V, Guagnano V, Brümmendorf T, Sellers WR, Hofmann F, Roberts CW, Graus Porta D.

PLoS One. 2013 Oct 30;8(10):e77652. doi: 10.1371/journal.pone.0077652. eCollection 2013.

7.

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.

PMID:
23726034
8.

Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets.

Wöhrle S, Henninger C, Bonny O, Thuery A, Beluch N, Hynes NE, Guagnano V, Sellers WR, Hofmann F, Kneissel M, Graus Porta D.

J Bone Miner Res. 2013 Apr;28(4):899-911. doi: 10.1002/jbmr.1810.

9.

FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor.

Guagnano V, Kauffmann A, Wöhrle S, Stamm C, Ito M, Barys L, Pornon A, Yao Y, Li F, Zhang Y, Chen Z, Wilson CJ, Bordas V, Le Douget M, Gaither LA, Borawski J, Monahan JE, Venkatesan K, Brümmendorf T, Thomas DM, Garcia-Echeverria C, Hofmann F, Sellers WR, Graus-Porta D.

Cancer Discov. 2012 Dec;2(12):1118-33. doi: 10.1158/2159-8290.CD-12-0210. Epub 2012 Sep 20.

10.

Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth.

Harbinski F, Craig VJ, Sanghavi S, Jeffery D, Liu L, Sheppard KA, Wagner S, Stamm C, Buness A, Chatenay-Rivauday C, Yao Y, He F, Lu CX, Guagnano V, Metz T, Finan PM, Hofmann F, Sellers WR, Porter JA, Myer VE, Graus-Porta D, Wilson CJ, Buckler A, Tiedt R.

Cancer Discov. 2012 Oct;2(10):948-59. doi: 10.1158/2159-8290.CD-12-0237. Epub 2012 Aug 8.

11.

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.

PMID:
21936542
12.

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Furet P, Caravatti G, Guagnano V, Lang M, Meyer T, Schoepfer J.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.

PMID:
18248988
13.

Novel beta-lactam derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome.

Imbach P, Lang M, García-Echeverría C, Guagnano V, Noorani M, Roesel J, Bitsch F, Rihs G, Furet P.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):358-62. Epub 2006 Oct 24.

PMID:
17095212
15.

Entry into a new class of potent proteasome inhibitors having high antiproliferative activity by structure-based design.

Furet P, Imbach P, Noorani M, Koeppler J, Laumen K, Lang M, Guagnano V, Fuerst P, Roesel J, Zimmermann J, García-Echeverría C.

J Med Chem. 2004 Sep 23;47(20):4810-3.

PMID:
15369383
16.

Synthesis and biological evaluation of highly potent analogues of epothilones B and D.

Altmann KH, Bold G, Caravatti G, Flörsheimer A, Guagnano V, Wartmann M.

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2765-8.

PMID:
11133086

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