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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. Fritsch C, et al. Among authors: caravatti g. Mol Cancer Ther. 2014 May;13(5):1117-29. doi: 10.1158/1535-7163.MCT-13-0865. Epub 2014 Mar 7. Mol Cancer Ther. 2014. PMID: 24608574
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. Fairhurst RA, et al. Among authors: caravatti g. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3575-81. doi: 10.1016/j.bmcl.2015.06.067. Epub 2015 Jun 26. Bioorg Med Chem Lett. 2015. PMID: 26199119
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. Fairhurst RA, et al. Among authors: caravatti g. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4729-4734. doi: 10.1016/j.bmcl.2016.08.041. Epub 2016 Aug 17. Bioorg Med Chem Lett. 2016. PMID: 27575470
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Fairhurst RA, Furet P, Imbach-Weese P, Stauffer F, Rueeger H, McCarthy C, Ripoche S, Oswald S, Arnaud B, Jary A, Maira M, Schnell C, Guthy DA, Wartmann M, Kiffe M, Desrayaud S, Blasco F, Widmer T, Seiler F, Gutmann S, Knapp M, Caravatti G. Fairhurst RA, et al. Among authors: caravatti g. J Med Chem. 2022 Jun 23;65(12):8345-8379. doi: 10.1021/acs.jmedchem.2c00267. Epub 2022 May 2. J Med Chem. 2022. PMID: 35500094
AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.
Traxler P, Allegrini PR, Brandt R, Brueggen J, Cozens R, Fabbro D, Grosios K, Lane HA, McSheehy P, Mestan J, Meyer T, Tang C, Wartmann M, Wood J, Caravatti G. Traxler P, et al. Among authors: caravatti g. Cancer Res. 2004 Jul 15;64(14):4931-41. doi: 10.1158/0008-5472.CAN-03-3681. Cancer Res. 2004. PMID: 15256466
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. Fabbro D, et al. Among authors: caravatti g. Pharmacol Ther. 2002 Feb-Mar;93(2-3):79-98. doi: 10.1016/s0163-7258(02)00179-1. Pharmacol Ther. 2002. PMID: 12191602 Review.
Selective GRB2 SH2 inhibitors as anti-Ras therapy.
Gay B, Suarez S, Caravatti G, Furet P, Meyer T, Schoepfer J. Gay B, et al. Among authors: caravatti g. Int J Cancer. 1999 Oct 8;83(2):235-41. doi: 10.1002/(sici)1097-0215(19991008)83:2<235::aid-ijc15>3.0.co;2-b. Int J Cancer. 1999. PMID: 10471533 Free article.
44 results