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Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)-Mixed Lineage Leukemia (MLL) Protein-Protein Interaction.
Karatas H, Li Y, Liu L, Ji J, Lee S, Chen Y, Yang J, Huang L, Bernard D, Xu J, Townsend EC, Cao F, Ran X, Li X, Wen B, Sun D, Stuckey JA, Lei M, Dou Y, Wang S. Karatas H, et al. Among authors: huang l. J Med Chem. 2017 Jun 22;60(12):4818-4839. doi: 10.1021/acs.jmedchem.6b01796. Epub 2017 Jun 12. J Med Chem. 2017. PMID: 28603984
Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.
Zhang M, Aguilar A, Xu S, Huang L, Chinnaswamy K, Sleger T, Wang B, Gross S, Nicolay BN, Ronseaux S, Harvey K, Wang Y, McEachern D, Kirchhoff PD, Liu Z, Stuckey J, Tron AE, Liu T, Wang S. Zhang M, et al. Among authors: huang l. J Med Chem. 2021 Jul 22;64(14):10333-10349. doi: 10.1021/acs.jmedchem.1c00789. Epub 2021 Jul 1. J Med Chem. 2021. PMID: 34196551 Free PMC article.
Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction.
Xu S, Aguilar A, Xu T, Zheng K, Huang L, Stuckey J, Chinnaswamy K, Bernard D, Fernández-Salas E, Liu L, Wang M, McEachern D, Przybranowski S, Foster C, Wang S. Xu S, et al. Among authors: huang l. Angew Chem Int Ed Engl. 2018 Feb 5;57(6):1601-1605. doi: 10.1002/anie.201711828. Epub 2018 Jan 15. Angew Chem Int Ed Engl. 2018. PMID: 29284071 Free article.
Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction.
Aguilar A, Zheng K, Xu T, Xu S, Huang L, Fernandez-Salas E, Liu L, Bernard D, Harvey KP, Foster C, McEachern D, Stuckey J, Chinnaswamy K, Delproposto J, Kampf JW, Wang S. Aguilar A, et al. Among authors: huang l. J Med Chem. 2019 Jul 11;62(13):6015-6034. doi: 10.1021/acs.jmedchem.9b00021. Epub 2019 Jun 22. J Med Chem. 2019. PMID: 31244110 Free PMC article.
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.
Qin C, Hu Y, Zhou B, Fernandez-Salas E, Yang CY, Liu L, McEachern D, Przybranowski S, Wang M, Stuckey J, Meagher J, Bai L, Chen Z, Lin M, Yang J, Ziazadeh DN, Xu F, Hu J, Xiang W, Huang L, Li S, Wen B, Sun D, Wang S. Qin C, et al. Among authors: huang l. J Med Chem. 2018 Aug 9;61(15):6685-6704. doi: 10.1021/acs.jmedchem.8b00506. Epub 2018 Jul 18. J Med Chem. 2018. PMID: 30019901 Free PMC article.
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong In Vivo Antitumor Activity.
Xu S, Aguilar A, Huang L, Xu T, Zheng K, McEachern D, Przybranowski S, Foster C, Zawacki K, Liu Z, Chinnaswamy K, Stuckey J, Wang S. Xu S, et al. Among authors: huang l. J Med Chem. 2020 May 14;63(9):4997-5010. doi: 10.1021/acs.jmedchem.0c00547. Epub 2020 Apr 27. J Med Chem. 2020. PMID: 32338903 Free PMC article.
Discovery of N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), a highly selective, orally bioavailable inhibitor of aurora kinases with activity against multidrug-resistant cancer cell lines.
Geuns-Meyer S, Cee VJ, Deak HL, Du B, Hodous BL, Nguyen HN, Olivieri PR, Schenkel LB, Vaida KR, Andrews P, Bak A, Be X, Beltran PJ, Bush TL, Chaves MK, Chung G, Dai Y, Eden P, Hanestad K, Huang L, Lin MH, Tang J, Ziegler B, Radinsky R, Kendall R, Patel VF, Payton M. Geuns-Meyer S, et al. Among authors: huang l. J Med Chem. 2015 Jul 9;58(13):5189-207. doi: 10.1021/acs.jmedchem.5b00183. Epub 2015 May 31. J Med Chem. 2015. PMID: 25970324
Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.
Hua Z, Bregman H, Buchanan JL, Chakka N, Guzman-Perez A, Gunaydin H, Huang X, Gu Y, Berry V, Liu J, Teffera Y, Huang L, Egge B, Emkey R, Mullady EL, Schneider S, Andrews PS, Acquaviva L, Dovey J, Mishra A, Newcomb J, Saffran D, Serafino R, Strathdee CA, Turci SM, Stanton M, Wilson C, Dimauro EF. Hua Z, et al. Among authors: huang l, huang x. J Med Chem. 2013 Dec 27;56(24):10003-15. doi: 10.1021/jm401317z. Epub 2013 Dec 11. J Med Chem. 2013. PMID: 24294969
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.
Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio C, Butler JR, Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT Jr, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M, Kornecook T, Kreiman CR, La DS, Ligutti J, Milgram BC, Lin MJ, Marx IE, Nguyen HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA, Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD, Weiss MM. Graceffa RF, et al. Among authors: huang l, huang h. J Med Chem. 2017 Jul 27;60(14):5990-6017. doi: 10.1021/acs.jmedchem.6b01850. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28324649
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