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Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
Wittlinger F, Heppner DE, To C, Günther M, Shin BH, Rana JK, Schmoker AM, Beyett TS, Berger LM, Berger BT, Bauer N, Vasta JD, Corona CR, Robers MB, Knapp S, Jänne PA, Eck MJ, Laufer SA. Wittlinger F, et al. Among authors: vasta jd. J Med Chem. 2022 Jan 27;65(2):1370-1383. doi: 10.1021/acs.jmedchem.1c00848. Epub 2021 Oct 20. J Med Chem. 2022. PMID: 34668706 Free PMC article.
Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.
Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB. Vasta JD, et al. Cell Chem Biol. 2018 Feb 15;25(2):206-214.e11. doi: 10.1016/j.chembiol.2017.10.010. Epub 2017 Nov 22. Cell Chem Biol. 2018. PMID: 29174542 Free PMC article.
Collagen Prolyl 4-Hydroxylase as a Therapeutic Target.
Vasta JD, Raines RT. Vasta JD, et al. J Med Chem. 2018 Dec 13;61(23):10403-10411. doi: 10.1021/acs.jmedchem.8b00822. Epub 2018 Jul 23. J Med Chem. 2018. PMID: 29986141 Free PMC article. Review.
Binding Kinetics Survey of the Drugged Kinome.
Georgi V, Schiele F, Berger BT, Steffen A, Marin Zapata PA, Briem H, Menz S, Preusse C, Vasta JD, Robers MB, Brands M, Knapp S, Fernández-Montalván A. Georgi V, et al. Among authors: vasta jd. J Am Chem Soc. 2018 Nov 21;140(46):15774-15782. doi: 10.1021/jacs.8b08048. Epub 2018 Nov 6. J Am Chem Soc. 2018. PMID: 30362749
Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.
Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, Fedorov O, Raynaud F, Donovan A, Blagg J, Bavetsias V, Oppermann U, Bountra C, Kawamura A, Brennan PE. Vazquez-Rodriguez S, et al. Among authors: vasta jd. Angew Chem Int Ed Engl. 2019 Jan 8;58(2):515-519. doi: 10.1002/anie.201810179. Epub 2018 Dec 7. Angew Chem Int Ed Engl. 2019. PMID: 30431220 Free PMC article.
A High-Throughput BRET Cellular Target Engagement Assay Links Biochemical to Cellular Activity for Bruton's Tyrosine Kinase.
Ong LL, Vasta JD, Monereau L, Locke G, Ribeiro H, Pattoli MA, Skala S, Burke JR, Watterson SH, Tino JA, Meisenheimer PL, Arey B, Lippy J, Zhang L, Robers MB, Tebben A, Chaudhry C. Ong LL, et al. Among authors: vasta jd. SLAS Discov. 2020 Feb;25(2):176-185. doi: 10.1177/2472555219884881. Epub 2019 Nov 9. SLAS Discov. 2020. PMID: 31709883 Free article.
Quantifying Target Occupancy of Small Molecules Within Living Cells.
Robers MB, Friedman-Ohana R, Huber KVM, Kilpatrick L, Vasta JD, Berger BT, Chaudhry C, Hill S, Müller S, Knapp S, Wood KV. Robers MB, et al. Among authors: vasta jd. Annu Rev Biochem. 2020 Jun 20;89:557-581. doi: 10.1146/annurev-biochem-011420-092302. Epub 2020 Mar 24. Annu Rev Biochem. 2020. PMID: 32208767 Review.
Discovery of a selective inhibitor of doublecortin like kinase 1.
Ferguson FM, Nabet B, Raghavan S, Liu Y, Leggett AL, Kuljanin M, Kalekar RL, Yang A, He S, Wang J, Ng RWS, Sulahian R, Li L, Poulin EJ, Huang L, Koren J, Dieguez-Martinez N, Espinosa S, Zeng Z, Corona CR, Vasta JD, Ohi R, Sim T, Kim ND, Harshbarger W, Lizcano JM, Robers MB, Muthaswamy S, Lin CY, Look AT, Haigis KM, Mancias JD, Wolpin BM, Aguirre AJ, Hahn WC, Westover KD, Gray NS. Ferguson FM, et al. Among authors: vasta jd. Nat Chem Biol. 2020 Jun;16(6):635-643. doi: 10.1038/s41589-020-0506-0. Epub 2020 Apr 6. Nat Chem Biol. 2020. PMID: 32251410 Free PMC article.
31 results