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Page 1
Preclinical and clinical evaluation of the LRRK2 inhibitor DNL201 for Parkinson's disease.
Jennings D, Huntwork-Rodriguez S, Henry AG, Sasaki JC, Meisner R, Diaz D, Solanoy H, Wang X, Negrou E, Bondar VV, Ghosh R, Maloney MT, Propson NE, Zhu Y, Maciuca RD, Harris L, Kay A, LeWitt P, King TA, Kern D, Ellenbogen A, Goodman I, Siderowf A, Aldred J, Omidvar O, Masoud ST, Davis SS, Arguello A, Estrada AA, de Vicente J, Sweeney ZK, Astarita G, Borin MT, Wong BK, Wong H, Nguyen H, Scearce-Levie K, Ho C, Troyer MD. Jennings D, et al. Among authors: negrou e. Sci Transl Med. 2022 Jun 8;14(648):eabj2658. doi: 10.1126/scitranslmed.abj2658. Epub 2022 Jun 8. Sci Transl Med. 2022. PMID: 35675433
Understanding LRRK2 kinase activity in preclinical models and human subjects through quantitative analysis of LRRK2 and pT73 Rab10.
Wang X, Negrou E, Maloney MT, Bondar VV, Andrews SV, Montalban M, Llapashtica C, Maciuca R, Nguyen H, Solanoy H, Arguello A, Przybyla L, Moerke NJ, Huntwork-Rodriguez S, Henry AG. Wang X, et al. Among authors: negrou e. Sci Rep. 2021 Jun 18;11(1):12900. doi: 10.1038/s41598-021-91943-4. Sci Rep. 2021. PMID: 34145320 Free PMC article.
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model.
Vandeveer GH, Arduini RM, Baker DP, Barry K, Bohnert T, Bowden-Verhoek JK, Conlon P, Cullen PF, Guan B, Jenkins TJ, Liao SY, Lin L, Liu YT, Marcotte D, Mertsching E, Metrick CM, Negrou E, Powell N, Scott D, Silvian LF, Hopkins BT. Vandeveer GH, et al. Among authors: negrou e. Bioorg Med Chem Lett. 2023 Jan 15;80:129108. doi: 10.1016/j.bmcl.2022.129108. Epub 2022 Dec 17. Bioorg Med Chem Lett. 2023. PMID: 36538993
Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Hopkins BT, Bame E, Bell N, Bohnert T, Bowden-Verhoek JK, Bui M, Cancilla MT, Conlon P, Cullen P, Erlanson DA, Fan J, Fuchs-Knotts T, Hansen S, Heumann S, Jenkins TJ, Gua C, Liu Y, Liu Y, Lulla M, Marcotte D, Marx I, McDowell B, Mertsching E, Negrou E, Romanowski MJ, Scott D, Silvian L, Yang W, Zhong M. Hopkins BT, et al. Among authors: negrou e. Bioorg Med Chem. 2021 Aug 15;44:116275. doi: 10.1016/j.bmc.2021.116275. Epub 2021 Jun 15. Bioorg Med Chem. 2021. PMID: 34314938
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.
Hopkins BT, Bame E, Bell N, Bohnert T, Bowden-Verhoek JK, Bui M, Cancilla MT, Conlon P, Cullen P, Erlanson DA, Fan J, Fuchs-Knotts T, Hansen S, Heumann S, Jenkins TJ, Marcotte D, McDowell B, Mertsching E, Negrou E, Otipoby KL, Poreci U, Romanowski MJ, Scott D, Silvian L, Yang W, Zhong M. Hopkins BT, et al. Among authors: negrou e. Bioorg Med Chem. 2019 Jul 1;27(13):2905-2913. doi: 10.1016/j.bmc.2019.05.021. Epub 2019 May 14. Bioorg Med Chem. 2019. PMID: 31138459
A mouse Fcgamma-Fcepsilon protein that inhibits mast cells through activation of FcgammaRIIB, SH2 domain-containing inositol phosphatase 1, and SH2 domain-containing protein tyrosine phosphatases.
Mertsching E, Bafetti L, Hess H, Perper S, Giza K, Allen LC, Negrou E, Hathaway K, Hopp J, Chung J, Perret D, Shields M, Saxon A, Kehry MR. Mertsching E, et al. Among authors: negrou e. J Allergy Clin Immunol. 2008 Feb;121(2):441-447.e5. doi: 10.1016/j.jaci.2007.08.051. Epub 2007 Oct 18. J Allergy Clin Immunol. 2008. PMID: 17949802
11 results