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Page 1
Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.
Jenkins TJ, Guan B, Dai M, Li G, Lightburn TE, Huang S, Freeze BS, Burdi DF, Jacutin-Porte S, Bennett R, Chen W, Minor C, Ghosh S, Blackburn C, Gigstad KM, Jones M, Kolbeck R, Yin W, Smith S, Cardillo D, Ocain TD, Harriman GC. Jenkins TJ, et al. J Med Chem. 2007 Feb 8;50(3):566-84. doi: 10.1021/jm061118e. J Med Chem. 2007. PMID: 17266208
Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4.
Blackburn C, Guan B, Brown J, Cullis C, Condon SM, Jenkins TJ, Peluso S, Ye Y, Gimeno RE, Punreddy S, Sun Y, Wu H, Hubbard B, Kaushik V, Tummino P, Sanchetti P, Yu Sun D, Daniels T, Tozzo E, Balani SK, Raman P. Blackburn C, et al. Among authors: jenkins tj. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3504-9. doi: 10.1016/j.bmcl.2006.03.102. Epub 2006 Apr 27. Bioorg Med Chem Lett. 2006. PMID: 16644217
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: jenkins tj. 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
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: jenkins tj. 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
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: jenkins tj. 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
Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases.
Marcotte DJ, Liu YT, Arduini RM, Hession CA, Miatkowski K, Wildes CP, Cullen PF, Hong V, Hopkins BT, Mertsching E, Jenkins TJ, Romanowski MJ, Baker DP, Silvian LF. Marcotte DJ, et al. Among authors: jenkins tj. Protein Sci. 2010 Mar;19(3):429-39. doi: 10.1002/pro.321. Protein Sci. 2010. PMID: 20052711 Free PMC article.
36 results