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Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis.
Sugawara T, Nevedomskaya E, Heller S, Böhme A, Lesche R, von Ahsen O, Grünewald S, Nguyen HM, Corey E, Baumgart SJ, Georgi V, Pütter V, Fernández-Montalván A, Vasta JD, Robers MB, Politz O, Mumberg D, Haendler B. Sugawara T, et al. Among authors: vasta jd. Mol Oncol. 2024 Mar;18(3):726-742. doi: 10.1002/1878-0261.13577. Epub 2024 Jan 15. Mol Oncol. 2024. PMID: 38225213 Free PMC article.
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.
Quantifying CDK inhibitor selectivity in live cells.
Wells CI, Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Ingold MR, Pickett JE, Drewry DH, Pugh KM, Schwinn MK, Hwang BB, Zegzouti H, Huber KVM, Cong M, Meisenheimer PL, Willson TM, Robers MB. Wells CI, et al. Among authors: vasta jd. Nat Commun. 2020 Jun 2;11(1):2743. doi: 10.1038/s41467-020-16559-0. Nat Commun. 2020. PMID: 32488087 Free PMC article.
KRAS is vulnerable to reversible switch-II pocket engagement in cells.
Vasta JD, Peacock DM, Zheng Q, Walker JA, Zhang Z, Zimprich CA, Thomas MR, Beck MT, Binkowski BF, Corona CR, Robers MB, Shokat KM. Vasta JD, et al. Nat Chem Biol. 2022 Jun;18(6):596-604. doi: 10.1038/s41589-022-00985-w. Epub 2022 Mar 21. Nat Chem Biol. 2022. PMID: 35314814 Free PMC article.
31 results