Publications

2020

• Targeted protein degradation as a powerful research tool in basic biology and drug target discovery
  ​Wu T, Yoon H, Xiong Y,  Dixon-Clarke SE, Nowak RP, Fischer ES. Nature Structural and Molecular Biology. 2020 June 15.
• Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations
  Jang J, To C, De Clercq DJH, Park E, Ponthier CM, Shin BH, Mushajiang M, Nowak RP, Fischer ES, Eck MJ, Jänne PA, Gray NS. Angewandte Chemie. 2020 Jun 8. 
• The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K
  Slabicki M*, Kozicka Z*, Petzold G, Li Yen-Der, Manojkumar M, Bunker R, Donovan KA, Sievers QL, Koeppel J, Suchyta D, Sperling AS, Gasser JA, Wang LR, Corsello SM, Sellar RS, Jan M, Fink EC, Gillingham D, Scholl C, Fröhling S, Golub TR, Fischer ES, Thomä NH‡, Ebert BL‡. Nature. 2020.
• Development of CDK2 and CDK5 Dual Degrader TMX‐2172
  Teng M, Jiang J, He Z, Kwaitkowski NP, Donovan KA, Mills CE, Victor C, Hatcher JM, Fischer ES, Sorger PK, Zhang T, Gray NS.  Angewandte Chemie. 2020 May 15
• Tubulin Resists Degradation by Cereblon-Recruiting PROTACs.
  Gasic I*, Groendyke BK*, Nowak RP, Yuan JC, Kalabathula J, Fischer ES, Gray NS, Mitchison TJ. Cells. 2020 Apr 27;9(5).
• Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2.
  Morita K, He S, Nowak RP, Wang J, Zimmerman MW, Fu C, Durbin AD, Martel MW, Prutsch N, Gray NS, Fischer ES, Look AT. Cell. 2020 Apr 14.
• Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface
  ​Teng M, Ficarro SB, Yoon H, Che J, Zhou J, Fischer ES, Marto JA, Zhang T‡, Gray NS‡. ACS Medicinal Chemistry Letters. 2020 Apr 3.

2019

• Exploring Targeted Degradation Strategy for Oncogenic KRASG12C
  Zheng M, Xiong Y, Safaee N, Nowak RP, Donovan KA, Yuan CJ, Nabet B, Gero TW, Feru F, Li L, Gondi S, Ombelets LJ, Quan C, Janne PA, Kostic M, Scott DA, Westover KD, Fischer ES, Gray NS.  Cell Chemical Biology. 2019 Dec 26
• Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling.
  You I*, Erickson EC*, Donovan KA, Eleuteri NA, Fischer ES, Gray NS‡, Toker A‡.  Cell Chemical Biology. 2019 Dec 10
• Development and Characterization of a Wee1 Kinase Degrader. 
  ​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. Cell Chemical Biology. 2019 Nov 14
• Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15.
  Faust TB*, Yoon H*, Nowak RP, Donovan KA, Li Z, Cai Q, Eleuteri NA, Zhang T, Gray NS, Fischer ES.  Nature Chemical Biology. 2019 Nov 4. 
  • ​Commentary:  Molecular glue concept solidifies. Baek K and Schulman BA. Nature Chemical Biology
• Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations.
  de Wispelaere M*, Du G*, Donovan KA, Zhang T, Eleuteri NA, Yuan JC, Kalabathula J, Nowak RP, Fischer ES, Gray NS, Yang PL.  Nature Communications. 2019 Aug 1;10(1):3468.
• Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. 
  Silva MC*, Ferguson FM*, Cai Q, Donovan KA, Nandi G, Patnaik D, Zhang T, Huang HT, Lucente DE, Dickerson BC, Mitchison TJ, Fischer ES, Gray NS‡, Haggarty SJ‡​. Elife. 2019 Mar 25;8. pii: e45457.
•  Development of Dual and Selective Degraders of Cyclin‐Dependent Kinases 4 and 6. 
  Jiang B*, Wang ES*, Donovan KA, Liang Y, Fischer ES, Zhang T, Gray NS. Angewandte Chemie. 2019 Feb 25. 
• Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. 
  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.Cell Chemical Biology. 2019 Feb 21;26(2):300-306.e9. Epub 2018 Dec 27. 
• Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. 
  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. Blood. 2019 Feb 28;133(9):952-961. Epub 2018 Dec 13. ​

2018

• Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. 
  Donovan KA, An J, Nowak RP, Yuan JC, Fink EC, Berry BC, Ebert BL, Fischer ES. Elife 2018 Aug 1;7. pii: e38430.
  • Commentary:  Unraveling the mystery of thalidomide. Kelly PN. Science.
  • Commentary: Thalidomide: Unlocking a dark past. Rodriguez-Perez F and Rape M. eLife.
• Genome-wide screen identifies cullin-RING ligase machinery required for lenalidomide-dependent CRL4CRBN activity.
  Sievers QL, Gasser JA, Cowley GS, Fischer ES, Ebert BL.  Blood. 2018 Sep 20;132(12):1293-1303. Epub 2018 Jul 24.
• Structure of the human cGAS–DNA complex reveals enhanced control of immune surveillance.
  Zhou W, Whiteley AT, de Oliveira Mann CC, Morehouse BR, Nowak RP, Fischer ES, Gray NS, Mekalanos JJ, Kranzusch PJ. Cell. 2018 Jul 12;174(2):300-311.e11. 
• Plasticity in binding confers selectivity in ligand-induced protein degradation.  
  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. Nature Chemical Biology Nat Chem Biol. 2018 Jul;14(7):706-714. Epub 2018 Jun 11. 
  • Commentary: Linkers for protein degradation. Chamberlain PP. Nature Chemical Biology
• Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). 
  Powell CE, Gao Y, Tan L, Donovan KA, Nowak RP, Loehr A, Bahcall M, Fischer ES, Jänne PA, George RE, Gray NS.  Journal of Medicinal Chemistry. 2018 May 10;61(9):4249-4255. Epub 2018 Apr 24. 

2017

• ER Stress Signaling Promotes the Survival of Cancer “Persister Cells” Tolerant to EGFR Tyrosine Kinase Inhibitors. 
  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. Cancer Research 2018 Feb 15;78(4):1044-1057. CAN-17-1904. Epub 2017 Dec 19. 
• 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. Nature Chemical Biology. 2018 Feb;14(2):163-170. Epub 2017 Dec 18.
• A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. 
  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. Cell Chemical Biology. 2018 Jan 18;25(1):88-99. Epub 2017 Nov 9.
• Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. 
  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. Cell Chemical Biology. 2017; 24(8):1005-1016.e3. Epub 2017 Aug 3.
• pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase. 
  An J, Ponthier CM, Sack R, Seebacher J, Stadler MB, Donovan KA, Fischer ES. Nature Communications 2017 May 22;8:15398.

2016

• Cullin–RING ubiquitin E3 ligase regulation by the COP9 signalosome. 
  ​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. Nature 2016 Mar 31;531(7596):598-603.
• SPLINTS: small-molecule protein ligand interface stabilizers. 
  Fischer, E.S.‡, Park, E., Eck, M.J.‡, Thomä, N.H‡. Current Opinion in Structural Biology 2016; 37:115-122.
• Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase. 
  Petzold, G., Fischer, E.S., Thomä, N.H. Nature 2016 Apr 7; 532(7597):127-130.

– 2015

• Functional regulation of the DNA damage-recognition factor DDB2 by ubiquitination and interaction with xeroderma pigmentosum group C protein. 
  Matsumoto S., Fischer ES, Yasuda T, Dohmae N, Iwai S, Mori T, Nishi R, Yoshino K, Sakai W, Hanaoka F, Thoma NH, Sugasawa K. Nucleic Acids Research 2015 Feb 18; 43(3): 1700-13. PMCID: PMC4330392.
• Crystal structure of the human COP9 signalosome.
  Lingaraju GM*, Bunker RD*, Cavadini S, Hess D, Hassiepen U, Renatus M, Fischer ES, Thomä NH.  Nature 2014; 512(7513): 161-165.
• Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide. 
  Fischer ES, Böhm K, Lydeard JR, Yang H, Stadler MB, Cavadini S, Nagel J, Acker V, Tichkule R, Forrester WC, Schirle M, Hassiepen U, Ottl J, Hild M, Beckwidth REJ, Harper JW, Jenkins JL, Thomä NH.  Nature 2014; 512(7512): 49-53. PMCID: PMC4423819.
• The Molecular Basis of CRL4DDB2/CSA Ubiquitin Ligase Architecture, Targeting, and Activation. 
  Fischer ES*, Scrima A*, Boehm K, Matsumoto S, Lingaraju, G.M., Faty M, Yasuda T, Cavadini S, Wakasugi M, Hanaoka F, Iwai S, Gut H, Sugasawa K, Thomä NH. Cell 2011; 147(5): 1024-1039.
• Detecting UV‐lesions in the genome: The modular CRL4 ubiquitin ligase does it best!.
  Scrima A, Fischer ES, Lingaraju GM, Böhm K, Cavadini S, Thomä NH.  FEBS Letters 2011; 585(18): 2818-25.

​* equal contribution
‡ shared corresponding authors

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