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Page 1
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Stachel SJ, Coburn CA, Steele TG, Jones KG, Loutzenhiser EF, Gregro AR, Rajapakse HA, Lai MT, Crouthamel MC, Xu M, Tugusheva K, Lineberger JE, Pietrak BL, Espeseth AS, Shi XP, Chen-Dodson E, Holloway MK, Munshi S, Simon AJ, Kuo L, Vacca JP. Stachel SJ, et al. J Med Chem. 2004 Dec 16;47(26):6447-50. doi: 10.1021/jm049379g. J Med Chem. 2004. PMID: 15588077
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
Stachel SJ, Coburn CA, Sankaranarayanan S, Price EA, Wu G, Crouthamel M, Pietrak BL, Huang Q, Lineberger J, Espeseth AS, Jin L, Ellis J, Holloway MK, Munshi S, Allison T, Hazuda D, Simon AJ, Graham SL, Vacca JP. Stachel SJ, et al. J Med Chem. 2006 Oct 19;49(21):6147-50. doi: 10.1021/jm060884i. J Med Chem. 2006. PMID: 17034118
A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.
Hills ID, Holloway MK, de León P, Nomland A, Zhu H, Rajapakse H, Allison TJ, Munshi SK, Colussi D, Pietrak BL, Toolan D, Haugabook SJ, Graham SL, Stachel SJ. Hills ID, et al. Among authors: stachel sj. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4993-5. doi: 10.1016/j.bmcl.2009.07.071. Epub 2009 Jul 17. Bioorg Med Chem Lett. 2009. PMID: 19640712
Discovery of pyrrolidine-based β-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.
Stachel SJ, Steele TG, Petrocchi A, Haugabook SJ, McGaughey G, Katharine Holloway M, Allison T, Munshi S, Zuck P, Colussi D, Tugasheva K, Wolfe A, Graham SL, Vacca JP. Stachel SJ, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):240-4. doi: 10.1016/j.bmcl.2011.11.024. Epub 2011 Nov 12. Bioorg Med Chem Lett. 2012. PMID: 22130130
Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain.
Stachel SJ, Sanders JM, Henze DA, Rudd MT, Su HP, Li Y, Nanda KK, Egbertson MS, Manley PJ, Jones KL, Brnardic EJ, Green A, Grobler JA, Hanney B, Leitl M, Lai MT, Munshi V, Murphy D, Rickert K, Riley D, Krasowska-Zoladek A, Daley C, Zuck P, Kane SA, Bilodeau MT. Stachel SJ, et al. J Med Chem. 2014 Jul 10;57(13):5800-16. doi: 10.1021/jm5006429. Epub 2014 Jun 19. J Med Chem. 2014. PMID: 24914455
Chondroitin sulfate promotes activation of cathepsin K.
Lemaire PA, Huang L, Zhuo Y, Lu J, Bahnck C, Stachel SJ, Carroll SS, Duong LT. Lemaire PA, et al. Among authors: stachel sj. J Biol Chem. 2014 Aug 1;289(31):21562-72. doi: 10.1074/jbc.M114.559898. Epub 2014 Jun 23. J Biol Chem. 2014. PMID: 24958728 Free PMC article.
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
Stachel SJ, Zerbinatti C, Rudd MT, Cosden M, Suon S, Nanda KK, Wessner K, DiMuzio J, Maxwell J, Wu Z, Uslaner JM, Michener MS, Szczerba P, Brnardic E, Rada V, Kim Y, Meissner R, Wuelfing P, Yuan Y, Ballard J, Holahan M, Klein DJ, Lu J, Fradera X, Parthasarathy G, Uebele VN, Chen Z, Li Y, Li J, Cooke AJ, Bennett DJ, Bilodeau MT, Renger J. Stachel SJ, et al. J Med Chem. 2016 Apr 14;59(7):3489-98. doi: 10.1021/acs.jmedchem.6b00176. Epub 2016 Apr 1. J Med Chem. 2016. PMID: 27011007
The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design.
Forster AB, Abeywickrema P, Bunda J, Cox CD, Cabalu TD, Egbertson M, Fay J, Getty K, Hall D, Kornienko M, Lu J, Parthasarathy G, Reid J, Sharma S, Shipe WD, Smith SM, Soisson S, Stachel SJ, Su HP, Wang D, Berger R. Forster AB, et al. Among authors: stachel sj. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5167-5171. doi: 10.1016/j.bmcl.2017.10.054. Epub 2017 Oct 23. Bioorg Med Chem Lett. 2017. PMID: 29113762
45 results