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2022 1
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Page 1
Targeting colorectal cancer with small-molecule inhibitors of ALDH1B1.
Feng Z, Hom ME, Bearrood TE, Rosenthal ZC, Fernández D, Ondrus AE, Gu Y, McCormick AK, Tomaske MG, Marshall CR, Kline T, Chen CH, Mochly-Rosen D, Kuo CJ, Chen JK. Feng Z, et al. Nat Chem Biol. 2022 Oct;18(10):1065-1075. doi: 10.1038/s41589-022-01048-w. Epub 2022 Jul 4. Nat Chem Biol. 2022. PMID: 35788181 Free PMC article.
Relocalizing transcriptional kinases to activate apoptosis.
Sarott RC, Gourisankar S, Karim B, Nettles S, Yang H, Dwyer BG, Simanauskaite JM, Tse J, Abuzaid H, Krokhotin A, Zhang T, Hinshaw SM, Green MR, Crabtree GR, Gray NS. Sarott RC, et al. Science. 2024 Oct 4;386(6717):eadl5361. doi: 10.1126/science.adl5361. Epub 2024 Oct 4. Science. 2024. PMID: 39361741
Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders.
Li YD, Ma MW, Hassan MM, Hunkeler M, Teng M, Puvar K, Lumpkin R, Sandoval B, Jin CY, Ficarro SB, Wang MY, Xu S, Groendyke BJ, Sigua LH, Tavares I, Zou C, Tsai JM, Park PMC, Yoon H, Majewski FC, Marto JA, Qi J, Nowak RP, Donovan KA, Słabicki M, Gray NS, Fischer ES, Ebert BL. Li YD, et al. bioRxiv [Preprint]. 2023 Feb 15:2023.02.14.528208. doi: 10.1101/2023.02.14.528208. bioRxiv. 2023. Update in: Nat Chem Biol. 2024 Dec;20(12):1640-1649. doi: 10.1038/s41589-024-01668-4 PMID: 36824856 Free PMC article. Updated. Preprint.
Discovery of electrophilic degraders that exploit SNAr chemistry.
Zhuang Z, Byun WS, Kozicka Z, Dwyer BG, Donovan KA, Jiang Z, Jones HM, Abeja DM, Nix MN, Zhong J, Słabicki M, Fischer ES, Ebert BL, Gray NS. Zhuang Z, et al. bioRxiv [Preprint]. 2024 Sep 27:2024.09.25.615094. doi: 10.1101/2024.09.25.615094. bioRxiv. 2024. PMID: 39386645 Free PMC article. Preprint.
Template-assisted covalent modification underlies activity of covalent molecular glues.
Li YD, Ma MW, Hassan MM, Hunkeler M, Teng M, Puvar K, Rutter JC, Lumpkin RJ, Sandoval B, Jin CY, Schmoker AM, Ficarro SB, Cheong H, Metivier RJ, Wang MY, Xu S, Byun WS, Groendyke BJ, You I, Sigua LH, Tavares I, Zou C, Tsai JM, Park PMC, Yoon H, Majewski FC, Sperling HT, Marto JA, Qi J, Nowak RP, Donovan KA, Słabicki M, Gray NS, Fischer ES, Ebert BL. Li YD, et al. Nat Chem Biol. 2024 Dec;20(12):1640-1649. doi: 10.1038/s41589-024-01668-4. Epub 2024 Jul 29. Nat Chem Biol. 2024. PMID: 39075252 Free PMC article.
Exploration of the Tunability of BRD4 Degradation by DCAF16 Trans-labelling Covalent Glues.
Hassan MM, Li YD, Ma MW, Teng M, Byun WS, Puvar K, Lumpkin R, Sandoval B, Rutter JC, Jin CY, Wang MY, Xu S, Schmoker AM, Cheong H, Groendyke BJ, Qi J, Fischer ES, Ebert BL, Gray NS. Hassan MM, et al. bioRxiv [Preprint]. 2023 Oct 10:2023.10.07.561308. doi: 10.1101/2023.10.07.561308. bioRxiv. 2023. Update in: Eur J Med Chem. 2024 Dec 5;279:116904. doi: 10.1016/j.ejmech.2024.116904 PMID: 37873358 Free PMC article. Updated. Preprint.
Activating p53Y220C with a Mutant-Specific Small Molecule.
Zhu X, Byun WS, Pieńkowska DE, Nguyen KT, Gerhartz J, Geng Q, Qiu T, Zhong J, Jiang Z, Wang M, Sarott RC, Hinshaw SM, Zhang T, Attardi LD, Nowak RP, Gray NS. Zhu X, et al. bioRxiv [Preprint]. 2024 Oct 28:2024.10.23.619961. doi: 10.1101/2024.10.23.619961. bioRxiv. 2024. PMID: 39554093 Free PMC article. Preprint.
13 results