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Page 1
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: ramos montoya a. 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.
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. 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
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. Nat Commun. 2019 Nov 7;10(1):5065. doi: 10.1038/s41467-019-12836-9. Nat Commun. 2019. PMID: 31699977 Free PMC article.
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: ramos montoya a. 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.
The DNA-PK Inhibitor AZD7648 Sensitizes Patient-Derived Ovarian Cancer Xenografts to Pegylated Liposomal Doxorubicin and Olaparib Preventing Abdominal Metastases.
Anastasia A, Dellavedova G, Ramos-Montoya A, James N, Chiorino G, Russo M, Baakza H, Wilson J, Ghilardi C, Cadogan EB, Giavazzi R, Bani MR. Anastasia A, et al. Among authors: ramos montoya a. Mol Cancer Ther. 2022 Apr 1;21(4):555-567. doi: 10.1158/1535-7163.MCT-21-0420. Mol Cancer Ther. 2022. PMID: 35149547
pRAD50: a novel and clinically applicable pharmacodynamic biomarker of both ATM and ATR inhibition identified using mass spectrometry and immunohistochemistry.
Jones GN, Rooney C, Griffin N, Roudier M, Young LA, Garcia-Trinidad A, Hughes GD, Whiteaker JR, Wilson Z, Odedra R, Zhao L, Ivey RG, Howat WJ, Harrington EA, Barrett JC, Ramos-Montoya A, Lau A, Paulovich AG, Cadogan EB, Pierce AJ. Jones GN, et al. Br J Cancer. 2018 Nov;119(10):1233-1243. doi: 10.1038/s41416-018-0286-4. Epub 2018 Nov 2. Br J Cancer. 2018. PMID: 30385821 Free PMC article.
Macrophage Activation Status Rather than Repolarization Is Associated with Enhanced Checkpoint Activity in Combination with PI3Kγ Inhibition.
Carnevalli LS, Taylor MA, King M, Coenen-Stass AML, Hughes AM, Bell S, Proia TA, Wang Y, Ramos-Montoya A, Wali N, Carroll D, Singh M, Moschetta M, Gutierrez PM, Gardelli C, Critchlow SE, Klinowska T, Fawell SE, Barry ST. Carnevalli LS, et al. Among authors: ramos montoya a. Mol Cancer Ther. 2021 Jun;20(6):1080-1091. doi: 10.1158/1535-7163.MCT-20-0961. Epub 2021 Mar 30. Mol Cancer Ther. 2021. PMID: 33785652
HES6 drives a critical AR transcriptional programme to induce castration-resistant prostate cancer through activation of an E2F1-mediated cell cycle network.
Ramos-Montoya A, Lamb AD, Russell R, Carroll T, Jurmeister S, Galeano-Dalmau N, Massie CE, Boren J, Bon H, Theodorou V, Vias M, Shaw GL, Sharma NL, Ross-Adams H, Scott HE, Vowler SL, Howat WJ, Warren AY, Wooster RF, Mills IG, Neal DE. Ramos-Montoya A, et al. EMBO Mol Med. 2014 May;6(5):651-61. doi: 10.1002/emmm.201303581. EMBO Mol Med. 2014. PMID: 24737870 Free PMC article.
41 results