Publications at the Fischer Lab

Preprints

• SMAC mimetics induce human macrophages to phagocytose live cancer cells
  ​Liu SY, Hulsman M, Leyendecker P, Chang E, Donovan KA, Strobel F, Dougan J, Fischer ES, Dougan M, Dougan SK, Qiang L. BioRxiv. 20224
• 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. bioRxiv. 2024
• Unveiling the hidden interactome of CRBN molecular glues with chemoproteomics
  ​Baek K*, Metivier RJ*, Roy Burman SS, Bushman JW, Yoon H, Lumpkin RJ, Abeja DM, Lakshminarayan M, Yue H, Ojeda S, Verano AL, Gray NS, Donovan KA‡, Fischer ES‡. bioRxiv. 2024
• Discovery of CRBN-dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library
  Razumkov H, Jiang Z, Baek K, You I, Geng Q, Donovan KA, Tang MT, Metivier RJ, Mageed N, Seo P, Li Z, Byun WS, Hinshaw SM, Sarott RC, Fischer ES, Gray NS. bioRxiv. 2024​​
• HUWE1 Amplifies Ubiquitin Modifications to Broadly Stimulate Clearance of Proteins and Aggregates
  Zhou M, Fang R, Colson L, Donovan KA, Hunkeler M, Song Y, Zhang C, Chen S, Lee DH, Bradshaw GA, Eisert R, Ye Y, Kalocsay M, Goldberg A, Fischer ES,  Lu Y. bioRxiv 2023 May​

 2024

• The differential interactomes of the KRAS splice variants identify BIRC6 as a ubiquitin ligase for KRAS4A
  Kochen Rossi J, Nuevo-Tapioles C, O'Keefe RA, Hunkeler M, Schmoker AM, Fissore-O'Leary M, Su W, Ahearn IM, Branco C, Cheong H, Esposito D, Clotea I, Ueberheide B, Fischer ES, Philips MR. Cell Reports. 2025 Jan
• A Kinetic Scout Approach Accelerates Targeted Protein Degrader Development
  Fan AT, Gadbois GE, Huang HT, Chaudhry C, Jiang J, Sigua LH, Smith ER, Wu S, Poirier GJ, Dunne-Dombrink K, Goyal P, Tao AJ, Sellers WR, Fischer ES, Donovan KA, Ferguson FM. Angewandte Chemie International Edition. 2024 Nov
• Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library
  Razumkov H*, Jiang Z*, Baek K*, You I, Geng Q, Donovan KA, Tang MT, Metivier RJ, Mageed N, Seo P, Li Z, Byun WS, Hinshaw SM, Sarott RC, Fischer ES‡, Gray NS‡. Journal of American Chemical Society. 2024 Nov
• 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. European Journal of Medicinal Chemistry. 2024 Dec
• ​Discovery of Potent Degraders of the Dengue Virus Envelope Protein
  Li Z*, Liu HY*, He Z, Chakravarty A, Golden RP, Jiang Z, You I, Yue H, Donovan KA, Du G, Che J, Tse J, Che I, Lu W, Fischer ES, Zhang T, Gray NS‡, Yang PL‡. Advanced Science. 2024 Oct
• 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‡. Nature Chemical Biology. 2024 Dec
• Polymerization of ZBTB transcription factors regulates chromatin occupancy
   Park PMC*, Park J*, Brown J, Hunkeler M, Roy Burman SS, Donovan KA, Yoon H, Nowak RP, Słabicki M, Ebert BL‡, Fischer ES‡. Molecular Cell. 2024 July
• Preclinical efficacy of potent and selective menin-KMT2A inhibitor JNJ-75276617 in KMT2A- and NPM1-altered leukemias
  Kwon MC, Thuring JW, Querolle O, Dai X, Verhulst T, Pande V, Marien A, Goffin D, Wenge DV, Yue H, Cutler JA, Jin C, Perner F, Hogeling SM, Shaffer PL, Jacobs F, Vinken P, Cai W, Keersmaekers V, Eyassu F, Bhogal B, Verstraeten K, Ashkar SE, Perry JA, Jayaguru P, Barreyro L, Kuchnio A, Darville N, Krosky D, Urbanietz G, Verbist B, Edwards JP, Cowley GS, Kirkpatrick R, Steele R, Ferrante L, Guttke C, Daskalakis N, Pietsch EC, Wilson DM, Attar RM, Elsayed YA, Fischer ES, Schuringa JJ, Armstrong SA, Packman K, Philippar U. Blood. 2024 June
• Broad-spectrum activity against mosquito-borne flaviviruses achieved by a targeted protein degradation mechanism
  Liu HY*, Li Z*, Reindl T, He Z, Qiu X, Golden RP, Donovan KA, Bailey A, Fischer ES, Zhang T, Gray NS‡, Yang PL‡. Nature Communications. 2024 June
• Targeted protein degradation: from mechanisms to clinic
  Tsai JM, Nowak RP, Ebert BL, Fischer ES. Nature Reviews Molecular Cell Biology. 2024 April
• Structural characterization of methylation-independent PP2A assembly guides alphafold2Multimer prediction of family-wide PP2A complexes
  Wachter F, Nowak RP, Ficarro S, Marto J, Fischer ES.  Journal of Biological Chemistry. 2024 May
• Targeting DCAF5 suppresses SMARCB1-mutant cancer by stabilizing SWI/SNF
  Radko-Juettner S*, Yue H*, Myers JA, Carter RD, Robertson AN, Mittal P, Zhu Z, Hansen BS, Donovan KA, Hunkeler M, Rosikiewicz W, Wu Z, McReynolds MG, Roy Burman SS, Schmoker AM, Mageed N, Brown SA, Mobley RJ, Partridge JF, Stewart EA, Pruett-Miller SM, Nabet B, Peng J, Gray NS, Fischer ES, Roberts CWM. Nature. 2024 April
• Ubiquitin-specific proximity labeling for the identification of E3 ligase substrates
  Huang HT, Lumpkin RJ, Tsai RW, Su S, Zhao X, Xiong Y, Chen J, Mageed N, Donovan KA, Fischer ES Sellers WR. Nature Chemical Biology. 2024 March
• Continuous evolution of compact protein degradation tags regulated by selective molecular glues
  Mercer JAM, DeCarlo SJ, Roy Burman SS, Sreekanth V, Nelson AT, Hunkeler M, Chen PJ, Donovan KA, Kokkonda P, Tiwari PK, Shoba VM, Deb A, Choudhary A, Fischer ES, Liu DR. Science. 2024 March
• Multiomic profiling of breast cancer cells uncovers stress MAPK-associated sensitivity to AKT degradation
  Erickson EC, You I, Perry G, Dugourd A, Donovan KA, Crafter C, Johannes JW, Williamson S, Moss JI, Ros S, Ziegler RE, Barry ST, Fischer ES, Gray NS, Madsen RR, Toker A. Science Signaling. 2024 Feb
• Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators
  Liu Y, Nowak RP, Che J, Donovan KA, Huerta F, Liu H, Metivier RJ, Fischer ES, Jones LH. RCS Medicinal Chemistry. 2024 Jan
• HDAC6/aggresome processing pathway importance for inflammasome formation is context-dependent
  ​Wang L, Shi S, Unterreiner A, Kapetanovic R, Ghosh S, Sanchez J, Aslani S, Xiong Y, Hsu CL, Donovan KA, Farady CJ, Fischer ES,, Bornancin F, Matthias P. Journal of Biological Chemistry. 2024 Jan
• 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. Nature Chemistry. 2024 Feb

 

2023

• Mezigdomide is effective alone and in combination with Menin inhibition in pre-clinical models of KMT2A-r and NPM1c AML
  ​Bourgeois W, Cutler JA, Aubrey BJ, Wenge D, Perner F, Martucci C, Henrich JA, Klega K, Nowak RP, Donovan KA, Boileau M, Wen Y, Hatton C, Apazidis AA, Olsen SN, Kirmani N, Pikman Y, Pollard JA, Perry JA, Sperling AS, Ebert BL, McGeehan GM, Crompton BD, Fischer ES, Armstrong SA. Blood. 2023 Dec
• Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange
  ​Cruite JT, Nowak RP, Donovan KA, Ficarro SB, Huang H, Liu H, Liu Y, Marto JA, Metivier RJ, Fischer ES, Jones LH. ACS Medicinal Chemistry Letters. 2023 Oct
• Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead
  Nowak RP, Ragosta L, Huerta F, Liu H, Ficarro SB, Cruite JT, Metivier RJ, Donovan KA, Marto JA, Fischer ES, Zerfas BL, Jones LH. RCS Chemical Biology. 2023 Aug
• Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry
  Sarott RC, You I, Li YD, Toenjes ST, Donovan KA, Seo P, Ordonez M, Byun WS, Hassan MM, Wachter F, Chouchani ET, Słabicki M, Fischer ES,  Ebert BL, Hinshaw SM, Gray NS. Journal of the American Chemical Society. 2023 Oct
• TP63 fusions drive multicomplex enhancer rewiring, lymphomagenesis, and EZH2 dependence
  Wu G, Yoshida N, Liu J, Zhang X, Xiong Y, Heavican-Foral TB, Mandato E, Liu H, Nelson GM, Yang L, Chen R, Donovan KA, Jones MK, Roshal M, Zhang Y, Xu R, Nirmal AJ, Jain S, Leahy C, Jones KL, Stevenson KE, Galasso N, Ganesan N, Chang T, Wu WC, Louissaint A, Debaize L, Yoon H, Dal Cin P, Chan WC, Ho Sui SJ, Ng SY, Feldman AL, Horwitz SM, Adelman K, Fischer ES,  Chen CW, Weinstock DM, Brown M. Science Translational Medicine. 2023 Sep
• Design principles for cyclin K molecular glue degraders
  Kozicka Z, Suchyta DJ, Focht V, Kempf G, Petzold G, Jentzsch M, Zou C, Di Genua C, Donovan KA, Coomar S, Cigler M, Mayor-Ruiz C, Schmid-Burgk JL, Häussinger D, Winter GE, Fischer ES,, Słabicki M, Gillingham D, Ebert BL, Thomä NH. Nature Chemical Biology. 2023 Sep
• Proteomics-Based Discovery of First-in-Class Chemical Probes for Programmed Cell Death Protein 2 (PDCD2)
  Ji W, Byun WS, Lu W, Zhu X, Donovan KA, Dwyer BG, Che J, Yuan L, Abulaiti X, Corsello SM, Fischer ES,  Zhang T, Gray NS. Angewandte Chemie International Edition. 2023 Oct
• UBR5 forms ligand-dependent complexes on chromatin to regulate nuclear hormone receptor stability
  Tsai JM, Aguirre JD, Li YD, Brown J, Focht V, Kater L, Kempf G, Sandoval B, Schmitt S, Rutter JC, Galli P, Sandate CR, Cutler JA, Zou C, Donovan KA, Lumpkin RJ, Cavadini S, Park PMC, Sievers Q, Hatton C, Ener E, Regalado BD, Sperling MT, Słabicki M, Kim J, Zon R, Zhang Z, Miller PG, Belizaire R, Sperling AS, Fischer ES, Irizarry R, Armstrong SA, Thomä NH, Ebert BL. Molecular Cell. 2023 Aug
• HAPSTR1 localizes HUWE1 to the nucleus to limit stress signaling pathways
  ​Monda JK, Ge X, Hunkeler M, Donovan KA, Ma MW, Jin CY, Leonard M, Fischer ES, Bennett EJ. Cell Reports. 2023 May
• The human E3 ligase RNF185 is a regulator of the SARS-CoV-2 envelope protein
  Zou C, Yoon H, Park PMC, Patten JJ, Pellman J, Carreiro J, Tsai JM, Li YD, Roy Burman SS, Donovan KA, Gasser J, Sperling AS, Nowak RP, Fischer ES, Davey RA, Ebert BL, Słabicki M. iScience. 2023 May
• ​Development and characterization of selective FAK inhibitors and PROTACs with in vivo activity
  Koide E, Mohardt ML, Doctor ZM, Yang A, Hao M, Donovan KA, Kuismi CC, Nelson AJ, Abell K, Aguiar M, Che J, Stokes MP, Zhang T, Aguirre AJ, Fischer ES, Gray NS, Jiang B, Nabet B. ChemBioChem. 2023 Apr
• Diagnostic TR-FRET assays for detection of antibodies in patient samples
  Yue H, Nowak RP, Overwijn D, Payne NC, Fischinger S, Atyeo C, Lam EC, St Denis K, Brais LK, Konishi Y, Sklavenitis-Pistofidis R, Baden LR, Nilles EJ, Karlson EW, Yu XG, Li JZ, Woolley AE, Ghobrial IM, Meyerhardt JA, Balazs AB, Alter G, Mazitschek R, Fischer ES. Cell Reports Methods. 2023 Feb​
• Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions
  Gao Y, Jiang B, Kim H, Berberich MJ, Che J, Donovan KA, Hatcher JM, Huerta F, Kwiatkowski NP, Liu Y, Liuni PP, Metivier RJ, Murali VK, Nowak RP, Zhang T, Fischer ES, Gray NS, Jones LH. Journal of Medicinal Chemistry. 2023 Apr
• ITK degradation to block T cell receptor signaling and overcome therapeutic resistance in T cell lymphomas
  Jiang B, Weinstock DM, Donovan KA, Sun HW, Wolfe A, Amaka S, Donaldson NL, Wu G, Jiang Y, Wilcox RA, Fischer ES, Gray NS, Wu W. Cell Chemical Biology. 2023 Apr
• MEN1 mutations mediate clinical resistance to menin inhibition
  ​Perner F, Stein EM, Wenge DV, Singh S, Kim J, Apazidis A, Rahnamoun H, Anand D, Marinaccio C, Hatton C, Wen Y, Stone RM, Schaller D, Mowla S, Xiao W, Gamlen HA, Stonestrom AJ, Persaud S, Ener E, Cutler JA, Doench JG, McGeehan GM, Volkamer A, Chodera JD, Nowak RP, Fischer ES, Levine RL, Armstrong SA, Cai SF. Nature. 2023 Mar
• Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader
  Teng M, Jiang J, Wang ES, Geng Q, Toenjes ST, Donovan KA, Mageed N, Yue H, Nowak RP, Wang J, Manz TD, Fischer ES, Cantley LC, Gray NS. Angew Chem Int Ed Engl. 2023 Mar
• Structures of BIRC6-client complexes provide a mechanism of SMAC-mediated release of caspases​
  Hunkeler M, Jin CY, Fischer ES. Science. 2023 Feb
• E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance
  Hanzl A, Barone E, Bauer S, Yue H, Nowak RP, Hahn E, Pankevich EV, Koren A, Kubicek S, Fischer ES,  Winter GE. Journal of American Chemical Society. 2023 Jan
• 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. Nature. 2023 Jan
• Development of potent and selective degraders of PI5P4Kγ
  Ji W, Wang ES, Manz TD, Jiang J, Donovan KA, Abulaiti X, Fischer ES, Cantley LC, Zhang T, Gray NS.  European Journal of Medicinal Chemistry. 2023 Feb

 

2022

• Machine Learning Modeling of Protein-intrinsic Features Predicts Tractability of Targeted Protein Degradation
  ​Zhang W, Roy Burman SS, Chen J, Donovan KA, Cao Y, Zhang B, Zeng Z, Zhang Y, Li D, Fischer ES, Tokheim C. Genomics Proteomics Bioinformatics. 2022 Dec
• Development and Utility of a PAK1-Selective Degrader
  Chow HY, Karchugina S, Groendyke BJ, Toenjes S, Hatcher J, Donovan KA, Fischer ES, Abalakov G, Faezov B, Dunbrack R, Gray NS, Chernoff J. Journal of Medicinal Chemistry. 2022 Dec.
• Acute pharmacological degradation of ERK5 does not inhibit cellular immune response or proliferation
  You I, Donovan KA, Krupnick NM, Boghossian AS, Rees MG, Ronan MM, Roth JA, Fischer ES, Wang ES, Gray NS. Cell Chemical Biology. 2022 Nov
• A STUB1 ubiquitin ligase/CHIC2 protein complex negatively regulates the IL-3, IL-5, and GM-CSF cytokine receptor common β chain (CSF2RB) protein stability
  Koochaki SHJ, Słabicki M, Lumpkin R, Zou C, Belizaire R, Fischer ES, Ebert BL. Journal of Biological Chemistry. 2022 Oct
• Exploring the target scope of KEAP1 E3 ligase-based PROTACs
  Du G, Jiang J, Henning NJ, Safaee N, Koide E, Nowak RP, Donovan KA, Yoon H, You I, Yue H, Eleuteri NA, He Z, Li Z, Huang HT, Che J, Nabet B, Zhang T, Fischer ES, Gray NS.  Cell Chemical Biology. 2022 Oct
• Redirecting the Neo-Substrate Specificity of Cereblon-Targeting PROTACs to Helios
  Verano AL, You I, Donovan KA, Mageed N, Yue H, Nowak RP, Fischer ES, Wang ES, Gray NS. ACS Chemical Biology. 2022 Sep
• Cereblon covalent modulation through structure-based design of histidine targeting chemical probes
  Cruite JT, Dann GP, Che J, Donovan KA, Ferrao S, Ficarro SB, Fischer ES, Gray NS, Huerta F, Kong NR, Liu H, Marto JA, Metivier RJ, Nowak RP, Zerfas BL, Jones LH. RCS Chemical Biology. 2022 July
• Temporal resolution of gene derepression and proteome changes upon PROTAC-mediated degradation of BCL11A protein in erythroid cells
  Mehta S, Buyanbat A, Kai Y, Karayel O, Goldman SR, Seruggia D, Zhang K, Fujiwara Y, Donovan KA, Zhu Q, Yang H, Nabet B, Gray NS, Mann M, FIscher ES, Adelman K, Orkin SH. Cell Chemical Biology. 2022 Aug
• Allosteric inhibition of PPM1D serine/threonine phosphatase via an altered conformational state
  ​Miller PG, Sathappa M, Moroco JA, Jiang W, Qian Y, Iqbal S, Guo Q, Giacomelli AO, Shaw S, Vernier C, Bajrami B, Yang X, Raffier C, Sperling AS, Gibson CJ, Kahn J, Jin C, Ranaghan M, Caliman A, Brousseau M, Fischer ES, Lintner R, Piccioni F, Campbell AJ, Root DE, Garvie CW, Ebert BL. Nature Communications. 2022 Jun
• Allosteric inhibition of PPM1D serine/threonine phosphatase via an altered conformational state
  ​Miller PG*, Sathappa M*, Moroco JA*, Jiang W, Qian Y, Iqbal S, Guo Q, Giacomelli AO, Shaw S, Vernier C, Bajrami B, Yang X, Raffier C, Sperling AS, Gibson CJ, Kahn J, Jin C, Ranaghan M, Caliman A, Brousseau M, Fischer ES, Lintner R, Piccioni F, Campbell AJ, Root DE, Garvie CW, Ebert BL. Nature Communications. 2022 Jun
• Degradation of GSPT1 causes TP53-independent cell death in leukemia whilst sparing normal hematopoietic stem cells
  Sellar RS, Sperling AS, Słabicki M, Gasser JA, McConkey ME, Donovan KA, Mageed N, Adams DN, Zou C, Miller PG, Dutta RK, Boettcher S, Lin AE, Sandoval BE, Quevedo Barrios VA, Shkolnik V, Koeppel J, Henderson EK, Fink EC, Yang L, Chan AK, Pokharel SP, Bergstrom EJ, Burt R, Udeshi ND, Carr SA, Fischer ES, Chen CW, Ebert BL. The Journal of Clinical Investigation. 2022 Jun
• IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia
  Aubrey BJ*, Cutler JA*, Bourgeois W*, Donovan KA, Gu S, Hatton C, Perlee S, Perner F, Rahnamoun H, Theall ACP, Henrich JA, Zhu Q, Nowak RP, Kim YJ, Parvin S, Cremer A, Olsen SN, Eleuteri NA, Pikman Y, McGeehan GM, Stegmaier K, Letai A, Fischer ES, Liu XS, Armstrong SA. Nature Cancer. 2022 May
• BTBBCL6 dimers as building blocks for reversible drug-induced protein oligomerization
  Nitsch L, Jensen P, Yoon H, Koeppel J, Roy Burman SS, Fischer ES, Scholl C, Fröhling S, Słabicki M. Cell Reports Methods. 2022 Apr 13
• Serological testing for SARS-CoV-2 antibodies of employees shows low transmission working in a cancer center
  Meyerhardt JA, Yue H, Nowak RP, Brais L, Ma C, Johnson S, Harrod J, Roy Burman SS, Hendrickson LM, Fischinger S, Alter G, Hahn W, Johnson BE, Fischer ES. PLoS One. 2022 Apr 12
• Small molecule modulation of protein polymerization
  Fischer ES, Jones LH. Chemical Society reviews. 2022 Apr 4
• Discovery and Optimization of Tau Targeted Protein Degraders Enabled by Patient Induced Pluripotent Stem Cells-Derived Neuronal Models of Tauopathy
  Silva MC, Nandi G, Donovan KA, Cai Q, Berry BC, Nowak RP, Fischer ES, Gray NS, Ferguson FM, Haggarty SJ. Frontiers in Cellular Neuroscience. 2022 Mar 3
• Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216
  ​Teng M, Lu W, Donovan KA, Sun J, Krupnick NM, Nowak RP, Li YD, Sperling AS, Zhang T, Ebert BL, Fischer ES, Gray NS.  Journal of Medicinal Chemistry.  2022 Jan 13
• Attenuated response to SARS-CoV-2 vaccine in patients with asymptomatic precursor stages of multiple myeloma and Waldenstrom macroglobulinemia
  ​Konishi Y, Sklavenitis-Pistofidis R, Yue H, Ferrari F, Redd RA, Lightbody ED, Russo M, Perry J, Horowitz E, Justis AV, Shayegh NA, Savell A, Prescott J, Varmeh S, Nowak RP, Hamilton M, Auclair D, Marinac CR, Trippa L, Fischer ES, Ghobrial IM. Cancer Cell. 2022 Jan 10

 

 2021

• Overcoming IMiD Resistance in T-cell Lymphomas Through Potent Degradation of ZFP91 and IKZF1
  Wu W, Nelson G, Koch R, Donovan KA, Nowak RP, Heavican-Foral TB, Nirmal AJ, Liu H, Yang L, Duffy J, Powers F, Stevenson KE, Jones M, Ng SY, Wu G, Jain S, Xu R, Amaka S, Trevisani C, Donaldson N, Hagner PR, de Leval L, Gaulard P, Iqbal J, Thakurta A, Fischer ES, Adelman K, Weinstock DM. Blood. 2021 Dec 22
• Early cross-coronavirus reactive signatures of humoral immunity against COVID-19
  Kaplonek P, Wang C, Bartsch Y, Fischinger S, Gorman MJ, Bowman K, Kang J, Dayal D, Martin P, Nowak RP, Villani AC, Hsieh CL, Charland NC, Gonye ALK, Gushterova I, Khanna HK, LaSalle TJ, Lavin-Parsons KM, Lilley BM, Lodenstein CL, Manakongtreecheep K, Margolin JD, McKaig BN, Rojas-Lopez M, Russo BC, Sharma N, Tantivit J, Thomas MF, Sade-Feldman M, Feldman J, Julg B, Nilles EJ, Musk ER, Menon AS, Fischer ES, McLellan JS, Schmidt A, Goldberg MB, Filbin MR, Hacohen N, Lauffenburger DA, Alter G. Science Immunology. 2021 Oct 15
• INK4 tumor suppressor proteins mediate resistance to CDK4/6 kinase inhibitors
  Li Q*, Jiang B*, Guo J*, Shao H, Del Priore IS, Chang Q, Kudo R, Li Z, Razavi P, Liu B, Boghossian AS, Rees MG, Ronan MM, Roth JA, Donovan KA, Palafox M, Reis-Filho JS, de Stanchina E, Fischer ES, Rosen N, Serra V, Koff A, Chodera JD, Gray NS, Chandarlapaty S. Cancer Discovery. 2021 Sep 20
• Selective degradation-inducing probes for studying cereblon (CRBN) biology
  Powell CE, Du G, Bushman JW, He Z, Zhang T, Fischer ES, Gray NS. RSC Medicinal Chemistry. 2021 Jul 6
• Methods for Quantitative Assessment of Protein Degradation
  Nowak RP, Yue H, Park EY, Fischer ES. Methods Molecular Biology. 2021
• Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development.
  Teng M, Jiang J, Ficarro SB, Seo HS, Bae JH, Donovan KA, Fischer ES, Zhang T, Dhe-Paganon S, Marto JA‡, Gray NS‡. ACS Medicinal Chemistry Letters. 2021 Jul 21
• Targeted Degradation of the Oncogenic Phosphatase SHP2.
  Vemulapalli V, Donovan KA, Seegar TCM, Rogers JM, Bae M, Lumpkin RJ, Cao R, Henke MT, Ray SS, Fischer ES, Cuny GD, Blacklow SC. Biochemistry. 2021 Aug 31
• METTL1-mediated m7G modification of Arg-TCT tRNA drives oncogenic transformation.
  Orellana EA, Liu Q, Yankova E, Pirouz M, De Braekeleer E, Zhang W, Lim J, Aspris D, Sendinc E, Garyfallos DA, Gu M, Ali R, Gutierrez A, Mikutis S, Bernardes GJL, Fischer ES, Bradley A, Vassiliou GS, Slack FJ, Tzelepis K, Gregory RI.  Molecular Cell. 2021 Jul 29
• TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma.
  Seong BKA, Dharia NV, Lin S, Donovan KA, Chong S, Robichaud A, Conway A, Hamze A, Ross L, Alexe G, Adane B, Nabet B, Ferguson FM, Stolte B, Wang EJ, Sun J, Darzacq X, Piccioni F, Gray NS, Fischer ES, Stegmaier K. Cancer Cell. 2021 Jul 22
• Solenoid architecture of HUWE1 contributes to ligase activity and substrate recognition.
  Hunkeler M, Jin CY, Ma MW, Monda JK, Overwijn D, Bennett EJ, Fischer ES. Molecular Cell. 2021 Jul 16
• Chemo-proteomics exploration of HDAC degradability by small molecule degraders.
  Xiong Y*, Donovan KA*, Eleuteri NA, Kirmani N, Yue H, Razov A, Krupnick NM, Nowak RP, Fischer ES. Cell Chemical Biology. 2021 Jul 15
• Structure-Guided Design of a “Bump-and-Hole” Bromodomain-Based Degradation Tag.
  Nowak RP*, Xiong Y*, Kirmani N, Kalabathula J, Donovan KA, Eleuteri NA, Yuan JC, Fischer ES.  Journal of Medicinal Chemistry. 2021 Jul 19
• Selective degradation-inducing probes for studying cereblon (CRBN) biology.
  Powell CE*, Du G*, Bushman JW*, He Z, Zhang T, Fischer ES, Gray NS. RSC Medicinal Chemistry. 2021 Jul 6
• Acute pharmacological degradation of Helios destabilizes regulatory T cells. Wang ES*, Verano AL*, Nowak RP*, Yuan JC*, Donovan KA, Eleuteri NA, Yue H, Ngo KH, Lizotte PH, Gokhale PC, Gray NS‡, Fischer ES‡. Nature Chemical Biology. 2021 May 25
• Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2. Du G, Jiang J, Wu Q, Henning NJ, Donovan KA, Yue H, Che J, Lu W, Fischer ES,Bardeesy N, Zhang T, Gray NS. Angewandte Chemie International Edition. 2021 April 29
• A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders. Fischer PD, Papadopoulos E, Dempersmier JM, Wang ZF, Nowak RP, Donovan KA, Kalabathula J, Gorgulla C, Junghanns PPM, Kabha E, Dimitrakakis N, Petrov OI, Mitsiades C, Ducho C, Gelev V, Fischer ES, Wagner G, Arthanari H. European Journal Medicinal Chemistry. 2021 Jul 5
• Local Deuteration Enables NMR Observation of Methyl Groups in Proteins from Eukaryotic and Cell-Free Expression Systems. Dubey A, Stoyanov N, Viennet T, Chhabra S, Elter S, Borggräfe J, Viegas A, Nowak RP, Burdzhiev N, Petrov O, Fischer ES, Etzkorn M, Gelev V, Arthanari H. Angewandte Chemie International Edition. 2021 March 26
• Humoral signatures of protective and pathological SARS-CoV-2 infection in children. Bartsch YC, Wang C, Zohar T, Fischinger S, Atyeo C, Burke JS, Kang J, Edlow AG, Fasano A, Baden LR, Nilles EJ, Woolley AE, Karlson EW, Hopke AR, Irimia D, Fischer ES, Ryan ET, Charles RC, Julg BD, Lauffenburger DA, Yonker LM, Alter G. Nature Medicine. 2021 Feb 12.
• Targeting oncoproteins with a positive selection assay for protein degraders. Koduri V, Duplaquet L, Lampson BL, Wang AC, Sabet AH, Ishoey M, Paulk J, Teng M, Harris IS, Endress JE, Liu X, Dasilva E, Paulo JA, Briggs KJ, Doench JG, Ott CJ, Zhang T, Donovan KA, Fischer ES, Gygi SP, Gray NS, Bradner J, Medin JA, Buhrlage SJ, Oser MG, Kaelin WG Jr. Science Advances. 2021 Feb 5
• Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins
  Shirasaki R, Matthews GM, Gandolfi S, de Matos Simoes R, Buckley DL, Raja Vora J, Sievers QL, Brüggenthies JB, Dashevsky O, Poarch H, Tang H, Bariteau MA, Sheffer M, Hu Y, Downey-Kopyscinski SL, Hengeveld PJ, Glassner BJ, Dhimolea E, Ott CJ, Zhang T, Kwiatkowski NP, Laubach JP, Schlossman RL, Richardson PG, Culhane AC, Groen RWJ, Fischer ES, Vazquez F, Tsherniak A, Hahn WC, Levy J, Auclair D, Licht JD, Keats JJ, Boise LH, Ebert BL, Bradner JE, Gray NS, Mitsiades CS. Cell Reports. 2021 Jan 5

 

 2020

• Small-Molecule Approaches to Targeted Protein Degradation
  Faust TB*, Donovan KA*, Yue H, Chamberlain PP‡, Fischer ES‡. Annual Review Cancer Biology. 2020 Dec 8.
• Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development.
  Donovan KA*, Ferguson FM*, Bushman JB, 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‡, Gray NS‡, Fischer ES‡. Cell. 2020 Dec 3.
• 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‡. Nature. 2020 Nov 18.
• Proteomics-Based Identification of DUB Substrates Using Selective Inhibitors
  Bushman JW, Donovan KA, Schauer NJ, Liu X, Hu W, Varca AC, Buhrlage SJ, Fischer ES.  Cell Chemical Biology. 2020 Oct 1.
• Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library
  Powell CE, Du G, Che J, He Z, Donovan KA, Yue H, Wang ES, Nowak RP, Zhang T, Fischer ES, Gray NS.. ACS Chemical Biology. 2020 Aug 31.
• 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 International Edition. 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 International Edition. 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 International Edition. 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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