A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases MS Eram, Y Shen, MM Szewczyk, H Wu, G Senisterra, F Li, KV Butler, ... ACS chemical biology 11 (3), 772-781, 2016 | 243 | 2016 |
Therapeutic targeting of RNA splicing catalysis through inhibition of protein arginine methylation JY Fong, L Pignata, PA Goy, KC Kawabata, SCW Lee, CM Koh, D Musiani, ... Cancer cell 36 (2), 194-209. e9, 2019 | 217 | 2019 |
Pharmacologic modulation of RNA splicing enhances anti-tumor immunity SX Lu, E De Neef, JD Thomas, E Sabio, B Rousseau, M Gigoux, DA Knorr, ... Cell 184 (15), 4032-4047. e31, 2021 | 164 | 2021 |
Cancer selective target degradation by folate-caged PROTACs J Liu, H Chen, Y Liu, Y Shen, F Meng, HU Kaniskan, J Jin, W Wei Journal of the American Chemical Society 143 (19), 7380-7387, 2021 | 140 | 2021 |
A chemical biology toolbox to study protein methyltransferases and epigenetic signaling S Scheer, S Ackloo, TS Medina, M Schapira, F Li, JA Ward, AM Lewis, ... Nature communications 10 (1), 19, 2019 | 111 | 2019 |
EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis J Wang, X Yu, W Gong, X Liu, KS Park, A Ma, YH Tsai, Y Shen, T Onikubo, ... Nature cell biology 24 (3), 384-399, 2022 | 103 | 2022 |
A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models X Yu, D Li, J Kottur, Y Shen, HS Kim, KS Park, YH Tsai, W Gong, J Wang, ... Science translational medicine 13 (613), eabj1578, 2021 | 81 | 2021 |
Discovery of a potent, selective, and cell-active dual inhibitor of protein arginine methyltransferase 4 and protein arginine methyltransferase 6 Y Shen, MM Szewczyk, MS Eram, D Smil, HU Kaniskan, ... Journal of medicinal chemistry 59 (19), 9124-9139, 2016 | 80 | 2016 |
Harnessing the E3 ligase KEAP1 for targeted protein degradation J Wei, F Meng, KS Park, H Yim, J Velez, P Kumar, L Wang, L Xie, H Chen, ... Journal of the American Chemical Society 143 (37), 15073-15083, 2021 | 79 | 2021 |
Discovery of First-in-class Protein Arginine Methyltransferase 5 (PRMT5) Degraders Y Shen, G Gao, X Yu, HS Kim, L Wang, L Xie, M Schwarz, X Chen, ... Journal of Medicinal Chemistry, 63 (17), 9977-9989, 2020 | 70 | 2020 |
PRMT1-mediated FLT3 arginine methylation promotes maintenance of FLT3-ITD+ acute myeloid leukemia X He, Y Zhu, YC Lin, M Li, J Du, H Dong, J Sun, L Zhu, H Wang, Z Ding, ... Blood, The Journal of the American Society of Hematology 134 (6), 548-560, 2019 | 66 | 2019 |
PRMT inhibition induces a viral mimicry response in triple-negative breast cancer Q Wu, DY Nie, W Ba-Alawi, YS Ji, ZW Zhang, J Cruickshank, J Haight, ... Nature chemical biology 18 (8), 821-830, 2022 | 52 | 2022 |
Discovery of G protein-biased D2 dopamine receptor partial agonists X Chen, JD McCorvy, MG Fischer, KV Butler, Y Shen, BL Roth, J Jin Journal of medicinal chemistry 59 (23), 10601-10618, 2016 | 52 | 2016 |
Smad6 methylation represses NFκB activation and periodontal inflammation T Zhang, J Wu, N Ungvijanpunya, O Jackson-Weaver, Y Gou, J Feng, ... Journal of Dental Research 97 (7), 810-819, 2018 | 44 | 2018 |
AKT degradation selectively inhibits the growth of PI3K/PTEN pathway–mutant cancers with wild-type KRAS and BRAF by destabilizing aurora kinase B J Xu, X Yu, TC Martin, A Bansal, K Cheung, A Lubin, E Stratikopoulos, ... Cancer discovery 11 (12), 3064-3089, 2021 | 40 | 2021 |
Design, synthesis, and evaluation of potent, selective, and bioavailable AKT kinase degraders X Yu, J Xu, L Xie, L Wang, Y Shen, KM Cahuzac, X Chen, J Liu, ... Journal of medicinal chemistry 64 (24), 18054-18081, 2021 | 32 | 2021 |
Discovery of a First-in-class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor Y Shen, F Li, MM Szewczyk, L Halabelian, K Park, I Chau, A Dong, ... Journal of Medicinal Chemistry 63 (10), 5477–5487, 2020 | 31 | 2020 |
Targeting PRMT1-mediated FLT3 methylation disrupts maintenance of MLL-rearranged acute lymphoblastic leukemia Y Zhu, X He, YC Lin, H Dong, L Zhang, X Chen, Z Wang, Y Shen, M Li, ... Blood, The Journal of the American Society of Hematology 134 (15), 1257-1268, 2019 | 31 | 2019 |
Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic D Li, X Yu, J Kottur, W Gong, Z Zhang, AJ Storey, YH Tsai, H Uryu, Y Shen, ... Oncogene 41 (24), 3328-3340, 2022 | 30 | 2022 |
Targeting triple-negative breast cancer by a novel proteolysis targeting chimera degrader of enhancer of zeste homolog 2 B Dale, C Anderson, KS Park, HU Kaniskan, A Ma, Y Shen, C Zhang, ... ACS Pharmacology & Translational Science 5 (7), 491-507, 2022 | 28 | 2022 |