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Page 1
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. Among authors: guthy d. 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.
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: guthy d. 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.
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. Among authors: guthy d. 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
New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse.
Stauffer F, Weiss A, Scheufler C, Möbitz H, Ragot C, Beyer KS, Calkins K, Guthy D, Kiffe M, Van Eerdenbrugh B, Tiedt R, Gaul C. Stauffer F, et al. Among authors: guthy d. ACS Med Chem Lett. 2019 Dec 4;10(12):1655-1660. doi: 10.1021/acsmedchemlett.9b00452. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857842 Free PMC article.
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 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: guthy da. 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
20 results