An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer C To, TS Beyett, J Jang, WW Feng, M Bahcall, HM Haikala, BH Shin, ... Nature cancer 3 (4), 402-417, 2022 | 69 | 2022 |
Carboxylic acid derivatives of amlexanox display enhanced potency toward TBK1 and IKKε and reveal mechanisms for selective inhibition TS Beyett, X Gan, SM Reilly, L Chang, AV Gomez, AR Saltiel, ... Molecular pharmacology 94 (4), 1210-1219, 2018 | 39 | 2018 |
Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors TS Beyett, C To, DE Heppner, JK Rana, AM Schmoker, J Jang, ... Nature communications 13 (1), 2530, 2022 | 38 | 2022 |
Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno [2, 3-b] pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases … TS Beyett, X Gan, SM Reilly, AV Gomez, L Chang, JJG Tesmer, AR Saltiel, ... Bioorganic & medicinal chemistry 26 (20), 5443-5461, 2018 | 31 | 2018 |
Comprehensive functional evaluation of variants of fibroblast growth factor receptor genes in cancer IT Nakamura, S Kohsaka, M Ikegami, H Ikeuchi, T Ueno, K Li, TS Beyett, ... npj Precision Oncology 5 (1), 66, 2021 | 24 | 2021 |
Navigating the conformational landscape of G protein–coupled receptor kinases during allosteric activation XQ Yao, MC Cato, E Labudde, TS Beyett, JJG Tesmer, BJ Grant Journal of Biological Chemistry 292 (39), 16032-16043, 2017 | 23 | 2017 |
Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe TS Beyett, AE Fraley, E Labudde, D Patra, RC Coleman, A Eguchi, ... Proceedings of the National Academy of Sciences 116 (32), 15895-15900, 2019 | 22 | 2019 |
A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non–Small Cell Lung Cancer J Son, J Jang, TS Beyett, Y Eum, HM Haikala, A Verano, M Lin, ... Cancer research 82 (8), 1633-1645, 2022 | 20 | 2022 |
Design of a “two-in-one” mutant-selective epidermal growth factor receptor inhibitor that spans the orthosteric and allosteric sites F Wittlinger, DE Heppner, C To, M Günther, BH Shin, JK Rana, ... Journal of medicinal chemistry 65 (2), 1370-1383, 2021 | 18 | 2021 |
Structural basis for inhibition of mutant EGFR with lazertinib (YH25448) DE Heppner, F Wittlinger, TS Beyett, T Shaurova, DA Urul, B Buckley, ... ACS medicinal chemistry letters 13 (12), 1856-1863, 2022 | 13 | 2022 |
Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC TW Gero, DE Heppner, TS Beyett, C To, SC Azevedo, J Jang, T Bunnell, ... Bioorganic & medicinal chemistry letters 68, 128718, 2022 | 10 | 2022 |
Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib E Tkacik, K Li, G Gonzalez-Del Pino, BH Ha, J Vinals, E Park, TS Beyett, ... Journal of Biological Chemistry 299 (5), 2023 | 8 | 2023 |
Macrocyclization of quinazoline-based EGFR inhibitors leads to exclusive mutant selectivity for EGFR L858R and Del19 JA Amrhein, TS Beyett, WW Feng, A Krämer, J Weckesser, IK Schaeffner, ... Journal of medicinal chemistry 65 (23), 15679-15697, 2022 | 8 | 2022 |
Biochemical characterization of the interaction between KRAS and Argonaute 2 JJ Waninger, TS Beyett, VV Gadkari, RF Siebenaler, C Kenum, S Shankar, ... Biochemistry and Biophysics Reports 29, 101191, 2022 | 7 | 2022 |
Characterization of a hyperphosphorylated variant of G protein-coupled receptor kinase 5 expressed in E. coli TS Beyett, Q Chen, EJ Labudde, J Krampen, PV Sharma, JJG Tesmer Protein expression and purification 168, 105547, 2020 | 4 | 2020 |
Oncogenic K-Ras suppresses global miRNA function B Shui, TS Beyett, Z Chen, X Li, G La Rocca, WM Gazlay, MJ Eck, KS Lau, ... Molecular Cell 83 (14), 2509-2523. e13, 2023 | 3 | 2023 |
Structural elements that enable specificity for mutant EGFR kinase domains with next-generation small-molecule inhibitors. T Damghani, F Wittlinger, TS Beyett, MJ Eck, SA Laufer, DE Heppner | 3 | 2023 |
Examining molecular factors of inactive versus active bivalent EGFR inhibitors: A missing link in fragment-based drug design. F Wittlinger, BC Ogboo, CD Pham, IK Schaeffner, SP Chitnis, T Damghani, ... | 3 | 2023 |
Synthesis of deuterium‐labelled amlexanox and its metabolic stability against mouse, rat, and human microsomes X Gan, MW Wilson, TS Beyett, B Wen, D Sun, SD Larsen, JJG Tesmer, ... Journal of Labelled Compounds and Radiopharmaceuticals 62 (5), 202-208, 2019 | 3 | 2019 |
Molecular basis for targeting, inhibition, and receptor phosphorylation in the G protein-coupled receptor kinase 4 subfamily TS Beyett, SJ Bandekar, JJG Tesmer G Protein-Coupled Receptor Kinases, 59-74, 2016 | 3 | 2016 |