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Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation.
Qi W, Chan H, Teng L, Li L, Chuai S, Zhang R, Zeng J, Li M, Fan H, Lin Y, Gu J, Ardayfio O, Zhang JH, Yan X, Fang J, Mi Y, Zhang M, Zhou T, Feng G, Chen Z, Li G, Yang T, Zhao K, Liu X, Yu Z, Lu CX, Atadja P, Li E. Qi W, et al. Among authors: lin y. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5. doi: 10.1073/pnas.1210371110. Epub 2012 Dec 10. Proc Natl Acad Sci U S A. 2012. PMID: 23236167 Free PMC article.
Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED.
Li L, Zhang H, Zhang M, Zhao M, Feng L, Luo X, Gao Z, Huang Y, Ardayfio O, Zhang JH, Lin Y, Fan H, Mi Y, Li G, Liu L, Feng L, Luo F, Teng L, Qi W, Ottl J, Lingel A, Bussiere DE, Yu Z, Atadja P, Lu C, Li E, Gu J, Zhao K. Li L, et al. Among authors: lin y. PLoS One. 2017 Jan 10;12(1):e0169855. doi: 10.1371/journal.pone.0169855. eCollection 2017. PLoS One. 2017. PMID: 28072869 Free PMC article.
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.
Qi W, Zhao K, Gu J, Huang Y, Wang Y, Zhang H, Zhang M, Zhang J, Yu Z, Li L, Teng L, Chuai S, Zhang C, Zhao M, Chan H, Chen Z, Fang D, Fei Q, Feng L, Feng L, Gao Y, Ge H, Ge X, Li G, Lingel A, Lin Y, Liu Y, Luo F, Shi M, Wang L, Wang Z, Yu Y, Zeng J, Zeng C, Zhang L, Zhang Q, Zhou S, Oyang C, Atadja P, Li E. Qi W, et al. Among authors: lin y. Nat Chem Biol. 2017 Apr;13(4):381-388. doi: 10.1038/nchembio.2304. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135235
Upregulation of CD11b and CD86 through LSD1 inhibition promotes myeloid differentiation and suppresses cell proliferation in human monocytic leukemia cells.
Fang J, Ying H, Mao T, Fang Y, Lu Y, Wang H, Zang I, Wang Z, Lin Y, Zhao M, Luo X, Wang Z, Zhang Y, Zhang C, Xiao W, Wang Y, Tan W, Chen Z, Lu C, Atadja P, Li E, Zhao K, Liu J, Gu J. Fang J, et al. Among authors: lin y. Oncotarget. 2017 Jun 19;8(49):85085-85101. doi: 10.18632/oncotarget.18564. eCollection 2017 Oct 17. Oncotarget. 2017. PMID: 29156705 Free PMC article.
Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).
Kaniskan HÜ, Eram MS, Zhao K, Szewczyk MM, Yang X, Schmidt K, Luo X, Xiao S, Dai M, He F, Zang I, Lin Y, Li F, Dobrovetsky E, Smil D, Min SJ, Lin-Jones J, Schapira M, Atadja P, Li E, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Liu F, Yu Z, Vedadi M, Jin J. Kaniskan HÜ, et al. Among authors: lin jones j, lin y. J Med Chem. 2018 Feb 8;61(3):1204-1217. doi: 10.1021/acs.jmedchem.7b01674. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29244490 Free PMC article.
Discovery of Potent Small-Molecule Inhibitors of WDR5-MYC Interaction.
Ding J, Li G, Liu H, Liu L, Lin Y, Gao J, Zhou G, Shen L, Zhao M, Yu Y, Guo W, Hommel U, Ottl J, Blank J, Aubin N, Wei Y, He H, Sage DR, Atadja PW, Li E, Jain RK, Tallarico JA, Canham SM, Chiang YL, Wang H. Ding J, et al. Among authors: lin y. ACS Chem Biol. 2023 Jan 20;18(1):34-40. doi: 10.1021/acschembio.2c00843. Epub 2023 Jan 3. ACS Chem Biol. 2023. PMID: 36594833
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. Kaniskan HÜ, et al. Among authors: lin jones j, lin y. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. doi: 10.1002/anie.201412154. Epub 2015 Feb 27. Angew Chem Int Ed Engl. 2015. PMID: 25728001 Free PMC article.
DOT1L inhibition is lethal for multiple myeloma due to perturbation of the endoplasmic reticulum stress pathway.
Dafflon C, Gaulis S, Barys L, Kapur K, Cornacchione V, Schukur L, Bergling S, Traggiai E, Jansky S, Hellmann L, Engstler BS, Kerr G, de Weck A, Ruddy DA, Naumann U, Stauffer F, Gaul C, Lin Y, Billy E, Weiss A, Hofmann F, Ito M, Tiedt R. Dafflon C, et al. Among authors: lin y. Oncotarget. 2020 Mar 17;11(11):956-968. doi: 10.18632/oncotarget.27493. eCollection 2020 Mar 17. Oncotarget. 2020. PMID: 32215184 Free PMC article.
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