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Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
Johannes JW, Balazs AYS, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey KJ, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner CJB, Leo E, Liu L, Madin A, 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: fawell s. J Med Chem. 2024 Dec 10. doi: 10.1021/acs.jmedchem.4c01725. Online ahead of print. J Med Chem. 2024. PMID: 39655996
Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations.
Bashi AC, Coker EA, Bulusu KC, Jaaks P, Crafter C, Lightfoot H, Milo M, McCarten K, Jenkins DF, van der Meer D, Lynch JT, Barthorpe S, Andersen CL, Barry ST, Beck A, Cidado J, Gordon JA, Hall C, Hall J, Mali I, Mironenko T, Mongeon K, Morris J, Richardson L, Smith PD, Tavana O, Tolley C, Thomas F, Willis BS, Yang W, O'Connor MJ, McDermott U, Critchlow SE, Drew L, Fawell SE, Mettetal JT, Garnett MJ. Bashi AC, et al. Among authors: fawell se. Cancer Discov. 2024 May 1;14(5):846-865. doi: 10.1158/2159-8290.CD-23-0388. Cancer Discov. 2024. PMID: 38456804 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. Among authors: fawell s. Nat Commun. 2024 Feb 24;15(1):1700. doi: 10.1038/s41467-024-45996-4. Nat Commun. 2024. PMID: 38402224 Free PMC article.
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: fawell s. Clin Cancer Res. 2024 Apr 1;30(7):1338-1351. doi: 10.1158/1078-0432.CCR-23-2094. Clin Cancer Res. 2024. PMID: 37967136
Novel Arginase Inhibitor, AZD0011, Demonstrates Immune Cell Stimulation and Antitumor Efficacy with Diverse Combination Partners.
Doshi AS, Cantin S, Hernandez M, Srinivasan S, Tentarelli S, Griffin M, Wang Y, Pop-Damkov P, Prickett LB, Kankkonen C, Shen M, Martin MS, Wu S, Castaldi MP, Ghadially H, Varnes J, Gales S, Henry D, Hoover C, Mele DA, Simpson I, Gangl ET, Mlynarski SN, Finlay MRV, Drew L, Fawell SE, Shao W, Schuller AG. Doshi AS, et al. Among authors: fawell se. Mol Cancer Ther. 2023 May 4;22(5):630-645. doi: 10.1158/1535-7163.MCT-22-0431. Mol Cancer Ther. 2023. PMID: 36912782
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: fawell s. 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.
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: fawell s. 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.
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: fawell s. 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
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: fawell se. 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
How a new drug is born.
Caporali A, Fawell S, Scaltriti M. Caporali A, et al. Among authors: fawell s. Eur Heart J. 2021 Aug 21;42(32):3039-3041. doi: 10.1093/eurheartj/ehab076. Eur Heart J. 2021. PMID: 33718951 No abstract available.
83 results