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Page 1
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: romanowski mj. Protein Sci. 2010 Mar;19(3):429-39. doi: 10.1002/pro.321. Protein Sci. 2010. PMID: 20052711 Free PMC article.
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: romanowski mj. 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
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: romanowski mj. 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 a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.
Erlanson DA, Arndt JW, Cancilla MT, Cao K, Elling RA, English N, Friedman J, Hansen SK, Hession C, Joseph I, Kumaravel G, Lee WC, Lind KE, McDowell RS, Miatkowski K, Nguyen C, Nguyen TB, Park S, Pathan N, Penny DM, Romanowski MJ, Scott D, Silvian L, Simmons RL, Tangonan BT, Yang W, Sun L. Erlanson DA, et al. Among authors: romanowski mj. Bioorg Med Chem Lett. 2011 May 15;21(10):3078-83. doi: 10.1016/j.bmcl.2011.03.032. Epub 2011 Mar 17. Bioorg Med Chem Lett. 2011. PMID: 21459573
A small-molecule inhibitor of C5 complement protein.
Jendza K, Kato M, Salcius M, Srinivas H, De Erkenez A, Nguyen A, McLaughlin D, Be C, Wiesmann C, Murphy J, Bolduc P, Mogi M, Duca J, Namil A, Capparelli M, Darsigny V, Meredith E, Tichkule R, Ferrara L, Heyder J, Liu F, Horton PA, Romanowski MJ, Schirle M, Mainolfi N, Anderson K, Michaud GA. Jendza K, et al. Among authors: romanowski mj. Nat Chem Biol. 2019 Jul;15(7):666-668. doi: 10.1038/s41589-019-0303-9. Epub 2019 Jun 17. Nat Chem Biol. 2019. PMID: 31209353
Mouse Aurora A: expression in Escherichia coli and purification.
Elling RA, Tangonan BT, Penny DM, Smith JT, Vincent DE, Hansen SK, O'Brien T, Romanowski MJ. Elling RA, et al. Among authors: romanowski mj. Protein Expr Purif. 2007 Jul;54(1):139-46. doi: 10.1016/j.pep.2007.03.002. Epub 2007 Mar 12. Protein Expr Purif. 2007. PMID: 17434748
Discovery of a potent and selective aurora kinase inhibitor.
Oslob JD, Romanowski MJ, Allen DA, Baskaran S, Bui M, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris S, Heumann SA, Hoch U, Jacobs JW, Lam J, Lawrence CE, McDowell RS, Nannini MA, Shen W, Silverman JA, Sopko MM, Tangonan BT, Teague J, Yoburn JC, Yu CH, Zhong M, Zimmerman KM, O'Brien T, Lew W. Oslob JD, et al. Among authors: romanowski mj. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4880-4. doi: 10.1016/j.bmcl.2008.07.073. Epub 2008 Jul 24. Bioorg Med Chem Lett. 2008. PMID: 18678489
2-Aminobenzimidazoles as potent Aurora kinase inhibitors.
Zhong M, Bui M, Shen W, Baskaran S, Allen DA, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris SO, Heumann SA, Hoch U, Ivy SN, Jacobs JW, Lam S, Lee H, McDowell RS, Oslob JD, Purkey HE, Romanowski MJ, Silverman JA, Tangonan BT, Taverna P, Yang W, Yoburn JC, Yu CH, Zimmerman KM, O'Brien T, Lew W. Zhong M, et al. Among authors: romanowski mj. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5158-61. doi: 10.1016/j.bmcl.2009.07.016. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19646866
40 results