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Structural and mechanistic insights into the inhibition of respiratory syncytial virus polymerase by a non-nucleoside inhibitor.
Yu X, Abeywickrema P, Bonneux B, Behera I, Anson B, Jacoby E, Fung A, Adhikary S, Bhaumik A, Carbajo RJ, De Bruyn S, Miller R, Patrick A, Pham Q, Piassek M, Verheyen N, Shareef A, Sutto-Ortiz P, Ysebaert N, Van Vlijmen H, Jonckers THM, Herschke F, McLellan JS, Decroly E, Fearns R, Grosse S, Roymans D, Sharma S, Rigaux P, Jin Z. Yu X, et al. Among authors: carbajo rj. Commun Biol. 2023 Oct 21;6(1):1074. doi: 10.1038/s42003-023-05451-4. Commun Biol. 2023. PMID: 37865687 Free PMC article.
Structure of human spermine oxidase in complex with a highly selective allosteric inhibitor.
Diaz E, Adhikary S, Tepper AWJW, Riley D, Ortiz-Meoz R, Krosky D, Buyck C, Lamenca CM, Llaveria J, Fang L, Kalin JH, Klaren VNA, Fahmy S, Shaffer PL, Kirkpatrick R, Carbajo RJ, Thomsen M, Impagliazzo A. Diaz E, et al. Among authors: carbajo rj. Commun Biol. 2022 Aug 5;5(1):787. doi: 10.1038/s42003-022-03735-9. Commun Biol. 2022. PMID: 35931745 Free PMC article.
Design of rigid protein-protein interaction inhibitors enables targeting of undruggable Mcl-1.
Hargreaves D, Carbajo RJ, Bodnarchuk MS, Embrey K, Rawlins PB, Packer M, Degorce SL, Hird AW, Johannes JW, Chiarparin E, Schade M. Hargreaves D, et al. Among authors: carbajo rj. Proc Natl Acad Sci U S A. 2023 May 23;120(21):e2221967120. doi: 10.1073/pnas.2221967120. Epub 2023 May 15. Proc Natl Acad Sci U S A. 2023. PMID: 37186857 Free PMC article.
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: carbajo rj. Commun Biol. 2024 May 13;7(1):563. doi: 10.1038/s42003-024-06238-x. Commun Biol. 2024. PMID: 38740899
Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. Among authors: carbajo rj. J Med Chem. 2023 Feb 23;66(4):2918-2945. doi: 10.1021/acs.jmedchem.2c01964. Epub 2023 Feb 1. J Med Chem. 2023. PMID: 36727211
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: carbajo rj. 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
66 results