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Page 1
Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
Michaelides IN, Collie GW, Börjesson U, Vasalou C, Alkhatib O, Barlind L, Cheung T, Dale IL, Embrey KJ, Hennessy EJ, Khurana P, Koh CM, Lamb ML, Liu J, Moss TA, O'Neill DJ, Phillips C, Shaw J, Snijder A, Storer RI, Stubbs CJ, Han F, Li C, Qiao J, Sun DQ, Wang J, Wang P, Yang W. Michaelides IN, et al. Among authors: phillips c. J Med Chem. 2023 Jul 13;66(13):8782-8807. doi: 10.1021/acs.jmedchem.3c00401. Epub 2023 Jun 21. J Med Chem. 2023. PMID: 37343272 Free PMC article.
KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe.
Bery N, Legg S, Debreczeni J, Breed J, Embrey K, Stubbs C, Kolasinska-Zwierz P, Barrett N, Marwood R, Watson J, Tart J, Overman R, Miller A, Phillips C, Minter R, Rabbitts TH. Bery N, et al. Among authors: phillips c. Nat Commun. 2019 Jun 13;10(1):2607. doi: 10.1038/s41467-019-10419-2. Nat Commun. 2019. PMID: 31197133 Free PMC article.
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.
Collie GW, Koh CM, O'Neill DJ, Stubbs CJ, Khurana P, Eddershaw A, Snijder A, Mauritzson F, Barlind L, Dale IL, Shaw J, Phillips C, Hennessy EJ, Cheung T, Narvaez AJ. Collie GW, et al. Among authors: phillips c. ACS Med Chem Lett. 2019 Aug 2;10(9):1322-1327. doi: 10.1021/acsmedchemlett.9b00276. eCollection 2019 Sep 12. ACS Med Chem Lett. 2019. PMID: 31531204 Free PMC article.
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X. Kettle JG, et al. Among authors: phillips c. J Med Chem. 2020 May 14;63(9):4468-4483. doi: 10.1021/acs.jmedchem.9b01720. Epub 2020 Feb 13. J Med Chem. 2020. PMID: 32023060
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Collie GW, Michaelides IN, Embrey K, Stubbs CJ, Börjesson U, Dale IL, Snijder A, Barlind L, Song K, Khurana P, Phillips C, Storer RI. Collie GW, et al. Among authors: phillips c. ACS Med Chem Lett. 2020 Dec 8;12(1):162-167. doi: 10.1021/acsmedchemlett.0c00392. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488978 Free PMC article.
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Boyd S, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Davies NL, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Hanson L, Harlfinger S, Howard M, Howells R, Jackson A, Kemmitt P, Lamont G, Lamont S, Lewis HJ, Liu L, Niedbala MJ, Phillips C, Polanski R, Raubo P, Robb G, Robinson DM, Ross S, Sanders MG, Tonge M, Whiteley R, Wilkinson S, Yang J, Zhang W. Kettle JG, et al. Among authors: phillips c. J Med Chem. 2022 May 12;65(9):6940-6952. doi: 10.1021/acs.jmedchem.2c00369. Epub 2022 Apr 26. J Med Chem. 2022. PMID: 35471939
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.
Kettle JG, Bagal SK, Barratt D, Bodnarchuk MS, Boyd S, Braybrooke E, Breed J, Cassar DJ, Cosulich S, Davies M, Davies NL, Deng C, Eatherton A, Evans L, Feron LJ, Fillery S, Gleave ES, Goldberg FW, Cortés González MA, Guerot C, Haider A, Harlfinger S, Howells R, Jackson A, Johnström P, Kemmitt PD, Koers A, Kondrashov M, Lamont GM, Lamont S, Lewis HJ, Liu L, Mylrea M, Nash S, Niedbala MJ, Peter A, Phillips C, Pike K, Raubo P, Robb GR, Ross S, Sanders MG, Schou M, Simpson I, Steward O. Kettle JG, et al. Among authors: phillips c. J Med Chem. 2023 Jul 13;66(13):9147-9160. doi: 10.1021/acs.jmedchem.3c00746. Epub 2023 Jul 3. J Med Chem. 2023. PMID: 37395055
Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders.
Lucas SCC, Ahmed A, Ashraf SN, Argyrou A, Bauer MR, De Donatis GM, Demanze S, Eisele F, Fusani L, Hock A, Kadamur G, Li S, Macmillan-Jones A, Michaelides IN, Phillips C, Rehnström M, Richter M, Rodrigo-Brenni MC, Shilliday F, Wang P, Storer RI. Lucas SCC, et al. Among authors: phillips c. J Med Chem. 2024 Apr 11;67(7):5538-5566. doi: 10.1021/acs.jmedchem.3c02136. Epub 2024 Mar 21. J Med Chem. 2024. PMID: 38513086
Structural insights and activating mutations in diverse pathologies define mechanisms of deregulation for phospholipase C gamma enzymes.
Liu Y, Bunney TD, Khosa S, Macé K, Beckenbauer K, Askwith T, Maslen S, Stubbs C, de Oliveira TM, Sader K, Skehel M, Gavin AC, Phillips C, Katan M. Liu Y, et al. Among authors: phillips c. EBioMedicine. 2020 Jan;51:102607. doi: 10.1016/j.ebiom.2019.102607. Epub 2020 Jan 6. EBioMedicine. 2020. PMID: 31918402 Free PMC article.
4,311 results