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126 results

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Page 1
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC.
Hayhow TG, Williamson B, Lawson M, Cureton N, Braybrooke EL, Campbell A, Carbajo RJ, Cheraghchi-Bashi A, Chiarparin E, Diène CR, Fallan C, Fisher DI, Goldberg FW, Hopcroft L, Hopcroft P, Jackson A, Kettle JG, Klinowska T, Künzel U, Lamont G, Lewis HJ, Maglennon G, Martin S, Gutierrez PM, Morrow CJ, Nikolaou M, Nissink JWM, O'Shea P, Polanski R, Schade M, Scott JS, Smith A, Weber J, Wilson J, Yang B, Crafter C. Hayhow TG, et al. Among authors: goldberg fw. Commun Biol. 2024 May 13;7(1):563. doi: 10.1038/s42003-024-06238-x. Commun Biol. 2024. PMID: 38740899 Free PMC article.
α-Functionalisation of Cyclic Sulfides Enabled by Lithiation Trapping.
Seling N, Atobe M, Kasten K, Firth JD, Karadakov PB, Goldberg FW, O'Brien P. Seling N, et al. Among authors: goldberg fw. Angew Chem Int Ed Engl. 2024 Jan 8;63(2):e202314423. doi: 10.1002/anie.202314423. Epub 2023 Dec 7. Angew Chem Int Ed Engl. 2024. PMID: 37984884 Free PMC article.
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: goldberg fw. 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 a series of novel, potent and selective Macrocyclic SYK inhibitors.
Grimster NP, Gingipalli L, Balazs A, Barlaam B, Boiko S, Boyd S, Dry H, Goldberg FW, Ikeda T, Johnson T, Kawatkar S, Kemmitt P, Lamont S, Lorthioir O, Mfuh A, Patel J, Pike A, Read J, Romero R, Sarkar U, Sha L, Simpson I, Song K, Su Q, Wang H, Watson D, Wu A, Zehnder TE, Zheng X, Li S, Dong Z, Yang D, Song Y, Wang P, Liu X, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: goldberg fw. Bioorg Med Chem Lett. 2023 Jul 15;91:129352. doi: 10.1016/j.bmcl.2023.129352. Epub 2023 Jun 2. Bioorg Med Chem Lett. 2023. PMID: 37270074
Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8H-purin-8-one Inhibitors of DNA-PK.
Goldberg FW, Ting AKT, Beattie D, Lamont GM, Fallan C, Finlay MRV, Williamson B, Schimpl M, Harmer AR, Adeyemi OB, Nordell P, Cronin AS, Vazquez-Chantada M, Barratt D, Ramos-Montoya A, Cadogan EB, Davies BR. Goldberg FW, et al. ACS Med Chem Lett. 2022 Jul 7;13(8):1295-1301. doi: 10.1021/acsmedchemlett.2c00172. eCollection 2022 Aug 11. ACS Med Chem Lett. 2022. PMID: 35978693 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: goldberg fw. 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
Direct targeting of FOXP3 in Tregs with AZD8701, a novel antisense oligonucleotide to relieve immunosuppression in cancer.
Revenko A, Carnevalli LS, Sinclair C, Johnson B, Peter A, Taylor M, Hettrick L, Chapman M, Klein S, Solanki A, Gattis D, Watt A, Hughes AM, Magiera L, Kar G, Ireland L, Mele DA, Sah V, Singh M, Walton J, Mairesse M, King M, Edbrooke M, Lyne P, Barry ST, Fawell S, Goldberg FW, MacLeod AR. Revenko A, et al. Among authors: goldberg fw. J Immunother Cancer. 2022 Apr;10(4):e003892. doi: 10.1136/jitc-2021-003892. J Immunother Cancer. 2022. PMID: 35387780 Free PMC article. Clinical Trial.
126 results