Gray, Nathanael S.

Fragment-based covalent ligand discovery

Lu, W., Kostic, M., Zhang, T., Che, J., Patricelli, M. P., Jones, L. H., Chouchani, E. T., & Gray, N. S. (2021) · RSC Chemical Biology

Click Chemistry and ApplicationsChemical Synthesis and Analysis

Cited by 136

Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C

Zeng, M., Lu, J., Li, L., Feru, F., Quan, C., Gero, T. W., Ficarro, S. B., Xiong, Y., Ambrogio, C., Paranal, R. M., et al. (2017) · Cell Chemical Biology

Protein Kinase Regulation and GTPase SignalingQuinazolinone synthesis and applications

Cited by 136

HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib

Yang, G., Buhrlage, S. J., Tan, L., Liu, X., Chen, J., Xu, L., Tsakmaklis, N., Chen, J. G., Patterson, C. J., Brown, J. R., et al. (2016) · Blood

Chronic Lymphocytic Leukemia ResearchLymphoma Diagnosis and Treatment

Cited by 135

Acute pharmacological degradation of Helios destabilizes regulatory T cells

Wang, E. S., Verano, A. L., Nowak, R. P., Yuan, J. C., Donovan, K. A., Eleuteri, N. A., Yue, H., Ngo, K. H., Lizotte, P. H., Gokhale, P. C., et al. (2021) · Nature Chemical Biology

Protein Degradation and InhibitorsT-cell and B-cell Immunology

Cited by 124

Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins

Shirasaki, R., Matthews, G. M., Gandolfi, S., de Matos Simoes, R., Buckley, D. L., Raja Vora, J., Sievers, Q. L., Brüggenthies, J. B., Dashevsky, O., Poarch, H., et al. (2021) · Cell Reports

Protein Degradation and InhibitorsUbiquitin and proteasome pathways

Cited by 123

Development of Selective Covalent Janus Kinase 3 Inhibitors

Tan, L., Akahane, K., McNally, R., Reyskens, K. M. S. E., Ficarro, S. B., Liu, S., Herter-Sprie, G. S., Koyama, S., Pattison, M. J., Labella, K., et al. (2015) · Journal of Medicinal Chemistry

Cytokine Signaling Pathways and InteractionsHeterocyclic Compound Synthesis and Bioactivity

Cited by 122

Genome-Wide CRISPR Screens Identify Multiple Synthetic Lethal Targets That Enhance KRASG12C Inhibitor Efficacy

Mukhopadhyay, S., Huang, H.-Y., Lin, Z., Ranieri, M., Li, S., Sahu, S., Liu, Y., Ban, Y., Guidry, K., Hu, H., et al. (2023) · Cancer Research

Lung Cancer Treatments and MutationsProtein Kinase Regulation and GTPase Signaling

Cited by 105

Systematic analysis of BRAFV600E melanomas reveals a role for JNK/c‐Jun pathway in adaptive resistance to drug‐induced apoptosis

Fallahi‐Sichani, M., Moerke, N. J., Niepel, M., Zhang, T., Gray, N. S., & Sorger, P. K. (2015) · Molecular Systems Biology

Melanoma and MAPK PathwaysProtein Kinase Regulation and GTPase Signaling

Cited by 99

Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers

Sulahian, R., Kwon, J. J., Walsh, K. H., Pailler, E., Bosse, T. L., Thaker, M., Almanza, D., Dempster, J. M., Pan, J., Piccioni, F., et al. (2019) · Cell Reports

Melanoma and MAPK PathwaysProtein Kinase Regulation and GTPase Signaling

Cited by 90

BTKCys481Ser drives ibrutinib resistance via ERK1/2 and protects BTKwild-type MYD88-mutated cells by a paracrine mechanism

Chen, J. G., Liu, X., Munshi, M., Xu, L., Tsakmaklis, N., Demos, M. G., Kofides, A., Guerrera, M. L., Chan, G. G., Patterson, C. J., et al. (2018) · Blood

Chronic Lymphocytic Leukemia ResearchLymphoma Diagnosis and Treatment

Cited by 88

A high-throughput immune-oncology screen identifies EGFR inhibitors as potent enhancers of antigen-specific cytotoxic T-lymphocyte tumor cell killing

Lizotte, P. H., Hong, R.-L., Luster, T. A., Cavanaugh, M. E., Taus, L. J., Wang, S., Dhaneshwar, A., Mayman, N., Yang, A., Kulkarni, M., et al. (2018) · Cancer Immunology Research

Cancer Immunotherapy and BiomarkersImmunotherapy and Immune Responses

Cited by 88

Defining and Targeting Adaptations to Oncogenic KRASG12C Inhibition Using Quantitative Temporal Proteomics

Santana-Codina, N., Chandhoke, A. S., Yu, Q., Małachowska, B., Kuljanin, M., Gikandi, A., Stańczak, M., Gableske, S., Jedrychowski, M. P., Scott, D. A., et al. (2020) · Cell Reports

Protein Kinase Regulation and GTPase SignalingAdvanced Proteomics Techniques and Applications

Cited by 77

Covalent disruptor of YAP-TEAD association suppresses defective Hippo signaling

Fan, M., Lu, W., Che, J., Kwiatkowski, N. P., Gao, Y., Seo, H.-S., Ficarro, S. B., Gokhale, P. C., Liu, Y., Geffken, E. A., et al. (2022) · eLife

Hippo pathway signaling and YAP/TAZCancer-related molecular mechanisms research

Cited by 68

Covalent Guanosine Mimetic Inhibitors of G12C KRAS

Xiong, Y., Lu, J., Hunter, J., Li, L., Scott, D., Choi, H. G., Lim, S. M., Manandhar, A., Gondi, S., Sim, T., et al. (2017) · ACS Medicinal Chemistry Letters

Protein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

Cited by 66

Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216

Teng, M., Lu, W., Donovan, K. A., Sun, J., Krupnick, N. M., Nowak, R. P., Li, Y.-D., Sperling, A. S., Zhang, T., Ebert, B. L., et al. (2022) · Journal of Medicinal Chemistry

Protein Degradation and InhibitorsChemical Synthesis and Analysis

Cited by 63

Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5

Gilbert, A. S., Seoane, P. I., Sephton-Clark, P., Bojarczuk, A., Hotham, R., Giurisato, E., Sarhan, A. R., Hillen, A., Velde, G. V., Gray, N. S., et al. (2017) · Science Advances

Cellular transport and secretionFungal Infections and Studies

Cited by 54

Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library

Razumkov, H., Jiang, Z., Baek, K., You, I., Geng, Q., Donovan, K. A., Tang, M. T., Metivier, R. J., Mageed, N., Seo, P., et al. (2024) · Journal of the American Chemical Society

Protein Degradation and InhibitorsChemical Synthesis and Analysis

Cited by 53

Targeting oncoproteins with a positive selection assay for protein degraders

Koduri, V., Duplaquet, L., Lampson, B. L., Wang, A. C., Sabet, A. H., Ishoey, M., Paulk, J., Teng, M., Harris, I. S., Endress, J. E., et al. (2021) · Science Advances

Protein Degradation and InhibitorsUbiquitin and proteasome pathways

Cited by 44

Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine

Du, G., Rao, S., Gurbani, D., Henning, N. J., Jiang, J., Che, J., Yang, A., Ficarro, S. B., Marto, J. A., Aguirre, A. J., et al. (2020) · Journal of Medicinal Chemistry

Heterocyclic Compound Synthesis and BioactivityProtein Kinase Regulation and GTPase Signaling

Cited by 39

Gemcitabine and Chk1 Inhibitor AZD7762 Synergistically Suppress the Growth of Lkb1-Deficient Lung Adenocarcinoma

Liu, Y., Li, Y., Wang, X., Liu, F., Gao, P., Quinn, M. M., Li, F., Merlino, A. A., Benes, C., Liu, Q., et al. (2017) · Cancer Research

Lung Cancer Treatments and MutationsDNA Repair Mechanisms

Cited by 33

Structure and Characterization of a Covalent Inhibitor of Src Kinase

Gurbani, D., Du, G., Henning, N. J., Rao, S., Bera, A. K., Zhang, T., Gray, N. S., & Westover, K. D. (2020) · Frontiers in Molecular Biosciences

Protein Kinase Regulation and GTPase SignalingCancer Mechanisms and Therapy

Cited by 29

A small molecule PTER-selective inhibitor reduces food intake and body weight

Fu, S., Wang, L., Li, V. L., Lyu, X., Wei, W., Shi, X., Deng, S., Barber, J. L., Tahir, U. A., Adams, C., et al. (2026) · Cell Chemical Biology

Regulation of Appetite and ObesityPharmacology and Obesity Treatment

Cited by 2

A small molecule PTER-selective inhibitor reduces food intake and body weight

Fu, S., Wang, L., Li, V. L., Lyu, X., Wei, W., Shi, X., Deng, S., Barber, J. L., Tahir, U. A., Adams, C., et al. (2026) · Cell chemical biology

Regulation of Appetite and ObesityPharmacology and Obesity Treatment

Cited by 2