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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. Among authors: machleidt t. 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.
Target engagement and drug residence time can be observed in living cells with BRET.
Robers MB, Dart ML, Woodroofe CC, Zimprich CA, Kirkland TA, Machleidt T, Kupcho KR, Levin S, Hartnett JR, Zimmerman K, Niles AL, Ohana RF, Daniels DL, Slater M, Wood MG, Cong M, Cheng YQ, Wood KV. Robers MB, et al. Among authors: machleidt t. Nat Commun. 2015 Dec 3;6:10091. doi: 10.1038/ncomms10091. Nat Commun. 2015. PMID: 26631872 Free PMC article.
Engineered luciferase reporter from a deep sea shrimp utilizing a novel imidazopyrazinone substrate.
Hall MP, Unch J, Binkowski BF, Valley MP, Butler BL, Wood MG, Otto P, Zimmerman K, Vidugiris G, Machleidt T, Robers MB, Benink HA, Eggers CT, Slater MR, Meisenheimer PL, Klaubert DH, Fan F, Encell LP, Wood KV. Hall MP, et al. Among authors: machleidt t. ACS Chem Biol. 2012 Nov 16;7(11):1848-57. doi: 10.1021/cb3002478. Epub 2012 Aug 30. ACS Chem Biol. 2012. PMID: 22894855 Free PMC article.
Highly Potent Cell-Permeable and Impermeable NanoLuc Luciferase Inhibitors.
Walker JR, Hall MP, Zimprich CA, Robers MB, Duellman SJ, Machleidt T, Rodriguez J, Zhou W. Walker JR, et al. Among authors: machleidt t. ACS Chem Biol. 2017 Apr 21;12(4):1028-1037. doi: 10.1021/acschembio.6b01129. Epub 2017 Feb 22. ACS Chem Biol. 2017. PMID: 28195704
Real-time analysis of the binding of fluorescent VEGF165a to VEGFR2 in living cells: Effect of receptor tyrosine kinase inhibitors and fate of internalized agonist-receptor complexes.
Kilpatrick LE, Friedman-Ohana R, Alcobia DC, Riching K, Peach CJ, Wheal AJ, Briddon SJ, Robers MB, Zimmerman K, Machleidt T, Wood KV, Woolard J, Hill SJ. Kilpatrick LE, et al. Among authors: machleidt t. Biochem Pharmacol. 2017 Jul 15;136:62-75. doi: 10.1016/j.bcp.2017.04.006. Epub 2017 Apr 7. Biochem Pharmacol. 2017. PMID: 28392095 Free PMC article.
Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.
Dart ML, Machleidt T, Jost E, Schwinn MK, Robers MB, Shi C, Kirkland TA, Killoran MP, Wilkinson JM, Hartnett JR, Zimmerman K, Wood KV. Dart ML, et al. Among authors: machleidt t. ACS Med Chem Lett. 2018 Apr 16;9(6):546-551. doi: 10.1021/acsmedchemlett.8b00081. eCollection 2018 Jun 14. ACS Med Chem Lett. 2018. PMID: 29937980 Free PMC article.
72 results