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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: hansen sk. 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
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. 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. 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
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: hansen sk. 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
Allosteric inhibition of protein tyrosine phosphatase 1B.
Wiesmann C, Barr KJ, Kung J, Zhu J, Erlanson DA, Shen W, Fahr BJ, Zhong M, Taylor L, Randal M, McDowell RS, Hansen SK. Wiesmann C, et al. Among authors: hansen sk. Nat Struct Mol Biol. 2004 Aug;11(8):730-7. doi: 10.1038/nsmb803. Epub 2004 Jul 18. Nat Struct Mol Biol. 2004. PMID: 15258570
SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo.
Arbitrario JP, Belmont BJ, Evanchik MJ, Flanagan WM, Fucini RV, Hansen SK, Harris SO, Hashash A, Hoch U, Hogan JN, Howlett AR, Jacobs JW, Lam JW, Ritchie SC, Romanowski MJ, Silverman JA, Stockett DE, Teague JN, Zimmerman KM, Taverna P. Arbitrario JP, et al. Among authors: hansen sk. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17. doi: 10.1007/s00280-009-1076-8. Epub 2009 Aug 1. Cancer Chemother Pharmacol. 2010. PMID: 19649632
Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C.
Shin Y, Jeong JW, Wurz RP, Achanta P, Arvedson T, Bartberger MD, Campuzano IDG, Fucini R, Hansen SK, Ingersoll J, Iwig JS, Lipford JR, Ma V, Kopecky DJ, McCarter J, San Miguel T, Mohr C, Sabet S, Saiki AY, Sawayama A, Sethofer S, Tegley CM, Volak LP, Yang K, Lanman BA, Erlanson DA, Cee VJ. Shin Y, et al. Among authors: hansen sk. ACS Med Chem Lett. 2019 Aug 20;10(9):1302-1308. doi: 10.1021/acsmedchemlett.9b00258. eCollection 2019 Sep 12. ACS Med Chem Lett. 2019. PMID: 31531201 Free PMC article.
120 results