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Powell CE, Du G, Che J, He Z, Donovan KA, Yue H, Wang ES, Nowak RP, Zhang T, Fischer ES, Gray NS. Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library. ACS Chem Biol. 2020 Oct 16;15(10):2722-2730. doi: 10.1021/acschembio.0c00520. Epub 2020 Sep 28. PubMed PMID: 32865967.
Bushman JW, Donovan KA, Schauer NJ, Liu X, Hu W, Varca AC, Buhrlage SJ, Fischer ES. Proteomics-Based Identification of DUB Substrates Using Selective Inhibitors. Cell Chem Biol. 2020 Sep 23;. doi: 10.1016/j.chembiol.2020.09.005. [Epub ahead of print] PubMed PMID: 33007217; NIHMSID:NIHMS1630459.
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. The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K. Nature. 2020 Sep;585(7824):293-297. doi: 10.1038/s41586-020-2374-x. Epub 2020 Jun 3. PubMed PMID: 32494016; PubMed Central PMCID: PMC7486275.
Teng M, Jiang J, He Z, Kwiatkowski NP, Donovan KA, Mills CE, Victor C, Hatcher JM, Fischer ES, Sorger PK, Zhang T, Gray NS. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020 Aug 10;59(33):13865-13870. doi: 10.1002/anie.202004087. Epub 2020 Jun 3. PubMed PMID: 32415712; NIHMSID:NIHMS1637531.
Morita K, He S, Nowak RP, Wang J, Zimmerman MW, Fu C, Durbin AD, Martel MW, Prutsch N, Gray NS, Fischer ES, Look AT. Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2. Cell. 2020 Apr 30;181(3):702-715.e20. doi: 10.1016/j.cell.2020.03.051. Epub 2020 Apr 20. PubMed PMID: 32315619; PubMed Central PMCID: PMC7397863.
Gasic I, Groendyke BJ, Nowak RP, Yuan JC, Kalabathula J, Fischer ES, Gray NS, Mitchison TJ. Tubulin Resists Degradation by Cereblon-Recruiting PROTACs. Cells. 2020 Apr 27;9(5). doi: 10.3390/cells9051083. PubMed PMID: 32349222; PubMed Central PMCID: PMC7290497.
You I, Erickson EC, Donovan KA, Eleuteri NA, Fischer ES, Gray NS, Toker A. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 Jan 16;27(1):66-73.e7. doi: 10.1016/j.chembiol.2019.11.014. Epub 2019 Dec 16. PubMed PMID: 31859249; PubMed Central PMCID: PMC6980747.
Li Z, Pinch BJ, Olson CM, Donovan KA, Nowak RP, Mills CE, Scott DA, Doctor ZM, Eleuteri NA, Chung M, Sorger PK, Fischer ES, Gray NS. Development and Characterization of a Wee1 Kinase Degrader. Cell Chem Biol. 2020 Jan 16;27(1):57-65.e9. doi: 10.1016/j.chembiol.2019.10.013. Epub 2019 Nov 14. PubMed PMID: 31735695; PubMed Central PMCID: PMC6980656.
Faust TB, Yoon H, Nowak RP, Donovan KA, Li Z, Cai Q, Eleuteri NA, Zhang T, Gray NS, Fischer ES. Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15. Nat Chem Biol. 2020 Jan;16(1):7-14. doi: 10.1038/s41589-019-0378-3. Epub 2019 Nov 4. PubMed PMID: 31686031; PubMed Central PMCID: PMC6917914.
de Wispelaere M, Du G, Donovan KA, Zhang T, Eleuteri NA, Yuan JC, Kalabathula J, Nowak RP, Fischer ES, Gray NS, Yang PL. Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. Nat Commun. 2019 Aug 1;10(1):3468. doi: 10.1038/s41467-019-11429-w. PubMed PMID: 31371704; PubMed Central PMCID: PMC6672008.
Jiang B, Wang ES, Donovan KA, Liang Y, Fischer ES, Zhang T, Gray NS. Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 May 6;58(19):6321-6326. doi: 10.1002/anie.201901336. Epub 2019 Mar 29. PubMed PMID: 30802347; NIHMSID:NIHMS1637526.
Dobrovolsky D, Wang ES, Morrow S, Leahy C, Faust T, Nowak RP, Donovan KA, Yang G, Li Z, Fischer ES, Treon SP, Weinstock DM, Gray NS. Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood. 2019 Feb 28;133(9):952-961. doi: 10.1182/blood-2018-07-862953. Epub 2018 Dec 13. PubMed PMID: 30545835; PubMed Central PMCID: PMC6396177.
Brand M, Jiang B, Bauer S, Donovan KA, Liang Y, Wang ES, Nowak RP, Yuan JC, Zhang T, Kwiatkowski N, Müller AC, Fischer ES, Gray NS, Winter GE. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chem Biol. 2019 Feb 21;26(2):300-306.e9. doi: 10.1016/j.chembiol.2018.11.006. Epub 2018 Dec 27. PubMed PMID: 30595531; PubMed Central PMCID: PMC6444916.
Sievers QL, Gasser JA, Cowley GS, Fischer ES, Ebert BL. Genome-wide screen identifies cullin-RING ligase machinery required for lenalidomide-dependent CRL4CRBN activity. Blood. 2018 Sep 20;132(12):1293-1303. doi: 10.1182/blood-2018-01-821769. Epub 2018 Jul 24. PubMed PMID: 30042095; PubMed Central PMCID: PMC6148446.
Donovan KA, An J, Nowak RP, Yuan JC, Fink EC, Berry BC, Ebert BL, Fischer ES. Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. Elife. 2018 Aug 1;7. doi: 10.7554/eLife.38430. PubMed PMID: 30067223; PubMed Central PMCID: PMC6156078.
Zhou W, Whiteley AT, de Oliveira Mann CC, Morehouse BR, Nowak RP, Fischer ES, Gray NS, Mekalanos JJ, Kranzusch PJ. Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell. 2018 Jul 12;174(2):300-311.e11. doi: 10.1016/j.cell.2018.06.026. PubMed PMID: 30007416; PubMed Central PMCID: PMC6084792.
Nowak RP, DeAngelo SL, Buckley D, He Z, Donovan KA, An J, Safaee N, Jedrychowski MP, Ponthier CM, Ishoey M, Zhang T, Mancias JD, Gray NS, Bradner JE, Fischer ES. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714. doi: 10.1038/s41589-018-0055-y. Epub 2018 Jun 11. PubMed PMID: 29892083; PubMed Central PMCID: PMC6202246.
Powell CE, Gao Y, Tan L, Donovan KA, Nowak RP, Loehr A, Bahcall M, Fischer ES, Jänne PA, George RE, Gray NS. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2018 May 10;61(9):4249-4255. doi: 10.1021/acs.jmedchem.7b01655. Epub 2018 Apr 24. PubMed PMID: 29660984; PubMed Central PMCID: PMC6294449.
Terai H, Kitajima S, Potter DS, Matsui Y, Quiceno LG, Chen T, Kim TJ, Rusan M, Thai TC, Piccioni F, Donovan KA, Kwiatkowski N, Hinohara K, Wei G, Gray NS, Fischer ES, Wong KK, Shimamura T, Letai A, Hammerman PS, Barbie DA. ER Stress Signaling Promotes the Survival of Cancer "Persister Cells" Tolerant to EGFR Tyrosine Kinase Inhibitors. Cancer Res. 2018 Feb 15;78(4):1044-1057. doi: 10.1158/0008-5472.CAN-17-1904. Epub 2017 Dec 19. PubMed PMID: 29259014; PubMed Central PMCID: PMC5815936.
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. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat Chem Biol. 2018 Feb;14(2):163-170. doi: 10.1038/nchembio.2538. Epub 2017 Dec 18. PubMed PMID: 29251720; PubMed Central PMCID: PMC5912898.
Huang HT, Dobrovolsky D, Paulk J, Yang G, Weisberg EL, Doctor ZM, Buckley DL, Cho JH, Ko E, Jang J, Shi K, Choi HG, Griffin JD, Li Y, Treon SP, Fischer ES, Bradner JE, Tan L, Gray NS. A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. Cell Chem Biol. 2018 Jan 18;25(1):88-99.e6. doi: 10.1016/j.chembiol.2017.10.005. Epub 2017 Nov 9. PubMed PMID: 29129717; PubMed Central PMCID: PMC6427047.
Zeng M, Lu J, Li L, Feru F, Quan C, Gero TW, Ficarro SB, Xiong Y, Ambrogio C, Paranal RM, Catalano M, Shao J, Wong KK, Marto JA, Fischer ES, Jänne PA, Scott DA, Westover KD, Gray NS. Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. Cell Chem Biol. 2017 Aug 17;24(8):1005-1016.e3. doi: 10.1016/j.chembiol.2017.06.017. Epub 2017 Aug 3. PubMed PMID: 28781124.
An J, Ponthier CM, Sack R, Seebacher J, Stadler MB, Donovan KA, Fischer ES. pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase. Nat Commun. 2017 May 22;8:15398. doi: 10.1038/ncomms15398. PubMed PMID: 28530236; PubMed Central PMCID: PMC5458144.
Petzold G, Fischer ES, Thomä NH. Structural basis of lenalidomide-induced CK1α degradation by the CRL4(CRBN) ubiquitin ligase. Nature. 2016 Apr 7;532(7597):127-30. doi: 10.1038/nature16979. Epub 2016 Feb 24. PubMed PMID: 26909574.
Fischer ES, Park E, Eck MJ, Thomä NH. SPLINTS: small-molecule protein ligand interface stabilizers. Curr Opin Struct Biol. 2016 Apr;37:115-22. doi: 10.1016/j.sbi.2016.01.004. Epub 2016 Jan 30. Review. PubMed PMID: 26829757; PubMed Central PMCID: PMC4834252.
Cavadini S, Fischer ES, Bunker RD, Potenza A, Lingaraju GM, Goldie KN, Mohamed WI, Faty M, Petzold G, Beckwith RE, Tichkule RB, Hassiepen U, Abdulrahman W, Pantelic RS, Matsumoto S, Sugasawa K, Stahlberg H, Thomä NH. Cullin-RING ubiquitin E3 ligase regulation by the COP9 signalosome. Nature. 2016 Mar 31;531(7596):598-603. doi: 10.1038/nature17416. PubMed PMID: 27029275.
Matsumoto S, Fischer ES, Yasuda T, Dohmae N, Iwai S, Mori T, Nishi R, Yoshino K, Sakai W, Hanaoka F, Thomä NH, Sugasawa K. Functional regulation of the DNA damage-recognition factor DDB2 by ubiquitination and interaction with xeroderma pigmentosum group C protein. Nucleic Acids Res. 2015 Feb 18;43(3):1700-13. doi: 10.1093/nar/gkv038. Epub 2015 Jan 27. PubMed PMID: 25628365; PubMed Central PMCID: PMC4330392.
Lingaraju GM, Bunker RD, Cavadini S, Hess D, Hassiepen U, Renatus M, Fischer ES, Thomä NH. Crystal structure of the human COP9 signalosome. Nature. 2014 Aug 14;512(7513):161-5. doi: 10.1038/nature13566. Epub 2014 Jul 16. PubMed PMID: 25043011.
Fischer ES, Böhm K, Lydeard JR, Yang H, Stadler MB, Cavadini S, Nagel J, Serluca F, Acker V, Lingaraju GM, Tichkule RB, Schebesta M, Forrester WC, Schirle M, Hassiepen U, Ottl J, Hild M, Beckwith RE, Harper JW, Jenkins JL, Thomä NH. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature. 2014 Aug 7;512(7512):49-53. doi: 10.1038/nature13527. Epub 2014 Jul 16. PubMed PMID: 25043012; PubMed Central PMCID: PMC4423819.
Fischer ES, Scrima A, Böhm K, Matsumoto S, Lingaraju GM, Faty M, Yasuda T, Cavadini S, Wakasugi M, Hanaoka F, Iwai S, Gut H, Sugasawa K, Thomä NH. The molecular basis of CRL4DDB2/CSA ubiquitin ligase architecture, targeting, and activation. Cell. 2011 Nov 23;147(5):1024-39. doi: 10.1016/j.cell.2011.10.035. PubMed PMID: 22118460.
Scrima A, Fischer ES, Lingaraju GM, Böhm K, Cavadini S, Thomä NH. Detecting UV-lesions in the genome: The modular CRL4 ubiquitin ligase does it best!. FEBS Lett. 2011 Sep 16;585(18):2818-25. doi: 10.1016/j.febslet.2011.04.064. Epub 2011 May 6. Review. PubMed PMID: 21550341.
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