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Page 1
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: lingel a. Nat Chem Biol. 2017 Apr;13(4):381-388. doi: 10.1038/nchembio.2304. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135235
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
Lingel A, Sendzik M, Huang Y, Shultz MD, Cantwell J, Dillon MP, Fu X, Fuller J, Gabriel T, Gu J, Jiang X, Li L, Liang F, McKenna M, Qi W, Rao W, Sheng X, Shu W, Sutton J, Taft B, Wang L, Zeng J, Zhang H, Zhang M, Zhao K, Lindvall M, Bussiere DE. Lingel A, et al. J Med Chem. 2017 Jan 12;60(1):415-427. doi: 10.1021/acs.jmedchem.6b01473. Epub 2017 Jan 3. J Med Chem. 2017. PMID: 27992714
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: lingel a. PLoS One. 2017 Jan 10;12(1):e0169855. doi: 10.1371/journal.pone.0169855. eCollection 2017. PLoS One. 2017. PMID: 28072869 Free PMC article.
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
Huang Y, Zhang J, Yu Z, Zhang H, Wang Y, Lingel A, Qi W, Gu J, Zhao K, Shultz MD, Wang L, Fu X, Sun Y, Zhang Q, Jiang X, Zhang J, Zhang C, Li L, Zeng J, Feng L, Zhang C, Liu Y, Zhang M, Zhang L, Zhao M, Gao Z, Liu X, Fang D, Guo H, Mi Y, Gabriel T, Dillon MP, Atadja P, Oyang C. Huang Y, et al. Among authors: lingel a. J Med Chem. 2017 Mar 23;60(6):2215-2226. doi: 10.1021/acs.jmedchem.6b01576. Epub 2017 Feb 6. J Med Chem. 2017. PMID: 28092155
Two Distinct Mechanisms of Inhibition of LpxA Acyltransferase Essential for Lipopolysaccharide Biosynthesis.
Han W, Ma X, Balibar CJ, Baxter Rath CM, Benton B, Bermingham A, Casey F, Chie-Leon B, Cho MK, Frank AO, Frommlet A, Ho CM, Lee PS, Li M, Lingel A, Ma S, Merritt H, Ornelas E, De Pascale G, Prathapam R, Prosen KR, Rasper D, Ruzin A, Sawyer WS, Shaul J, Shen X, Shia S, Steffek M, Subramanian S, Vo J, Wang F, Wartchow C, Uehara T. Han W, et al. Among authors: lingel a. J Am Chem Soc. 2020 Mar 4;142(9):4445-4455. doi: 10.1021/jacs.9b13530. Epub 2020 Feb 17. J Am Chem Soc. 2020. PMID: 32064871
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Huang Y, Sendzik M, Zhang J, Gao Z, Sun Y, Wang L, Gu J, Zhao K, Yu Z, Zhang L, Zhang Q, Blanz J, Chen Z, Dubost V, Fang D, Feng L, Fu X, Kiffe M, Li L, Luo F, Luo X, Mi Y, Mistry P, Pearson D, Piaia A, Scheufler C, Terranova R, Weiss A, Zeng J, Zhang H, Zhang J, Zhao M, Dillon MP, Jeay S, Qi W, Moggs J, Pissot-Soldermann C, Li E, Atadja P, Lingel A, Oyang C. Huang Y, et al. Among authors: lingel a. J Med Chem. 2022 Apr 14;65(7):5317-5333. doi: 10.1021/acs.jmedchem.1c02148. Epub 2022 Mar 30. J Med Chem. 2022. PMID: 35352560
Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.
Moreau RJ, Skepper CK, Appleton BA, Blechschmidt A, Balibar CJ, Benton BM, Drumm JE 3rd, Feng BY, Geng M, Li C, Lindvall MK, Lingel A, Lu Y, Mamo M, Mergo W, Polyakov V, Smith TM, Takeoka K, Uehara K, Wang L, Wei JR, Weiss AH, Xie L, Xu W, Zhang Q, de Vicente J. Moreau RJ, et al. Among authors: lingel a. J Med Chem. 2018 Apr 26;61(8):3309-3324. doi: 10.1021/acs.jmedchem.7b01691. Epub 2018 Apr 9. J Med Chem. 2018. PMID: 29498517
Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity.
Skepper CK, Moreau RJ, Appleton BA, Benton BM, Drumm JE 3rd, Feng BY, Geng M, Hu C, Li C, Lingel A, Lu Y, Mamo M, Mergo W, Mostafavi M, Rath CM, Steffek M, Takeoka KT, Uehara K, Wang L, Wei JR, Xie L, Xu W, Zhang Q, de Vicente J. Skepper CK, et al. Among authors: lingel a. J Med Chem. 2018 Apr 26;61(8):3325-3349. doi: 10.1021/acs.jmedchem.7b01861. Epub 2018 Apr 13. J Med Chem. 2018. PMID: 29551072
Discovery of a selective and biologically active low-molecular weight antagonist of human interleukin-1β.
Hommel U, Hurth K, Rondeau JM, Vulpetti A, Ostermeier D, Boettcher A, Brady JP, Hediger M, Lehmann S, Koch E, Blechschmidt A, Yamamoto R, Tundo Dottorello V, Haenni-Holzinger S, Kaiser C, Lehr P, Lingel A, Mureddu L, Schleberger C, Blank J, Ramage P, Freuler F, Eder J, Bornancin F. Hommel U, et al. Among authors: lingel a. Nat Commun. 2023 Sep 7;14(1):5497. doi: 10.1038/s41467-023-41190-0. Nat Commun. 2023. PMID: 37679328 Free PMC article.
45 results