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Preclinical Characterization of AZD9574, a Blood-Brain Barrier Penetrant Inhibitor of PARP1.
Staniszewska AD, Pilger D, Gill SJ, Jamal K, Bohin N, Guzzetti S, Gordon J, Hamm G, Mundin G, Illuzzi G, Pike A, McWilliams L, Maglennon G, Rose J, Hawthorne G, Cortes Gonzalez M, Halldin C, Johnström P, Schou M, Critchlow SE, Fawell S, Johannes JW, Leo E, Davies BR, Cosulich S, Sarkaria JN, O'Connor MJ, Hamerlik P. Staniszewska AD, et al. Among authors: leo e. Clin Cancer Res. 2024 Apr 1;30(7):1338-1351. doi: 10.1158/1078-0432.CCR-23-2094. Clin Cancer Res. 2024. PMID: 37967136
Preclinical Characterization of AZD5305, A Next-Generation, Highly Selective PARP1 Inhibitor and Trapper.
Illuzzi G, Staniszewska AD, Gill SJ, Pike A, McWilliams L, Critchlow SE, Cronin A, Fawell S, Hawthorne G, Jamal K, Johannes J, Leonard E, Macdonald R, Maglennon G, Nikkilä J, O'Connor MJ, Smith A, Southgate H, Wilson J, Yates J, Cosulich S, Leo E. Illuzzi G, et al. Among authors: leo e. Clin Cancer Res. 2022 Nov 1;28(21):4724-4736. doi: 10.1158/1078-0432.CCR-22-0301. Clin Cancer Res. 2022. PMID: 35929986 Free PMC article.
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: leo e. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Design and Preclinical Evaluation of a Novel B7-H4-Directed Antibody-Drug Conjugate, AZD8205, Alone and in Combination with the PARP1-Selective Inhibitor AZD5305.
Kinneer K, Wortmann P, Cooper ZA, Dickinson NJ, Masterson L, Cailleau T, Hutchinson I, Vijayakrishnan B, McFarlane M, Ball K, Davies M, Lewis A, Huang Y, Rosenbaum AI, Yuan J, Chesebrough J, Anderton J, Monks N, Novick S, Wang J, Dimasi N, Christie RJ, Sabol D, Tosto FA, Wallez Y, Leo E, Albertella MR, Staniszewska AD, Tice DA, Howard PW, Luheshi N, Sapra P. Kinneer K, et al. Among authors: leo e. Clin Cancer Res. 2023 Mar 14;29(6):1086-1101. doi: 10.1158/1078-0432.CCR-22-2630. Clin Cancer Res. 2023. PMID: 36355054
Drug-gene Interaction Screens Coupled to Tumor Data Analyses Identify the Most Clinically Relevant Cancer Vulnerabilities Driving Sensitivity to PARP Inhibition.
Jamal K, Galbiati A, Armenia J, Illuzzi G, Hall J, Bentouati S, Barrell D, Ahdesmäki M; Functional Genomics Centre Group; O'Connor MJ, Leo E, Forment JV. Jamal K, et al. Among authors: leo e. Cancer Res Commun. 2022 Oct 21;2(10):1244-1254. doi: 10.1158/2767-9764.CRC-22-0119. eCollection 2022 Oct. Cancer Res Commun. 2022. PMID: 36969741 Free PMC article.
The PARP1 Inhibitor AZD5305 Impairs Ovarian Adenocarcinoma Progression and Visceral Metastases in Patient-derived Xenografts Alone and in Combination with Carboplatin.
Dellavedova G, Decio A, Formenti L, Albertella MR, Wilson J, Staniszewska AD, Leo E, Giavazzi R, Ghilardi C, Bani MR. Dellavedova G, et al. Among authors: leo e. Cancer Res Commun. 2023 Mar 27;3(3):489-500. doi: 10.1158/2767-9764.CRC-22-0423. eCollection 2023 Mar. Cancer Res Commun. 2023. PMID: 36994441 Free PMC article.
PARP inhibition is a modulator of anti-tumor immune response in BRCA-deficient tumors.
Staniszewska AD, Armenia J, King M, Michaloglou C, Reddy A, Singh M, San Martin M, Prickett L, Wilson Z, Proia T, Russell D, Thomas M, Delpuech O, O'Connor MJ, Leo E, Angell H, Valge-Archer V. Staniszewska AD, et al. Among authors: leo e. Oncoimmunology. 2022 Jun 18;11(1):2083755. doi: 10.1080/2162402X.2022.2083755. eCollection 2022. Oncoimmunology. 2022. PMID: 35756843 Free PMC article.
Rapid activation of epithelial-mesenchymal transition drives PARP inhibitor resistance in Brca2-mutant mammary tumours.
Ordonez LD, Hay T, McEwen R, Polanska UM, Hughes A, Delpuech O, Cadogan E, Powell S, Dry J, Tornillo G, Silcock L, Leo E, O'Connor MJ, Clarke AR, Smalley MJ. Ordonez LD, et al. Among authors: leo e. Oncotarget. 2019 Apr 5;10(27):2586-2606. doi: 10.18632/oncotarget.26830. eCollection 2019 Apr 5. Oncotarget. 2019. PMID: 31080552 Free PMC article.
456 results