[1]
|
Hawkins, T. and Kihara, D. (2007) Function Prediction of Uncharacterized Proteins. Journal of Bioinformatics and Computational Biology, 5, 1-30. https://doi.org/10.1142/S0219720007002503
|
[2]
|
Cruz L.M., Trefflich, S., Weiss, V.A. and Castro, M.A.A. (2017) Protein Function Prediction. In: Kaufmann, M., Klinger, C. and Savelsbergh, A., Eds., Functional Genomics, Humana Press, New York, 55-75.
https://doi.org/10.1007/978-1-4939-7231-9_5
|
[3]
|
Parada, L.F., Tabin, C.J., Shih, C. and Weinberg, R.A. (1982) Human EJ Bladder Carcinoma Oncogene Is Homologue of Harvey Sarcoma Virus Ras Gene. Nature, 297, 474-478. https://doi.org/10.1038/297474a0
|
[4]
|
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. and Westover, K.D. (2014) In Situ Selectivity Profiling and Crystal Structure of SML-8-73-1, an Active Site Inhibitor of Oncogenic K-Ras G12C. Proceedings of the National Academy of Sciences of the United States of America, 111, 8895-8900. https://doi.org/10.1073/pnas.1404639111
|
[5]
|
Hunter J.C., Manandhar, A., Carrasco, M.A., Gurbani, D., Gondi, S. and Westover, K.D. (2015) Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations. Molecular Cancer Research, 13, 1325-1335.
https://doi.org/10.1158/1541-7786.MCR-15-0203
|
[6]
|
McGee, J.H., Shim, S.Y., Lee, S.J., Swanson, P.K., Jiang, S.Y., Durney, M.A. and Verdine, G.L. (2018) Exceptionally High-Affinity Ras Binders That Remodel Its Effector Domain. The Journal of Biological Chemistry, 293, 3265-3280.
https://doi.org/10.1074/jbc.M117.816348
|
[7]
|
Kauke, M.J., Traxlmayr, M.W., Parker, J.A., Kiefer, J.D., Knihtila, R., McGee, J., Verdine, G., Mattos, C. and Wittrup, K.D. (2017) An Engineered Protein Antagonist of K-Ras/B-Raf Interaction. Scientific Reports, 7, Article No. 5831.
https://doi.org/10.1038/s41598-017-05889-7
|
[8]
|
Dhirendra, K.S., Dwight, V.N. and Frank, M. (2017) RAS Proteins and Their Regulators in Human Disease. Cell, 170, 17-33. https://doi.org/10.1016/j.cell.2017.06.009
|
[9]
|
Lu, S.Y., Jang, H., Gu, S., Zhang, J. and Nussinov, R. (2016) Drugging Ras GTPase: A Comprehensive Mechanistic and Signaling Structural View. Chemical Society Reviews, 45, 4929-4952. https://doi.org/10.1039/C5CS00911A
|
[10]
|
Maurer, T., Garrenton, L.S., Oh, A., Pitts, K., Anderson, D.J., Skelton, N.J., Fauber, B.P., Pan, B., Malek, S., Stokoe, D., Ludlam, M.J.C., Bowman, K.K., Wu, J.S., Giannetti, A.M., Starovasnik, M.A., Mellman, I., Jackson, P.K., Rudolph, J., Wang, W.R. and Fang, G.W. (2012) Small-Molecule Ligands Bind to a Distinct Pocket in Ras and Inhibit SOS-Mediated Nucleotide Exchange Activity. Proceedings of the National Academy of Sciences of the United States of America, 109, 5299-5304.
|
[11]
|
Hillig, R.C., Sautier, B., Schroeder, J., Moosmayer, D., Hilpmann, A., Stegmann, C.M., Werbeck, N.D., Briem, H., Boemer, U., Weiske, J., Badock, V., Mastouri, J., Petersen, K., Siemeister, G., Kahmann, J.D., Wegener, D., Böhnke, N., Eis, K., Graham, K., Wortmann, L., von Nussbaum, F. and Bader, B. (2019) Discovery of Potent SOS1 Inhibitors That Block RAS Activation via Disruption of the RAS-SOS1 Interaction. Proceedings of the National Academy of Sciences of the United States of America, 116, 2551-2560. https://doi.org/10.1073/pnas.1812963116
|
[12]
|
李歆, 王义俊, 刘平羽. 特异靶向KRAS-G12C突变的抗肿瘤药物研究进展[J]. 药学学报, 2021, 56(2): 374-382.
https://doi.org/10.16438/j.0513-4870.2020-1485
|
[13]
|
Mukhopadhyay, S., Vander, H.M.G. and McCormick, F. (2021) The Metabolic Landscape of RAS-Driven Cancers from Biology to Therapy. Nature Cancer, 2, 271-283. https://doi.org/10.1038/s43018-021-00184-x
|
[14]
|
Schubbert, S., Shannon, K. and Bollag, G. (2007) Hyperactive Ras in Developmental Disorders and Cancer. Nature Reviews Cancer, 7, 295-308. https://doi.org/10.1038/nrc2109
|
[15]
|
Liu, P.Y., Wang, Y.J. and Li, X. (2019) Targeting the Untargetable KRAS in Cancer Therapy. Acta Pharmaceutica Sinica B, 9, 871-879. https://doi.org/10.1016/j.apsb.2019.03.002
|
[16]
|
Douglas, H. and Robert, A.W. (2011) Hallmarks of Cancer: The Next Generation. Cell, 144, 646-674.
https://doi.org/10.1016/j.cell.2011.02.013
|
[17]
|
Pylayeva-Gupta, Y., Grabocka, E. and Bar-Sagi, D. (2011) RAS Oncogenes: Weaving a Tumorigenic Web. Nature Reviews Cancer, 11, 761-774. https://doi.org/10.1038/nrc3106
|
[18]
|
Ying, H.Q., Kimmelman, A.C., Lyssiotis, C.A., Hua, S.J., Chu, G.C., Fletcher-Sananikone, E., Locasale, J.W., Son, J., Zhang, H.L., Coloff, J.L., Yan, H.Y., Wang, W., Chen, S.J., Viale, A., Zheng, H.W., Paik, J., Lim, C., Guimaraes, A.R., Martin, E.S., Chang, J., Hezel, A.F., Perry, S.R., Hu, J., Gan, B.Y., Xiao, Y.H., Asara, J.M., Weissleder, R., Wang, Y.A., Chin, L., Cantley, L.C. and DePinho, R.A. (2012) Oncogenic Kras Maintains Pancreatic Tumors through Regulation of Anabolic Glucose Metabolism. Cell, 149, 656-670. https://doi.org/10.1016/j.cell.2012.01.058
|
[19]
|
Weijzen, S., Velders, M.P. and Kast, W.M. (1999) Modulation of the Immune Response and Tumor Growth by Activated Ras. Leukemia, 13, 502-513. https://doi.org/10.1038/sj.leu.2401367
|
[20]
|
Patricelli, M.P., Janes, M.R., Li, L.S., Hansen, R., Peters, U., Kessler, L.V., Chen, Y., Kucharski, J.M., Feng, J., Ely, T., Chen, J.H., Firdaus, S.J., Babbar, A., Ren, P.D. and Liu, Y. (2016) Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State. Cancer Discovery, 6, 316-329.
https://doi.org/10.1158/2159-8290.CD-15-1105
|
[21]
|
Bryant, K.L., Mancias, J.D., Kimmelman, A.C. and Der, C.J. (2014) KRAS: Feeding Pancreatic Cancer Proliferation. Trends in Biochemical Sciences, 39, 91-100. https://doi.org/10.1016/j.tibs.2013.12.004
|
[22]
|
Hofmann, M.H., Gerlach, D., Misale, S., Petronczki, M. and Kraut, N. (2022) Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants. Cancer Discovery, 12, 924-937.
https://doi.org/10.1158/2159-8290.c.6549598.v1
|
[23]
|
Haigis, K.M. (2017) KRAS Alleles: The Devil Is in the Detail. Trends in Cancer, 3, 686-697.
https://doi.org/10.1016/j.trecan.2017.08.006
|
[24]
|
Reck, M., Carbone, D.P., Garassino, M. and Barlesi, F. (2021) Targeting KRAS in Non-Small Cell Lung Cancer: Recent Progress and New Approaches. Annals of Oncology, 32, 1101-1110. https://doi.org/10.1016/j.annonc.2021.06.001
|
[25]
|
Sun, Q., Burke, J.P., Phan, J., Burns, M.C., Olejniczak, E.T., Waterson, A.G., Lee, T., Rossanese, O.W. and Fesik, S.W. (2012) Discovery of Small Molecules That Bind to K-Ras and Inhibit Sos-Mediated Activation. Angewandte Chemie International Edition, 51, 6140-6143. https://doi.org/10.1002/anie.201201358
|
[26]
|
Wu, H.Z., Xiao, J.Q., Xiao, S.S. and Cheng, Y. (2019) KRAS: A Promising Therapeutic Target for Cancer Treatment. Current Topics in Medicinal Chemistry, 19, 2081-2097. https://doi.org/10.2174/1568026619666190905164144
|
[27]
|
Ni, D., Li, X.Y., He, X.H., Zhang, H., Zhang, J. and Lu, S.Y. (2019) Drugging K-Ras G12C through Covalent Inhibitors: Mission Possible? Pharmacology and Therapeutics, 202, 1-17. https://doi.org/10.1016/j.pharmthera.2019.06.007
|
[28]
|
Gupta, A.K., Wang, X., Pagba, C.V., Prakash, P., Sarkar-Banerjee, S., Putkey, J. and Gorfe, A.A. (2019) Multi-Target, Ensemble-Based Virtual Screening Yields Novel Allosteric KRAS Inhibitors at High Success Rate. Chemical Biology & Drug Design, 94, 1441-1456. https://doi.org/10.1111/cbdd.13519
|
[29]
|
Huang, L.M., Guo, Z.X., Wang, F. and Fu, L.W. (2021) KRAS Mutation: From Undruggable to Druggable in Cancer. Signal Transduction and Targeted Therapy, 6, Article No. 386. https://doi.org/10.1038/s41392-021-00780-4
|
[30]
|
Yan, W.P., Markegard, E., Dharmaiah, S., Urisman, A., Drew, M., Esposito, D., Scheffzek, K., Nissley, D.V., McCormick, F. and Simanshu, D.K. (2020) Structural Insights into the SPRED1-Neurofibromin-KRAS Complex and Disruption of SPRED1-Neurofibromin Interaction by Oncogenic EGFR. Cell Reports, 32, Article ID: 107909.
https://doi.org/10.1016/j.celrep.2020.107909
|
[31]
|
Nnadi, C.I., Jenkins, M.L., Gentile, D.R., Bateman, L.A., Zaidman, D., Balius, T.E., Nomura, D.K., Burke, J.E., Shokat, K.M. and Nir, L. (2018) Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange. Journal of Chemical Information and Modeling, 58, 464-471. https://doi.org/10.1021/acs.jcim.7b00399
|
[32]
|
Kettle, J.G., Bagal, S.K., Bickerton, S., Bodnarchuk, M.S., Breed, J., Carbajo, R.J., Cassar, D.J., Chakraborty, A., Cosulich, S., Cumming, I., Davies, M., Eatherton, A., Evans, L., Feron, L., Fillery, S., Gleave, E.S., Goldberg, F.W., Harlfinger, S., Hanson, L., Howard, M., Howells, R., Jackson, A., Kemmitt, P., Kingston, J.K., Lamont, S., Lewis, H.J., Li, S., Liu, L., Ogg, D., Phillips, C., Polanski, R., Robb, G., Robinson, D., Ross, S., Smith, J.M., Tonge, M., Whiteley, R., Yang, J., Zhang, L. and Zhao, X. (2020) Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C. Journal of Medicinal Chemistry, 63, 4468-4483.
https://doi.org/10.1021/acs.jmedchem.9b01720
|
[33]
|
Dirk, K., Andreas, B., Jark, B., Gerhard, F., Sandra, D., Melanie, H., Barbara, M., Alexander, W.P. and McConnell, D.B. (2020) Drugging All RAS Isoforms with One Pocket. Future Medicinal Chemistry, 12, 1911-1923.
https://doi.org/10.4155/fmc-2020-0221
|
[34]
|
Hansen, R., Peters, U., Babbar, A., Chen, Y., Feng, J., Janes, M.R., Li, L.S., Ren, P., Liu, Y. and Zarrinkar, P.P. (2018) The Reactivity-Driven Biochemical Mechanism of Covalent KRASG12C Inhibitors. Nature Structural & Molecular Biology, 25, 454-462. https://doi.org/10.1038/s41594-018-0061-5
|
[35]
|
Goebel, L., Mueller, M.P., Goody, R.S. and Rauh, D. (2020) KRasG12C Inhibitors in Clinical Trials: A Short Historical Perspective. RSC Medicinal Chemistry, 11, 760-770. https://doi.org/10.1039/D0MD00096E
|
[36]
|
Ostrem, J.M.L. and Shokat, K.M. (2016) Direct Small-Molecule Inhibitors of KRAS: From Structural Insights to Mechanism-Based Design. Nature Reviews Drug Discovery, 15, 771-785. https://doi.org/10.1038/nrd.2016.139
|
[37]
|
Mishto, M., Mansurkhodzhaev, A., Ying, G., Bitra, A., Cordfunke, R.A., Henze, S., Paul, D., Sidney, J., Urlaub, H., Neefjes, J., Sette, A., Zajonc, D.M. and Liepe, J. (2019) An in Silico—in Vitro Pipeline Identifying an HLA-A*02: 01+ KRAS G12V+ Spliced Epitope Candidate for a Broad Tumor-Immune Response in Cancer Patients. Frontiers in Immunology, 10, Article 2572. https://doi.org/10.3389/fimmu.2019.02572
|
[38]
|
Kwan, A.K., Piazza, G.A., Keeton, A.B. and Leite, C.A. (2022) The Path to the Clinic: A Comprehensive Review on Direct KRASG12C Inhibitors. Journal of Experimental & Clinical Cancer Research, 41, Article No. 27.
https://doi.org/10.1186/s13046-021-02225-w
|
[39]
|
Cox, A.D., Fesik, S.W., Kimmelman, A.C., Luo, J. and Der, C.J. (2014) Drugging the Undruggable RAS: Mission Possible? Nature Reviews Drug Discovery, 13, 828-851. https://doi.org/10.1038/nrd4389
|
[40]
|
Désage, A.L., Léonce, C., Swalduz, A. and Ortiz, C.S. (2022) Targeting KRAS Mutant in Non-Small Cell Lung Cancer: Novel Insights into Therapeutic Strategies. Frontiers in Oncology, 12, Article 796832.
https://doi.org/10.3389/fonc.2022.796832
|
[41]
|
许俨钊, 文辉, 崔华清. KRAS抑制剂的研究进展[J]. 药学学报, 2021, 56(6): 1562-1570.
https://doi.org/10.16438/j.0513-4870.2020-1834
|
[42]
|
Bera, A.K., Lu, J., Lu, C., Li, L., Gondi, S., Yan, W., Nelson, A., Zhang, G. and Westover, K.D. (2020) GTP Hydrolysis Is Modulated by Arg34 in the RASopathy-Associated KRASP34R. Birth Defects Research, 112, 708-717.
https://doi.org/10.1002/bdr2.1647
|
[43]
|
Lu, J., Harrison, R.A., Li, L., Zeng, M., Gondi, S., Scott, D., Gray, N.S., Engen, J.R. and Westover, K.D. (2017) KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry. Structure, 25, 1442-1448.E3. https://doi.org/10.1016/j.str.2017.07.003
|
[44]
|
Ostrem, J.M., Peters, U., Sos, M.L., Wells, J.A. and Shokat, K.M. (2013) K-Ras (G12C) Inhibitors Allosterically Control GTP Affinity and Effector Interactions. Nature, 503, 548-551. https://doi.org/10.1038/nature12796
|
[45]
|
Janes, M.R., Zhang, J.C., Li, L.S., Hansen, R., Peters, U., Guo, X., Chen, Y.C., Babbar, A., Firdaus, S.J., Darjania, L., Feng, J., Chen, J.H., Li, S.W., Li, S.S., Long, Y.O., Thach, C., Liu, Y., Zarieh, A., Ely, T., Kucharski, J.M., Kessler, L.V., Wu, T., Yu, K., Wang, Y., Yao, Y., Deng, X.H., Zarrinkar, P.P., Brehmer, D., Dhanak, D., Lorenzi, M.V., Hu-Lowe, D., Patricelli, M.P., Ren, P. and Liu, Y. (2018) Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor. Cell, 172, 578-589.E17. https://doi.org/10.1016/j.cell.2018.01.006
|
[46]
|
Canon, J., Rex, K., Saiki, A.Y., Mohr, C., Cooke, K., Bagal, D., Gaida, K., Holt, T., Knutson, C.G., Koppada, N., Lanman, B.A., Werner, J., Rapaport, A.S., San, M.T., Ortiz, R., Osgood, T., Sun, J.R., Zhu, X., McCarter, J.D., Volak, L.P., Houk, B.E., Fakih, M.G., O’Neil, B.H., Price, T.J., Falchook, G.S., Desai, J., Kuo, J., Govindan, R., Hong, D.S., Ouyang, W., Henary, H., Arvedson, T., Cee, V.J. and Lipford, J.R. (2019) The Clinical KRAS(G12C) Inhibitor AMG 510 Drives Anti-Tumour Immunity. Nature, 575, 217-223. https://doi.org/10.1038/s41586-019-1694-1
|
[47]
|
Boike, L., Henning, N.J. and Nomura, D.K. (2022) Advances in Covalent Drug Discovery. Nature Reviews Drug Discovery, 21, 881-898. https://doi.org/10.1038/s41573-022-00542-z
|
[48]
|
Wang, H., Chi, L.L., Yu, F.Q., Dai, H.L., Gao, C., Si, X.J., Wang, Z.J., Liu, L.M., Zheng, J.X., Shan, L.H., Liu, H.M. and Zhang, Q.R. (2023) Annual Review of KRAS Inhibitors in 2022. European Journal of Medicinal Chemistry, 249, Article ID: 115124. https://doi.org/10.1016/j.ejmech.2023.115124
|