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Page 1
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Fucini RV, Hanan EJ, Romanowski MJ, Elling RA, Lew W, Barr KJ, Zhu J, Yoburn JC, Liu Y, Fahr BT, Fan J, Lu Y, Pham P, Choong IC, VanderPorten EC, Bui M, Purkey HE, Evanchik MJ, Yang W. Fucini RV, et al. Among authors: yang w. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5648-52. doi: 10.1016/j.bmcl.2008.08.095. Epub 2008 Aug 29. Bioorg Med Chem Lett. 2008. PMID: 18793847
Structure of the Brachydanio rerio Polo-like kinase 1 (Plk1) catalytic domain in complex with an extended inhibitor targeting the adaptive pocket of the enzyme.
Elling RA, Fucini RV, Hanan EJ, Barr KJ, Zhu J, Paulvannan K, Yang W, Romanowski MJ. Elling RA, et al. Among authors: yang w. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008 Aug 1;64(Pt 8):686-91. doi: 10.1107/S1744309108019623. Epub 2008 Jul 26. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008. PMID: 18678933 Free PMC article.
Water-soluble prodrugs of an Aurora kinase inhibitor.
Oslob JD, Heumann SA, Yu CH, Allen DA, Baskaran S, Bui M, Delarosa E, Fung AD, Hashash A, Hau J, Ivy S, Jacobs JW, Lew W, Maung J, McDowell RS, Ritchie S, Romanowski MJ, Silverman JA, Yang W, Zhong M, Fuchs-Knotts T. Oslob JD, et al. Among authors: yang w. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1409-12. doi: 10.1016/j.bmcl.2009.01.043. Epub 2009 Jan 19. Bioorg Med Chem Lett. 2009. PMID: 19186057
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: yang w. 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
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: yang w. 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
Fragment-based discovery of nonpeptidic BACE-1 inhibitors using tethering.
Yang W, Fucini RV, Fahr BT, Randal M, Lind KE, Lam MB, Lu W, Lu Y, Cary DR, Romanowski MJ, Colussi D, Pietrak B, Allison TJ, Munshi SK, Penny DM, Pham P, Sun J, Thomas AE, Wilkinson JM, Jacobs JW, McDowell RS, Ballinger MD. Yang W, et al. Biochemistry. 2009 Jun 2;48(21):4488-96. doi: 10.1021/bi900017q. Biochemistry. 2009. PMID: 19284778
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: yang w. 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. Among authors: yang w. 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
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