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Page 1
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Weiss A, Lorthiois E, Barys L, Beyer KS, Bomio-Confaglia C, Burks H, Chen X, Cui X, de Kanter R, Dharmarajan L, Fedele C, Gerspacher M, Guthy DA, Head V, Jaeger A, Núñez EJ, Kearns JD, Leblanc C, Maira SM, Murphy J, Oakman H, Ostermann N, Ottl J, Rigollier P, Roman D, Schnell C, Sedrani R, Shimizu T, Stringer R, Vaupel A, Voshol H, Wessels P, Widmer T, Wilcken R, Xu K, Zecri F, Farago AF, Cotesta S, Brachmann SM. Weiss A, et al. Among authors: guthy da. Cancer Discov. 2022 Jun 2;12(6):1500-1517. doi: 10.1158/2159-8290.CD-22-0158. Cancer Discov. 2022. PMID: 35404998 Free PMC article.
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. Maira SM, et al. Mol Cancer Ther. 2012 Feb;11(2):317-28. doi: 10.1158/1535-7163.MCT-11-0474. Epub 2011 Dec 21. Mol Cancer Ther. 2012. PMID: 22188813
Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations.
Brachmann SM, Kleylein-Sohn J, Gaulis S, Kauffmann A, Blommers MJ, Kazic-Legueux M, Laborde L, Hattenberger M, Stauffer F, Vaxelaire J, Romanet V, Henry C, Murakami M, Guthy DA, Sterker D, Bergling S, Wilson C, Brümmendorf T, Fritsch C, Garcia-Echeverria C, Sellers WR, Hofmann F, Maira SM. Brachmann SM, et al. Among authors: guthy da. Mol Cancer Ther. 2012 Aug;11(8):1747-57. doi: 10.1158/1535-7163.MCT-11-1021. Epub 2012 May 31. Mol Cancer Ther. 2012. PMID: 22653967
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. 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
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. Jeay S, et al. Among authors: guthy da. Elife. 2015 May 12;4:e06498. doi: 10.7554/eLife.06498. Elife. 2015. PMID: 25965177 Free PMC article.
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. Gerspacher M, et al. Among authors: 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. Bioorg Med Chem Lett. 2015. PMID: 26164189
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: guthy da. 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
Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition.
Herkert B, Kauffmann A, Mollé S, Schnell C, Ferrat T, Voshol H, Juengert J, Erasimus H, Marszalek G, Kazic-Legueux M, Billy E, Ruddy D, Stump M, Guthy D, Ristov M, Calkins K, Maira SM, Sellers WR, Hofmann F, Hall MN, Brachmann SM. Herkert B, et al. Cancer Res. 2016 Jan 15;76(2):390-402. doi: 10.1158/0008-5472.CAN-14-3358. Epub 2015 Nov 17. Cancer Res. 2016. PMID: 26577700
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C. Chen C, et al. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563395 Free PMC article.
20 results