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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: zecri f. 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.
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.
Hoegenauer K, Soldermann N, Hebach C, Hollingworth GJ, Lewis I, von Matt A, Smith AB, Wolf RM, Wilcken R, Haasen D, Burkhart C, Zécri F. Hoegenauer K, et al. Among authors: zecri f. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5657-5662. doi: 10.1016/j.bmcl.2016.10.069. Epub 2016 Oct 27. Bioorg Med Chem Lett. 2016. PMID: 27816514
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. Lorthiois E, et al. Among authors: zecri fj. J Med Chem. 2022 Dec 22;65(24):16173-16203. doi: 10.1021/acs.jmedchem.2c01438. Epub 2022 Nov 18. J Med Chem. 2022. PMID: 36399068
Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers.
Ferretti S, Hamon J, de Kanter R, Scheufler C, Andraos-Rey R, Barbe S, Bechter E, Blank J, Bordas V, Dammassa E, Decker A, Di Nanni N, Dourdoigne M, Gavioli E, Hattenberger M, Heuser A, Hemmerlin C, Hinrichs J, Kerr G, Laborde L, Jaco I, Núñez EJ, Martus HJ, Quadt C, Reschke M, Romanet V, Schaeffer F, Schoepfer J, Schrapp M, Strang R, Voshol H, Wartmann M, Welly S, Zécri F, Hofmann F, Möbitz H, Cortés-Cros M. Ferretti S, et al. Among authors: zecri f. Nature. 2024 May;629(8011):443-449. doi: 10.1038/s41586-024-07350-y. Epub 2024 Apr 24. Nature. 2024. PMID: 38658754 Free PMC article.
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C. Hoegenauer K, et al. Among authors: zecri f. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14. ACS Med Chem Lett. 2017. PMID: 28947947 Free PMC article.
Diversity-oriented synthesis encoded by deoxyoligonucleotides.
Hudson L, Mason JW, Westphal MV, Richter MJR, Thielman JR, Hua BK, Gerry CJ, Xia G, Osswald HL, Knapp JM, Tan ZY, Kokkonda P, Tresco BIC, Liu S, Reidenbach AG, Lim KS, Poirier J, Capece J, Bonazzi S, Gampe CM, Smith NJ, Bradner JE, Coley CW, Clemons PA, Melillo B, Hon CS, Ottl J, Dumelin CE, Schaefer JV, Faust AME, Berst F, Schreiber SL, Zécri FJ, Briner K. Hudson L, et al. Among authors: zecri fj. Nat Commun. 2023 Aug 15;14(1):4930. doi: 10.1038/s41467-023-40575-5. Nat Commun. 2023. PMID: 37582753 Free PMC article.
Author Correction: Diversity-oriented synthesis encoded by deoxyoligonucleotides.
Hudson L, Mason JW, Westphal MV, Richter MJR, Thielman JR, Hua BK, Gerry CJ, Xia G, Osswald HL, Knapp JM, Tan ZY, Kokkonda P, Tresco BIC, Liu S, Reidenbach AG, Lim KS, Poirier J, Capece J, Bonazzi S, Gampe CM, Smith NJ, Bradner JE, Coley CW, Clemons PA, Melillo B, Hon CS, Ottl J, Dumelin CE, Schaefer JV, Faust AME, Berst F, Schreiber SL, Zécri FJ, Briner K. Hudson L, et al. Among authors: zecri fj. Nat Commun. 2023 Nov 21;14(1):7589. doi: 10.1038/s41467-023-43518-2. Nat Commun. 2023. PMID: 37989745 Free PMC article. 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. Hoegenauer K, et al. Among authors: zecri f. ACS Med Chem Lett. 2016 Jun 2;7(8):762-7. doi: 10.1021/acsmedchemlett.6b00119. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563400 Free PMC article.
Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor.
Harrison TJ, Bauer D, Berdichevsky A, Chen X, Duvadie R, Hoogheem B, Hatsis P, Liu Q, Mao J, Miduturu V, Rocheford E, Zecri F, Zessis R, Zheng R, Zhu Q, Streeper R, Patel SJ. Harrison TJ, et al. Among authors: zecri f. ACS Med Chem Lett. 2019 Jun 20;10(8):1128-1133. doi: 10.1021/acsmedchemlett.9b00117. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413796 Free PMC article.
Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy.
Bonazzi S, d'Hennezel E, Beckwith REJ, Xu L, Fazal A, Magracheva A, Ramesh R, Cernijenko A, Antonakos B, Bhang HC, Caro RG, Cobb JS, Ornelas E, Ma X, Wartchow CA, Clifton MC, Forseth RR, Fortnam BH, Lu H, Csibi A, Tullai J, Carbonneau S, Thomsen NM, Larrow J, Chie-Leon B, Hainzl D, Gu Y, Lu D, Meyer MJ, Alexander D, Kinyamu-Akunda J, Sabatos-Peyton CA, Dales NA, Zécri FJ, Jain RK, Shulok J, Wang YK, Briner K, Porter JA, Tallarico JA, Engelman JA, Dranoff G, Bradner JE, Visser M, Solomon JM. Bonazzi S, et al. Among authors: zecri fj. Cell Chem Biol. 2023 Mar 16;30(3):235-247.e12. doi: 10.1016/j.chembiol.2023.02.005. Epub 2023 Mar 1. Cell Chem Biol. 2023. PMID: 36863346 Free article.
31 results