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Page 1
Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2.
Ferreira de Freitas R, Liu Y, Szewczyk MM, Mehta N, Li F, McLeod D, Zepeda-Velázquez C, Dilworth D, Hanley RP, Gibson E, Brown PJ, Al-Awar R, James LI, Arrowsmith CH, Barsyte-Lovejoy D, Min J, Vedadi M, Schapira M, Allali-Hassani A. Ferreira de Freitas R, et al. Among authors: gibson e. J Med Chem. 2021 Feb 11;64(3):1584-1592. doi: 10.1021/acs.jmedchem.0c01768. Epub 2021 Feb 1. J Med Chem. 2021. PMID: 33522809 Free PMC article.
A NSD3-targeted PROTAC suppresses NSD3 and cMyc oncogenic nodes in cancer cells.
Xu C, Meng F, Park KS, Storey AJ, Gong W, Tsai YH, Gibson E, Byrum SD, Li D, Edmondson RD, Mackintosh SG, Vedadi M, Cai L, Tackett AJ, Kaniskan HÜ, Jin J, Wang GG. Xu C, et al. Among authors: gibson e. Cell Chem Biol. 2022 Mar 17;29(3):386-397.e9. doi: 10.1016/j.chembiol.2021.08.004. Epub 2021 Aug 31. Cell Chem Biol. 2022. PMID: 34469831 Free PMC article.
A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization.
Dilworth D, Hanley RP, Ferreira de Freitas R, Allali-Hassani A, Zhou M, Mehta N, Marunde MR, Ackloo S, Carvalho Machado RA, Khalili Yazdi A, Owens DDG, Vu V, Nie DY, Alqazzaz M, Marcon E, Li F, Chau I, Bolotokova A, Qin S, Lei M, Liu Y, Szewczyk MM, Dong A, Kazemzadeh S, Abramyan T, Popova IK, Hall NW, Meiners MJ, Cheek MA, Gibson E, Kireev D, Greenblatt JF, Keogh MC, Min J, Brown PJ, Vedadi M, Arrowsmith CH, Barsyte-Lovejoy D, James LI, Schapira M. Dilworth D, et al. Among authors: gibson e. Nat Chem Biol. 2022 Jan;18(1):56-63. doi: 10.1038/s41589-021-00898-0. Epub 2021 Nov 15. Nat Chem Biol. 2022. PMID: 34782742 Free PMC article.
Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2.
Hanley RP, Nie DY, Tabor JR, Li F, Sobh A, Xu C, Barker NK, Dilworth D, Hajian T, Gibson E, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Herring LE, Wang GG, Licht JD, Vedadi M, Arrowsmith CH, James LI. Hanley RP, et al. Among authors: gibson e. J Am Chem Soc. 2023 Apr 12;145(14):8176-8188. doi: 10.1021/jacs.3c01421. Epub 2023 Mar 28. J Am Chem Soc. 2023. PMID: 36976643 Free PMC article.
Subpocket Similarity-Based Hit Identification for Challenging Targets: Application to the WDR Domain of LRRK2.
Eguida M, Bret G, Sindt F, Li F, Chau I, Ackloo S, Arrowsmith C, Bolotokova A, Ghiabi P, Gibson E, Halabelian L, Houliston S, Harding RJ, Hutchinson A, Loppnau P, Perveen S, Seitova A, Zeng H, Schapira M, Rognan D. Eguida M, et al. Among authors: gibson e. J Chem Inf Model. 2024 Jul 8;64(13):5344-5355. doi: 10.1021/acs.jcim.4c00601. Epub 2024 Jun 25. J Chem Inf Model. 2024. PMID: 38916159
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins.
Ackloo S, Li F, Szewczyk M, Seitova A, Loppnau P, Zeng H, Xu J, Ahmad S, Arnautova YA, Baghaie AJ, Beldar S, Bolotokova A, Centrella PA, Chau I, Clark MA, Cuozzo JW, Dehghani-Tafti S, Disch JS, Dong A, Dumas A, Feng JA, Ghiabi P, Gibson E, Gilmer J, Goldman B, Green SR, Guié MA, Guilinger JP, Harms N, Herasymenko O, Houliston S, Hutchinson A, Kearnes S, Keefe AD, Kimani SW, Kramer T, Kutera M, Kwak HA, Lento C, Li Y, Liu J, Loup J, Machado RAC, Mulhern CJ, Perveen S, Righetto GL, Riley P, Shrestha S, Sigel EA, Silva M, Sintchak MD, Slakman BL, Taylor RD, Thompson J, Torng W, Underkoffler C, von Rechenberg M, Walsh RT, Watson I, Wilson DJ, Wolf E, Yadav M, Yazdi AK, Zhang J, Zhang Y, Santhakumar V, Edwards AM, Barsyte-Lovejoy D, Schapira M, Brown PJ, Halabelian L, Arrowsmith CH. Ackloo S, et al. Among authors: gibson e. J Med Chem. 2024 Nov 4. doi: 10.1021/acs.jmedchem.4c02010. Online ahead of print. J Med Chem. 2024. PMID: 39495097
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: gibson e. 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
segcsvdWMH: A Convolutional Neural Network-Based Tool for Quantifying White Matter Hyperintensities in Heterogeneous Patient Cohorts.
Gibson E, Ramirez J, Woods LA, Ottoy J, Berberian S, Scott CJM, Yhap V, Gao F, Coello RD, Valdes Hernandez M, Lang AE, Tartaglia CM, Kumar S, Binns MA, Bartha R, Symons S, Swartz RH, Masellis M, Singh N, Moody A, MacIntosh BJ, Wardlaw JM, Black SE, Lim ASP, Goubran M; ONDRI Investigators, ADNI, CAIN Investigators, colleagues from the Foundation Leducq Transatlantic Network of Excellence. Gibson E, et al. Hum Brain Mapp. 2024 Dec 15;45(18):e70104. doi: 10.1002/hbm.70104. Hum Brain Mapp. 2024. PMID: 39723488 Free PMC article.
914 results