Publications

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2021

F. M. Ferguson. Harnessing antibody-mimetic selectivity for activation state-specific targeted degradation of endogenous K-Ras. ACS Central Science, 2021, DOI: 10.1021/acscentsci.1c00084.

2013-2020

* Denotes equal contribution. # Denotes co-corresponding authors.

K. A. Donovan*, F. M. Ferguson*, J. W. Bushman, N. A. Eleuteri, D. Bhunia, S-S Ryu, L. Tan, K. Shi, D. Dobrovolsky, B. Jiang, J. Wang, M. Hao, I. You, M. Teng, Y. Liang, J. Hatcher, Z. Li, T. D. Manz, B. Groendyke, W. Hu, Y. Nam, S. Sengupta, H. Cho, I. Shin, J. Che, S. Buhrlage, T.B. Sim#, N. S. Gray#, E. S. Fischer#. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell, 2020, DOI: j.cell.2020.10.038.

Y. Liu, F. M. Ferguson, L. Li, M. Kuljanin, W. Harshbarger, S. Gondi, J. Wang, J. D. Mancias, N. S. Gray, K. D. Westover. Chemical biology toolkit for DCLK1 reveals connection to RNA processing. Cell Chem. Biol., 2020, DOI: 10.1016/j.chembiol.2020.07.011.

B. Nabet*, F. M. Ferguson*, B. K. A. Seong, M. Kuljanin, D. L. Buckley, A. L. Leggett, M. L. Mohardt, S. P. Gygi, J. D. Mancias, J. E. Bradner, K. Stegmaier, N. S. Gray. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat. Comms., 2020, 10.1038/s41467-020-18377-w.

F. M. Ferguson, Y. Liu, W. Harshbarger, L. Huang, J. Wang, S. J. Capuzzi, E. N. Muratov, A. Tropsha, X. Deng, S. Muthuswamy, K. D. Westover, N. S. Gray. Synthesis and structure activity relationships of DCLK1 kinase inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold. J. Med. Chem., 2020, DOI: 10.1021/acs.jmedchem.0c00596.

M. G. Jaeger, B. Schwalb, S. D. Mackowiak, T. Velychko, A. Hanzl, H. Imrichova, M. Brand, B. Agerer, S. Chorn, B. Nabet, F. M. Ferguson, A. C. Müller, A. Bergthaler, N. S. Gray, J. E. Bradner, C. Bock, D. Hnisz, P. Cramer#, G. E. Winter#. Mechanistic basis for selective Mediator-dependence of cell type-specifying transcription. Nat. Genetics, 2020, DOI: 10.1038/s41588-020-0635-0.

T. D. Manz*, S. C. Sivakumaren*, F. M. Ferguson, T. Zhang, A. Yasgar, M. D. Hall, M. I. Davis, H-S Seo, S. B. Ficarro, J. D. Card, H. Shim, A. T. Sasaki, M. D. Boxer, A. Simeonov, M. Shen, J. A. Marto, S. Dhe-Paganon, L. C. Cantley, N. S. Gray. Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. J. Med. Chem., 2020, DOI: 10.1021/acs.jmedchem.0c00227.

F. M. Ferguson*, B. Nabet*, S. Raghavan, Y. Liu, A. L. Leggett, M. Kuljanin, R. L. Kalekar, A. Yang, S. He, Ji. Wang, R. W. S. Ng, R. Sulahian, L. Li, E. J. Poulin, L. Huang, J. Koren, N. Dieguez-Martinez, S. Espinosa, Z. Zeng, C. R. Corona, J. D. Vasta, R. Ohi, T. Sim, N. D. Kim, W. Harshbarger, J. M. Lizcano, M. B. Robers, S. Muthaswamy, C. Y. Lin, A. T. Look, K. M. Haigis, J. D. Mancias, B. M. Wolpin, A. J. Aguirre, W. C. Hahn, K. D. Westover, N. S. Gray. Discovery of a selective inhibitor of Doublecortin Like Kinase 1. Nat. Chem. Biol., 2020, DOI: 10.1038/s41589-020-0506-0.

S. C. Sivakumaren*, H. Shim*, T. Zhang*, F. M. Ferguson, M. R. Lundquist, C. M. Browne, B. Jiang, M.-F. Hao, N. P. Kwiatkowski, S. B. Ficarro, M. N. Paddock, D. G. Wang, H.-S. Seo, T. D. Manz, T. J. Yang, P. Krishnan, J. M. Cunningham, S. Dhe-Paganon, J. A. Marto, L. C. Cantley, N. S. Gray. Targeting the PI5P4K lipid kinase family in cancer using novel covalent inhibitors., Cell Chem. Biol., 2020, DOI: 10.1016/j.chembiol.2020.02.003

T. D. Manz, S. C. Sivakumaren, S, A. Yasgar, Dhe-Paganon, M. D. Hall, M. I . Davis, H-S Seo, J. D. Card, S. B. Ficarro, H. Shim, J. A. Marto, S. Dhe-Paganon, A. T. Sasaki, M. B. Boxer, A. Simeonov, L. C. Cantley, M. Shen, T. Zhang#, F. M. Ferguson#, N. S. Gray#. Structure-Activity Relationship Study of Covalent Pan-Phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. ACS Med. Chem. Lett., 2019, DOI: 10.1021/acsmedchemlett.9b00402.

D. Remillard, D. L. Buckley, H.-S. Seo, F. M. Ferguson, S. Dhe-Paganon, J. E. Bradner, N. S. Gray. Dual inhibition of TAF1 and BRD4 Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. ACS Med. Chem. Lett., 2019, DOI: 10.1021/acsmedchemlett.9b00243.

F. M. Ferguson*, Z. M. Doctor*, S. Ficaro, N. D. Kim, T. Sim, N. S. Gray. Synthesis and structure activity analysis of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14. Bioorg. Med. Chem. Lett. 2019, DOI: 10.1016/j.bmcl.2019.05.024.

M. C. Silva*, F. M. Ferguson*, Q. Cai, K. A. Donovan, G. Nandi, D. Patnaik, T. Zhang, H.-T. Huang, D. E. Lucente, B. C. Dickerson, T. J. Mitchison, E. S. Fischer, N. S. Gray, S. J. Haggarty. Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. eLife, 2019, DOI: 10.7554/eLife.45457.

F. M. Ferguson*, Z. M. Doctor*, S. B. Ficaro, C. M. Browne, J. A. Marto, J. L. Johnson, T. M. Yaron, L. C. Cantley, N. D. Kim, T. Sim, M. J. Berberich, M. Kalocsay, P. K. Sorger, N. S. Gray. Discovery of covalent CDK14 inhibitors with pan-TAIRE family specificity., Cell Chem. Biol., 2019, DOI: 10.1016/j.chembiol.2019.02.015.

J. Wang, T. Erazo, F. M. Ferguson, D. L. Buckley, J. Zhang, X. Deng, J. Qi, W. Massefski, J. M. Roberts, P. Cohen, J. Bradner, J. M. Lizcano, S. C. Blacklow, X. Xu, N. S. Gray. Structural and atropisomeric factors governing the selectivity profile of pyrimido-benzodiazipinones as inhibitors of kinases and bromodomains., ACS Chem. Bio., 2018, DOI: 10.1021/acschembio.7b00638.

F. M. Ferguson and N. S. Gray. Kinase inhibitors: The road ahead. Nat. Rev. Drug Discov., 2018, DOI:10.1038/nrd.2018.21.

F. M. Ferguson*, Z. M. Doctor*, A. Chikuad, T. Sim, N. D. Kim, S. Knapp, N. S. Gray. Characterization of a highly selective inhibitor of the Aurora kinases., Bioorg. Med. Chem. Lett., 2017, DOI: 10.1016/j.bmcl.2017.08.016.

F. M. Ferguson, J. Ni, T. Zhang, B. Tesar, T. Sim, N. D. Kim, X. Deng, J. R. Brown, J. J. Zhao, N. S. Gray. Discovery of a series of 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as selective PI3K-δ/γ inhibitors., ACS Med. Chem. Lett., 2016, DOI: 10.1021/acsmedchemlett.6b00209.

C. Tallant, E. Valentini, O. Fedorov, L. Overvoorde, F. M. Ferguson, P. Filippakopoulos, D. Svergun, S. Knapp, A. Ciulli. Molecular basis of histone tail recognition by human TIP5 PHD finger and Bromodomain of the chromatin remodelling complex NoRC., Structure, 2015, DOI: 10.1016/j.str.2014.10.017.

M. Baud*, E. Lin Shiao*, T. Cardote*, C. Tallant, A. Pschibul, K-H. Chan, M. Zengerle, J. Rosello, T. Kwan, F. M. Ferguson, A. Ciulli. A Bump-and-Hole Approach to Engineer Controlled Selectivity of BET Bromodomain Chemical Probes., Science, 2014, DOI: 10.1126/science.1249830.

F. M. Ferguson, D. M. Dias, J. P. G. L. M. Rodrigues, H. Weink, R. Boelens, A. M. J. J. Bonvin, C. Abell, A. Ciulli. Binding Hotspots of BAZ2B Bromodomain: Histone Interaction Revealed by Solution NMR Driven Docking, Biochemistry, 2014, DOI: 10.1021/bi500909d.

F. M. Ferguson, O. Fedorov A. Chaikuad, M. Philpott, J. R. C. Muniz, I. Felletar, F. von Delft, T. Heightman, S. Knapp, C. Abell, A. Ciulli. Targeting Low Druggability Bromodomains: Fragment Based Inhibitor Design Against the BAZ2B Bromodomain, J. Med. Chem., 2013, DOI: 10.1021/jm401582c.