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Page 1
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.
Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelais G, DiDonato M, Bursulaya B, Michellys PY, Epple R, Marsilje TH, McNeill M, Lu W, Harris J, Bender S, Wong KK, Jänne PA, Eck MJ. Jia Y, et al. Among authors: didonato m. Nature. 2016 Jun 2;534(7605):129-32. doi: 10.1038/nature17960. Epub 2016 May 25. Nature. 2016. PMID: 27251290 Free PMC article.
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY. Lelais G, et al. Among authors: didonato m. J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19. J Med Chem. 2016. PMID: 27433829
EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.
Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Pferdekamper AC, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, DiDonato M, Bursulaya B, Lelais G, Barretina J, McNeill M, Epple R, Marsilje TH, Pathan N, Engelman JA, Michellys PY, McNamara P, Harris J, Bender S, Kasibhatla S. Jia Y, et al. Among authors: didonato m. Cancer Res. 2016 Mar 15;76(6):1591-602. doi: 10.1158/0008-5472.CAN-15-2581. Epub 2016 Jan 29. Cancer Res. 2016. PMID: 26825170
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
Liu YA, Jin Q, Zou Y, Ding Q, Yan S, Wang Z, Hao X, Nguyen B, Zhang X, Pan J, Mo T, Jacobsen K, Lam T, Wu TY, Petrassi HM, Bursulaya B, DiDonato M, Gordon WP, Liu B, Baaten J, Hill R, Nguyen-Tran V, Qiu M, Zhang YQ, Kamireddy A, Espinola S, Deaton L, Ha S, Harb G, Jia Y, Li J, Shen W, Schumacher AM, Colman K, Glynne R, Pan S, McNamara P, Laffitte B, Meeusen S, Molteni V, Loren J. Liu YA, et al. Among authors: didonato m. J Med Chem. 2020 Mar 26;63(6):2958-2973. doi: 10.1021/acs.jmedchem.9b01624. Epub 2020 Feb 20. J Med Chem. 2020. PMID: 32077280
Inhibition of DYRK1A and GSK3B induces human β-cell proliferation.
Shen W, Taylor B, Jin Q, Nguyen-Tran V, Meeusen S, Zhang YQ, Kamireddy A, Swafford A, Powers AF, Walker J, Lamb J, Bursalaya B, DiDonato M, Harb G, Qiu M, Filippi CM, Deaton L, Turk CN, Suarez-Pinzon WL, Liu Y, Hao X, Mo T, Yan S, Li J, Herman AE, Hering BJ, Wu T, Martin Seidel H, McNamara P, Glynne R, Laffitte B. Shen W, et al. Among authors: didonato m. Nat Commun. 2015 Oct 26;6:8372. doi: 10.1038/ncomms9372. Nat Commun. 2015. PMID: 26496802 Free PMC article.
A Dual Inhibitor of DYRK1A and GSK3β for β-Cell Proliferation: Aminopyrazine Derivative GNF4877.
Liu YA, Jin Q, Ding Q, Hao X, Mo T, Yan S, Zou Y, Huang Z, Zhang X, Gao W, Wu TY, Li C, Bursalaya B, Di Donato M, Zhang YQ, Deaton L, Shen W, Taylor B, Kamireddy A, Harb G, Li J, Jia Y, Schumacher AM, Laffitte B, Glynne R, Pan S, McNamara P, Molteni V, Loren J. Liu YA, et al. ChemMedChem. 2020 Aug 19;15(16):1562-1570. doi: 10.1002/cmdc.202000183. Epub 2020 Jul 2. ChemMedChem. 2020. PMID: 32613743
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
Hur W, Velentza A, Kim S, Flatauer L, Jiang X, Valente D, Mason DE, Suzuki M, Larson B, Zhang J, Zagorska A, Didonato M, Nagle A, Warmuth M, Balk SP, Peters EC, Gray NS. Hur W, et al. Among authors: didonato m. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9. doi: 10.1016/j.bmcl.2008.07.062. Epub 2008 Jul 18. Bioorg Med Chem Lett. 2008. PMID: 18667312 Free PMC article.
Advances in high-throughput methodologies for crystallizing proteins.
Chamberlain PP, Klock HE, McMullan D, DiDonato M, Kreusch A, Lesley SA, Spraggon G. Chamberlain PP, et al. Among authors: didonato m. Biotechnol Genet Eng Rev. 2006;23:1-19. doi: 10.1080/02648725.2006.10648075. Biotechnol Genet Eng Rev. 2006. PMID: 22530499 Review. No abstract available.
76 results