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Page 1
Simultaneous inhibition of DNA-PK and Polϴ improves integration efficiency and precision of genome editing.
Wimberger S, Akrap N, Firth M, Brengdahl J, Engberg S, Schwinn MK, Slater MR, Lundin A, Hsieh PP, Li S, Cerboni S, Sumner J, Bestas B, Schiffthaler B, Magnusson B, Di Castro S, Iyer P, Bohlooly-Y M, Machleidt T, Rees S, Engkvist O, Norris T, Cadogan EB, Forment JV, Šviković S, Akcakaya P, Taheri-Ghahfarokhi A, Maresca M. Wimberger S, et al. Among authors: cadogan eb. Nat Commun. 2023 Aug 14;14(1):4761. doi: 10.1038/s41467-023-40344-4. Nat Commun. 2023. PMID: 37580318 Free PMC article.
AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity.
Fok JHL, Ramos-Montoya A, Vazquez-Chantada M, Wijnhoven PWG, Follia V, James N, Farrington PM, Karmokar A, Willis SE, Cairns J, Nikkilä J, Beattie D, Lamont GM, Finlay MRV, Wilson J, Smith A, O'Connor LO, Ling S, Fawell SE, O'Connor MJ, Hollingsworth SJ, Dean E, Goldberg FW, Davies BR, Cadogan EB. Fok JHL, et al. Among authors: cadogan eb. Nat Commun. 2019 Nov 7;10(1):5065. doi: 10.1038/s41467-019-12836-9. Nat Commun. 2019. PMID: 31699977 Free PMC article.
The ATR inhibitor ceralasertib potentiates cancer checkpoint immunotherapy by regulating the tumor microenvironment.
Hardaker EL, Sanseviero E, Karmokar A, Taylor D, Milo M, Michaloglou C, Hughes A, Mai M, King M, Solanki A, Magiera L, Miragaia R, Kar G, Standifer N, Surace M, Gill S, Peter A, Talbot S, Tohumeken S, Fryer H, Mostafa A, Mulgrew K, Lam C, Hoffmann S, Sutton D, Carnevalli L, Calero-Nieto FJ, Jones GN, Pierce AJ, Wilson Z, Campbell D, Nyoni L, Martins CP, Baker T, Serrano de Almeida G, Ramlaoui Z, Bidar A, Phillips B, Boland J, Iyer S, Barrett JC, Loembé AB, Fuchs SY, Duvvuri U, Lou PJ, Nance MA, Gomez Roca CA, Cadogan E, Critichlow SE, Fawell S, Cobbold M, Dean E, Valge-Archer V, Lau A, Gabrilovich DI, Barry ST. Hardaker EL, et al. Nat Commun. 2024 Feb 24;15(1):1700. doi: 10.1038/s41467-024-45996-4. Nat Commun. 2024. PMID: 38402224 Free PMC article.
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor.
Goldberg FW, Finlay MRV, Ting AKT, Beattie D, Lamont GM, Fallan C, Wrigley GL, Schimpl M, Howard MR, Williamson B, Vazquez-Chantada M, Barratt DG, Davies BR, Cadogan EB, Ramos-Montoya A, Dean E. Goldberg FW, et al. Among authors: cadogan eb. J Med Chem. 2020 Apr 9;63(7):3461-3471. doi: 10.1021/acs.jmedchem.9b01684. Epub 2020 Jan 15. J Med Chem. 2020. PMID: 31851518
Inhibition of DNA-PK with AZD7648 Sensitizes Tumor Cells to Radiotherapy and Induces Type I IFN-Dependent Durable Tumor Control.
Nakamura K, Karmokar A, Farrington PM, James NH, Ramos-Montoya A, Bickerton SJ, Hughes GD, Illidge TM, Cadogan EB, Davies BR, Dovedi SJ, Valge-Archer V. Nakamura K, et al. Among authors: cadogan eb. Clin Cancer Res. 2021 Aug 1;27(15):4353-4366. doi: 10.1158/1078-0432.CCR-20-3701. Epub 2021 May 19. Clin Cancer Res. 2021. PMID: 34011558 Free PMC article.
Identification of a Molecularly-Defined Subset of Breast and Ovarian Cancer Models that Respond to WEE1 or ATR Inhibition, Overcoming PARP Inhibitor Resistance.
Serra V, Wang AT, Castroviejo-Bermejo M, Polanska UM, Palafox M, Herencia-Ropero A, Jones GN, Lai Z, Armenia J, Michopoulos F, Llop-Guevara A, Brough R, Gulati A, Pettitt SJ, Bulusu KC, Nikkilä J, Wilson Z, Hughes A, Wijnhoven PWG, Ahmed A, Bruna A, Gris-Oliver A, Guzman M, Rodríguez O, Grueso J, Arribas J, Cortés J, Saura C, Lau A, Critchlow S, Dougherty B, Caldas C, Mills GB, Barrett JC, Forment JV, Cadogan E, Lord CJ, Cruz C, Balmaña J, O'Connor MJ. Serra V, et al. Clin Cancer Res. 2022 Oct 14;28(20):4536-4550. doi: 10.1158/1078-0432.CCR-22-0568. Clin Cancer Res. 2022. PMID: 35921524 Free PMC article.
A microfluidic system that replicates pharmacokinetic (PK) profiles in vitro improves prediction of in vivo efficacy in preclinical models.
Singh D, Deosarkar SP, Cadogan E, Flemington V, Bray A, Zhang J, Reiserer RS, Schaffer DK, Gerken GB, Britt CM, Werner EM, Gibbons FD, Kostrzewski T, Chambers CE, Davies EJ, Montoya AR, Fok JHL, Hughes D, Fabre K, Wagoner MP, Wikswo JP, Scott CW. Singh D, et al. PLoS Biol. 2022 May 26;20(5):e3001624. doi: 10.1371/journal.pbio.3001624. eCollection 2022 May. PLoS Biol. 2022. PMID: 35617197 Free PMC article.
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. Among authors: cadogan eb. 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.
27 results