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Page 1
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: gunnarsson a. J Med Chem. 2024 Dec 26;67(24):21717-21728. doi: 10.1021/acs.jmedchem.4c01725. Epub 2024 Dec 10. J Med Chem. 2024. PMID: 39655996
Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3-3 Protein-Protein Interaction.
Pallesen JS, Munier CC, Bosica F, Andrei SA, Edman K, Gunnarsson A, La Sala G, Putra OD, Srdanović S, Wilson AJ, Wissler L, Ottmann C, Perry MWD, O'Mahony G. Pallesen JS, et al. Among authors: gunnarsson a. J Med Chem. 2022 Dec 22;65(24):16818-16828. doi: 10.1021/acs.jmedchem.2c01635. Epub 2022 Dec 9. J Med Chem. 2022. PMID: 36484727 Free PMC article.
Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1,3,4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism.
Ripa L, Sandmark J, Hughes G, Shamovsky I, Gunnarsson A, Johansson J, Llinas A, Collins M, Jung B, Novén A, Pemberton N, Mogemark M, Xiong Y, Li Q, Tångefjord S, Ek M, Åstrand A. Ripa L, et al. Among authors: gunnarsson a. J Med Chem. 2023 Oct 26;66(20):14188-14207. doi: 10.1021/acs.jmedchem.3c01269. Epub 2023 Oct 5. J Med Chem. 2023. PMID: 37797307
Vinylpyridine as a Tunable Covalent Warhead Targeting C797 in EGFR.
Pemberton N, Compagne N, Argyrou A, Evertsson E, Gunnarsson A, Kettle JG, Orme JP, Ward RA. Pemberton N, et al. Among authors: gunnarsson a. ACS Med Chem Lett. 2024 Apr 5;15(5):583-589. doi: 10.1021/acsmedchemlett.3c00425. eCollection 2024 May 9. ACS Med Chem Lett. 2024. PMID: 38746885
CACHE Challenge #1: Targeting the WDR Domain of LRRK2, A Parkinson's Disease Associated Protein.
Li F, Ackloo S, Arrowsmith CH, Ban F, Barden CJ, Beck H, Beránek J, Berenger F, Bolotokova A, Bret G, Breznik M, Carosati E, Chau I, Chen Y, Cherkasov A, Corte DD, Denzinger K, Dong A, Draga S, Dunn I, Edfeldt K, Edwards A, Eguida M, Eisenhuth P, Friedrich L, Fuerll A, Gardiner SS, Gentile F, Ghiabi P, Gibson E, Glavatskikh M, Gorgulla C, Guenther J, Gunnarsson A, Gusev F, Gutkin E, Halabelian L, Harding RJ, Hillisch A, Hoffer L, Hogner A, Houliston S, Irwin JJ, Isayev O, Ivanova A, Jacquemard C, Jarrett AJ, Jensen JH, Kireev D, Kleber J, Koby SB, Koes D, Kumar A, Kurnikova MG, Kutlushina A, Lessel U, Liessmann F, Liu S, Lu W, Meiler J, Mettu A, Minibaeva G, Moretti R, Morris CJ, Narangoda C, Noonan T, Obendorf L, Pach S, Pandit A, Perveen S, Poda G, Polishchuk P, Puls K, Pütter V, Rognan D, Roskams-Edris D, Schindler C, Sindt F, Spiwok V, Steinmann C, Stevens RL, Talagayev V, Tingey D, Vu O, Walters WP, Wang X, Wang Z, Wolber G, Wolf CA, Wortmann L, Zeng H, Zepeda CA, Zhang KYJ, Zhang J, Zheng S, Schapira M. Li F, et al. Among authors: gunnarsson a. J Chem Inf Model. 2024 Nov 25;64(22):8521-8536. doi: 10.1021/acs.jcim.4c01267. Epub 2024 Nov 5. J Chem Inf Model. 2024. PMID: 39499532
Correction to "Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3-3 Protein-Protein Interaction".
Pallesen JS, Munier CC, Bosica F, Andrei SA, Edman K, Gunnarsson A, La Sala G, Putra OD, Srdanović S, Wilson AJ, Wissler L, Ottmann C, Perry MWD, O'Mahony G. Pallesen JS, et al. Among authors: gunnarsson a. J Med Chem. 2023 Feb 9;66(3):2205-2207. doi: 10.1021/acs.jmedchem.3c00076. Epub 2023 Jan 28. J Med Chem. 2023. PMID: 36708352 Free PMC article. No abstract available.
Quaternary glucocorticoid receptor structure highlights allosteric interdomain communication.
Postel S, Wissler L, Johansson CA, Gunnarsson A, Gordon E, Collins B, Castaldo M, Köhler C, Öling D, Johansson P, Fröderberg Roth L, Beinsteiner B, Dainty I, Delaney S, Klaholz BP, Billas IML, Edman K. Postel S, et al. Among authors: gunnarsson a. Nat Struct Mol Biol. 2023 Mar;30(3):286-295. doi: 10.1038/s41594-022-00914-4. Epub 2023 Feb 6. Nat Struct Mol Biol. 2023. PMID: 36747092
Creating Designer Engineered Extracellular Vesicles for Diverse Ligand Display, Target Recognition, and Controlled Protein Loading and Delivery.
Ivanova A, Badertscher L, O'Driscoll G, Bergman J, Gordon E, Gunnarsson A, Johansson C, Munson MJ, Spinelli C, Torstensson S, Vilén L, Voirel A, Wiseman J, Rak J, Dekker N, Lázaro-Ibáñez E. Ivanova A, et al. Among authors: gunnarsson a. Adv Sci (Weinh). 2023 Dec;10(34):e2304389. doi: 10.1002/advs.202304389. Epub 2023 Oct 22. Adv Sci (Weinh). 2023. PMID: 37867228 Free PMC article.
210 results