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Page 1
Preclinical evaluation of [11 C]L-235 as a radioligand for Positron Emission Tomography cathepsin K imaging in bone.
Bennacef I, Rubins D, Riffel K, Williams M, Posavec DJ, Holahan MA, Purcell ML, Haley HD, Wolf M, Stachel SJ, Lubbers LS, Wesolowski GA, Duong LT, Hamill TG, Evelhoch JL, Hostetler ED. Bennacef I, et al. Among authors: stachel sj. J Labelled Comp Radiopharm. 2021 Apr;64(4):159-167. doi: 10.1002/jlcr.3896. Epub 2020 Dec 2. J Labelled Comp Radiopharm. 2021. PMID: 33226657
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.
Lead optimization of cathepsin K inhibitors for the treatment of Osteoarthritis.
Ginnetti AT, Paone DV, Nanda KK, Li J, Busuek M, Johnson SA, Lu J, Soisson SM, Robinson R, Fisher J, Webber A, Wesolowski G, Ma B, Duong L, Carroll S, Burgey CS, Stachel SJ. Ginnetti AT, et al. Among authors: stachel sj. Bioorg Med Chem Lett. 2022 Oct 15;74:128927. doi: 10.1016/j.bmcl.2022.128927. Epub 2022 Aug 6. Bioorg Med Chem Lett. 2022. PMID: 35944849
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.
Egbertson M, McGaughey GB, Pitzenberger SM, Stauffer SR, Coburn CA, Stachel SJ, Yang W, Barrow JC, Neilson LA, McWherter M, Perlow D, Fahr B, Munshi S, Allison TJ, Holloway K, Selnick HG, Yang Z, Swestock J, Simon AJ, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Pietrak B, Haugabook S, Jin L, Chen IW, Holahan M, Stranieri-Michener M, Cook JJ, Vacca J, Graham SL. Egbertson M, et al. Among authors: stachel sj. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4812-4819. doi: 10.1016/j.bmcl.2015.06.082. Epub 2015 Jun 29. Bioorg Med Chem Lett. 2015. PMID: 26195137
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
Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation.
Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K. Hong C, et al. Among authors: stachel sj. Nat Commun. 2021 Feb 5;12(1):815. doi: 10.1038/s41467-021-21087-6. Nat Commun. 2021. PMID: 33547286 Free PMC article.
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.
Coburn CA, Stachel SJ, Li YM, Rush DM, Steele TG, Chen-Dodson E, Holloway MK, Xu M, Huang Q, Lai MT, DiMuzio J, Crouthamel MC, Shi XP, Sardana V, Chen Z, Munshi S, Kuo L, Makara GM, Annis DA, Tadikonda PK, Nash HM, Vacca JP, Wang T. Coburn CA, et al. Among authors: stachel sj. J Med Chem. 2004 Dec 2;47(25):6117-9. doi: 10.1021/jm049388p. J Med Chem. 2004. PMID: 15566281
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
42 results