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Page 1
Thoughts for the future.
Alkhalaf LM, Arrowsmith C, Balskus EP, Bergamini G, Bhandari R, Chang CJ, Chen P, Chen X, Ciulli A, Cricco JA, Davis BG, Delbianco M, Dudareva N, Dueber E, Ferguson F, de Giuseppe PO, Hamachi I, Hammond MC, Hatzios SK, Do Heo W, Janet JP, Kamat SS, Knapp S, Krishnan Y, Lang K, Laraia L, Leveson-Gower RB, Li XD, Liu DR, Liu MF, London N, Mahanta N, Mayor-Ruiz C, Muir T, Murakami MT, Rhee HW, Robers M, Satz A, Schulman BA, Shen B, Shoichet B, Strauss E, Suzuki T, Tiwary P, Waldmann H, Ward TR, Weeks A, Weerapana E, Winter G. Alkhalaf LM, et al. Among authors: arrowsmith c. Nat Chem Biol. 2025 Jan;21(1):6-15. doi: 10.1038/s41589-024-01802-2. Nat Chem Biol. 2025. PMID: 39719500 No abstract available.
Toward target 2035: EUbOPEN - a public-private partnership to enable & unlock biology in the open.
Tredup C, Ackloo S, Beck H, Brown PJ, Bullock AN, Ciulli A, Dikic I, Edfeldt K, Edwards AM, Elkins JM, Farin HF, Fon EA, Gstaiger M, Günther J, Gustavsson AL, Häberle S, Isigkeit L, Huber KVM, Kotschy A, Krämer O, Leach AR, Marsden BD, Matsui H, Merk D, Montel F, Mulder MPC, Müller S, Owen DR, Proschak E, Röhm S, Stolz A, Sundström M, von Delft F, Willson TM, Arrowsmith CH, Knapp S. Tredup C, et al. Among authors: arrowsmith ch. RSC Med Chem. 2024 Nov 29. doi: 10.1039/d4md00735b. Online ahead of print. RSC Med Chem. 2024. PMID: 39618964 Free PMC article.
A Covalent Chemical Probe for Chikungunya nsP2 Cysteine Protease with Antialphaviral Activity and Proteome-wide Selectivity.
Ghoshal A, Tse EG, Hossain MA, Asressu KH, Merten EM, Sears JD, Howell S, Perveen S, Burdick J, Morales NL, Martinez SA, Law I, Davenport BJ, Morrison TE, Streblow ZJ, Streblow DN, Mordant AL, Webb TS, Cabrera A, Herring LE, Arrowsmith CH, Pearce KH, Moorman NJ, Heise MT, Couñago RM, Brown PJ, Willson TM. Ghoshal A, et al. Among authors: arrowsmith ch. Res Sq [Preprint]. 2024 Nov 12:rs.3.rs-5363451. doi: 10.21203/rs.3.rs-5363451/v1. Res Sq. 2024. PMID: 39606462 Free PMC article. Preprint.
Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer.
Johnson RL, Graboski AL, Li F, Norris-Drouin JL, Walton WG, Arrowsmith CH, Redinbo MR, Frye SV, James LI. Johnson RL, et al. Among authors: arrowsmith ch. J Med Chem. 2024 Nov 28;67(22):20056-20075. doi: 10.1021/acs.jmedchem.4c01172. Epub 2024 Nov 7. J Med Chem. 2024. PMID: 39508435
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: arrowsmith ch. 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
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: arrowsmith ch. J Med Chem. 2024 Nov 4. doi: 10.1021/acs.jmedchem.4c02010. Online ahead of print. J Med Chem. 2024. PMID: 39495097
Inhibiting EZH2 targets atypical teratoid rhabdoid tumor by triggering viral mimicry via both RNA and DNA sensing pathways.
Feng S, Marhon SA, Sokolowski DJ, D'Costa A, Soares F, Mehdipour P, Ishak C, Loo Yau H, Ettayebi I, Patel PS, Chen R, Liu J, Zuzarte PC, Ho KC, Ho B, Ning S, Huang A, Arrowsmith CH, Wilson MD, Simpson JT, De Carvalho DD. Feng S, et al. Among authors: arrowsmith ch. Nat Commun. 2024 Oct 29;15(1):9321. doi: 10.1038/s41467-024-53515-8. Nat Commun. 2024. PMID: 39472584 Free PMC article.
The use of a multi-metric readout screen to identify EHMT2/G9a-inhibition as a modulator of cancer-associated fibroblast activation state.
Wu NC, Quevedo R, Nurse M, Hezaveh K, Liu H, Sun F, Muffat J, Sun Y, Simmons CA, McGaha TL, Prinos P, Arrowsmith CH, Ailles L, D'Arcangelo E, McGuigan AP. Wu NC, et al. Among authors: arrowsmith ch. Biomaterials. 2025 Mar;314:122879. doi: 10.1016/j.biomaterials.2024.122879. Epub 2024 Oct 5. Biomaterials. 2025. PMID: 39395244 Free article.
Identification of a cell-active chikungunya virus nsP2 protease inhibitor using a covalent fragment-based screening approach.
Merten EM, Sears JD, Leisner TM, Hardy PB, Ghoshal A, Hossain MA, Asressu KH, Brown PJ, Tse EG, Stashko MA, Li K, Norris-Drouin JL, Herring LE, Mordant AL, Webb TS, Mills CA, Barker NK, Streblow ZJ, Perveen S, Arrowsmith CH, Couñago RM, Arnold JJ, Cameron CE, Streblow DN, Moorman NJ, Heise MT, Willson TM, Popov KI, Pearce KH. Merten EM, et al. Among authors: arrowsmith ch. Proc Natl Acad Sci U S A. 2024 Oct 15;121(42):e2409166121. doi: 10.1073/pnas.2409166121. Epub 2024 Oct 10. Proc Natl Acad Sci U S A. 2024. PMID: 39388272
475 results