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Page 1
The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K.
Słabicki M, Kozicka Z, Petzold G, Li YD, Manojkumar M, Bunker RD, Donovan KA, Sievers QL, Koeppel J, Suchyta D, Sperling AS, Fink EC, Gasser JA, Wang LR, Corsello SM, Sellar RS, Jan M, Gillingham D, Scholl C, Fröhling S, Golub TR, Fischer ES, Thomä NH, Ebert BL. Słabicki M, et al. Nature. 2020 Sep;585(7824):293-297. doi: 10.1038/s41586-020-2374-x. Epub 2020 Jun 3. Nature. 2020. PMID: 32494016 Free PMC article.
Proteolysis-targeting chimeras with reduced off-targets.
Nguyen TM, Sreekanth V, Deb A, Kokkonda P, Tiwari PK, Donovan KA, Shoba V, Chaudhary SK, Mercer JAM, Lai S, Sadagopan A, Jan M, Fischer ES, Liu DR, Ebert BL, Choudhary A. Nguyen TM, et al. Nat Chem. 2024 Feb;16(2):218-228. doi: 10.1038/s41557-023-01379-8. Epub 2023 Dec 18. Nat Chem. 2024. PMID: 38110475 Free PMC article.
Small-molecule-induced polymerization triggers degradation of BCL6.
Słabicki M, Yoon H, Koeppel J, Nitsch L, Roy Burman SS, Di Genua C, Donovan KA, Sperling AS, Hunkeler M, Tsai JM, Sharma R, Guirguis A, Zou C, Chudasama P, Gasser JA, Miller PG, Scholl C, Fröhling S, Nowak RP, Fischer ES, Ebert BL. Słabicki M, et al. Nature. 2020 Dec;588(7836):164-168. doi: 10.1038/s41586-020-2925-1. Epub 2020 Nov 18. Nature. 2020. PMID: 33208943 Free PMC article.
Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development.
Donovan KA, Ferguson FM, Bushman JW, Eleuteri NA, Bhunia D, Ryu S, Tan L, Shi K, Yue H, Liu X, Dobrovolsky D, Jiang B, Wang J, Hao M, You I, Teng M, Liang Y, Hatcher J, Li Z, Manz TD, Groendyke B, Hu W, Nam Y, Sengupta S, Cho H, Shin I, Agius MP, Ghobrial IM, Ma MW, Che J, Buhrlage SJ, Sim T, Gray NS, Fischer ES. Donovan KA, et al. Cell. 2020 Dec 10;183(6):1714-1731.e10. doi: 10.1016/j.cell.2020.10.038. Epub 2020 Dec 3. Cell. 2020. PMID: 33275901 Free PMC article.
Targeted kinase degradation via the KLHDC2 ubiquitin E3 ligase.
Kim Y, Seo P, Jeon E, You I, Hwang K, Kim N, Tse J, Bae J, Choi HS, Hinshaw SM, Gray NS, Sim T. Kim Y, et al. Cell Chem Biol. 2023 Nov 16;30(11):1414-1420.e5. doi: 10.1016/j.chembiol.2023.07.008. Epub 2023 Aug 10. Cell Chem Biol. 2023. PMID: 37567174 Free PMC article.
Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
Olson CM, Jiang B, Erb MA, Liang Y, Doctor ZM, Zhang Z, Zhang T, Kwiatkowski N, Boukhali M, Green JL, Haas W, Nomanbhoy T, Fischer ES, Young RA, Bradner JE, Winter GE, Gray NS. Olson CM, et al. Nat Chem Biol. 2018 Feb;14(2):163-170. doi: 10.1038/nchembio.2538. Epub 2017 Dec 18. Nat Chem Biol. 2018. PMID: 29251720 Free PMC article.
Structural basis of regulated m7G tRNA modification by METTL1-WDR4.
Li J, Wang L, Hahn Q, Nowak RP, Viennet T, Orellana EA, Roy Burman SS, Yue H, Hunkeler M, Fontana P, Wu H, Arthanari H, Fischer ES, Gregory RI. Li J, et al. Nature. 2023 Jan;613(7943):391-397. doi: 10.1038/s41586-022-05566-4. Epub 2023 Jan 4. Nature. 2023. PMID: 36599985 Free PMC article.
CDK4/6 Inhibition Augments Antitumor Immunity by Enhancing T-cell Activation.
Deng J, Wang ES, Jenkins RW, Li S, Dries R, Yates K, Chhabra S, Huang W, Liu H, Aref AR, Ivanova E, Paweletz CP, Bowden M, Zhou CW, Herter-Sprie GS, Sorrentino JA, Bisi JE, Lizotte PH, Merlino AA, Quinn MM, Bufe LE, Yang A, Zhang Y, Zhang H, Gao P, Chen T, Cavanaugh ME, Rode AJ, Haines E, Roberts PJ, Strum JC, Richards WG, Lorch JH, Parangi S, Gunda V, Boland GM, Bueno R, Palakurthi S, Freeman GJ, Ritz J, Haining WN, Sharpless NE, Arthanari H, Shapiro GI, Barbie DA, Gray NS, Wong KK. Deng J, et al. Cancer Discov. 2018 Feb;8(2):216-233. doi: 10.1158/2159-8290.CD-17-0915. Epub 2017 Nov 3. Cancer Discov. 2018. PMID: 29101163 Free PMC article.
45 results