Gray, Nathanael S.

Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

Nabet, B., Ferguson, F. M., Seong, B. K. A., Kuljanin, M., Leggett, A. L., Mohardt, M. L., Robichaud, A., Conway, A. S., Buckley, D. L., Mancias, J. D., et al. (2020) · Nature Communications

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Therapeutic Targeting of Oncogenic K‐Ras by a Covalent Catalytic Site Inhibitor

Lim, S. M., Westover, K. D., Ficarro, S. B., Harrison, R. A., Choi, H. G., Pacold, M. E., Carrasco, M., Hunter, J., Kim, N. D., Xie, T., et al. (2014) · Angewandte Chemie International Edition

Protein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

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Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors.

Ercan, D., Xu, C., Yanagita, M., Monast, C. S., Pratilas, C. A., Montero, J., Butaney, M., Shimamura, T., Sholl, L., Ivanova, E. V., et al. (2012) · Cancer Discovery

Lung Cancer Treatments and MutationsHER2/EGFR in Cancer Research

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YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers

Galli, G. G., Carrara, M., Yuan, W.-C., Valdes-Quezada, C., Gurung, B., Pepe-Mooney, B., Zhang, T., Geeven, G., Gray, N. S., de Laat, W., et al. (2015) · Molecular Cell

Hippo pathway signaling and YAP/TAZGenomics and Chromatin Dynamics

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Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models

Silva, M. C., Ferguson, F. M., Cai, Q., Donovan, K. A., Nandi, G., Patnaik, D., Zhang, T., Huang, H.-T., Lucente, D. E., Dickerson, B. C., et al. (2019) · eLife

Alzheimer's disease research and treatmentsProtein Degradation and Inhibitors

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CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation

Krajewska, M., Dries, R., Grassetti, A. V., Dust, S., Gao, Y., Huang, H., Sharma, B., Day, D. S., Kwiatkowski, N., Pomaville, M., et al. (2019) · Nature Communications

RNA Research and SplicingGenomics and Chromatin Dynamics

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Exploring Targeted Degradation Strategy for Oncogenic KRASG12C

Zeng, M., Xiong, Y., Safaee, N., Nowak, R. P., Donovan, K. A., Yuan, C. J., Nabet, B., Gero, T. W., Feru, F., Li, L., et al. (2020) · Cell Chemical Biology

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Development of dual and selective degraders of cyclin-dependent kinases 4 and 6

Jiang, B., Wang, E. S., Donovan, K. A., Liang, Y., Fischer, E. S., Zhang, T., & Gray, N. S. (2019) · Angewandte Chemie International Edition

Protein Degradation and InhibitorsHistone Deacetylase Inhibitors Research

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Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML

Brand, M., Jiang, B., Bauer, S., Donovan, K. A., Liang, Y., Wang, E. S., Nowak, R. P., Yuan, J. C., Zhang, T., Kwiatkowski, N., et al. (2019) · Cell Chemical Biology

Protein Degradation and InhibitorsAcute Myeloid Leukemia Research

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Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1 H)-one as a Highly Potent, Selective Mammalian Target of Rapamycin (mTOR) Inhibitor for the Treatment of Cancer

Liu, Q., Chang, J. W., Wang, J., Kang, S. A., Thoreen, C. C., Markhard, A., Hur, W., Zhang, J., Sim, T., Sabatini, D. M., et al. (2010) · Journal of Medicinal Chemistry

PI3K/AKT/mTOR signaling in cancerHeterocyclic Compound Synthesis and Bioactivity

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In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C

Hunter, J. C., Gurbani, D., Ficarro, S. B., Carrasco, M. A., Lim, S. M., Choi, H. G., Xie, T., Marto, J. A., Chen, Z., Gray, N. S., et al. (2014) · Proceedings of the National Academy of Sciences

Protein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

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Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations

de Wispelaere, M., Du, G., Donovan, K. A., Zhang, T., Eleuteri, N. A., Yuan, J. C., Kalabathula, J., Nowak, R. P., Fischer, E. S., Gray, N. S., et al. (2019) · Nature Communications

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Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

Gechijian, L. N., Buckley, D. L., Lawlor, M. A., Reyes, J. M., Paulk, J., Ott, C. J., Winter, G. E., Erb, M. A., Scott, T. G., Xu, M., et al. (2018) · Nature Chemical Biology

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Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

Faust, T. B., Yoon, H., Nowak, R. P., Donovan, K. A., Li, Z., Cai, Q., Eleuteri, N. A., Zhang, T., Gray, N. S., & Fischer, E. S. (2020) · Nature Chemical Biology

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Pharmacological targeting of the pseudokinase Her3

Xie, T., Lim, S. M., Westover, K. D., Dodge, M. E., Ercan, D., Ficarro, S. B., Udayakumar, D., Gurbani, D., Tae, H. S., Riddle, S. M., et al. (2014) · Nature Chemical Biology

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Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

Powell, C. E., Gao, Y., Tan, L., Donovan, K. A., Nowak, R. P., Loehr, A., Bahcall, M., Fischer, E. S., Jänne, P. A., George, R. E., et al. (2018) · Journal of Medicinal Chemistry

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Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway.

Cortot, A. B., Repellin, C. E., Shimamura, T., Capelletti, M., Zejnullahu, K., Ercan, D., Christensen, J. G., Wong, K.-K., Gray, N. S., & Jänne, P. A. (2013) · Cancer Research

Lung Cancer Treatments and MutationsHER2/EGFR in Cancer Research

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Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation

Zhang, T., Hatcher, J. M., Teng, M., Gray, N. S., & Kostic, M. (2019) · Cell Chemical Biology

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EWS/FLI confers tumor cell synthetic lethality to CDK12 inhibition in Ewing sarcoma

Iniguez, A. B., Stolte, B., Wang, E. J., Conway, A. S., Alexe, G., Dharia, N. V., Kwiatkowski, N., Zhang, T., Abraham, B. J., Mora, J., et al. (2018) · Cancer Cell

Sarcoma Diagnosis and TreatmentPARP inhibition in cancer therapy

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Bruton tyrosine kinase degradation as a therapeutic strategy for cancer

Dobrovolsky, D., Wang, E. S., Morrow, S., Leahy, C., Faust, T., Nowak, R. P., Donovan, K. A., Yang, G., Li, Z., Fischer, E. S., et al. (2019) · Blood

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CDK13 cooperates with CDK12 to control global RNA polymerase II processivity

Fan, Z., Devlin, J. R., Hogg, S. J., Doyle, M. A., Harrison, P. F., Todorovski, I., Cluse, L. A., Knight, D. A., Sandow, J. J., Gregory, G., et al. (2020) · Science Advances

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Discovery and resistance mechanism of a selective CDK12 degrader

Jiang, B., Gao, Y., Che, J., Lu, W., Kaltheuner, I. H., Dries, R., Kalocsay, M., Berberich, M. J., Jiang, J., You, I., et al. (2021) · Nature Chemical Biology

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Inhibiting fungal multidrug resistance by disrupting an activator–Mediator interaction

Nishikawa, J. L., Boeszoermenyi, A., Vale-Silva, L. A., Torelli, R., Posteraro, B., Sohn, Y.-J., Ji, F., Gelev, V., Sanglard, D., Sanguinetti, M., et al. (2016) · Nature

Antifungal resistance and susceptibilityFungal and yeast genetics research

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ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1-mutant lung cancer

Deng, J., Thennavan, A., Dolgalev, I., Chen, T., Li, J., Marzio, A., Poirier, J. T., Peng, D. H., Bulatovic, M., Mukhopadhyay, S., et al. (2021) · Nature Cancer

Cancer Immunotherapy and BiomarkersAutophagy in Disease and Therapy

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