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Page 1
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Winneroski LL, Erickson JA, Green SJ, Lopez JE, Stout SL, Porter WJ, Timm DE, Audia JE, Barberis M, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hembre EJ, Hendle J, Garcia-Losada P, Minguez JM, Mathes BM, May PC, Monk SA, Rankovic Z, Shi Y, Watson BM, Yang Z, Mergott DJ. Winneroski LL, et al. Among authors: stout sl. Bioorg Med Chem. 2020 Jan 1;28(1):115194. doi: 10.1016/j.bmc.2019.115194. Epub 2019 Nov 15. Bioorg Med Chem. 2020. PMID: 31786008
Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.
May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM, Stout SL, Timm DE, Smith Labell E, Gonzales CR, Nakano M, Jhee SS, Yen M, Ereshefsky L, Lindstrom TD, Calligaro DO, Cocke PJ, Greg Hall D, Friedrich S, Citron M, Audia JE. May PC, et al. Among authors: stout sl. J Neurosci. 2011 Nov 16;31(46):16507-16. doi: 10.1523/JNEUROSCI.3647-11.2011. J Neurosci. 2011. PMID: 22090477 Free PMC article. Clinical Trial.
The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans.
May PC, Willis BA, Lowe SL, Dean RA, Monk SA, Cocke PJ, Audia JE, Boggs LN, Borders AR, Brier RA, Calligaro DO, Day TA, Ereshefsky L, Erickson JA, Gevorkyan H, Gonzales CR, James DE, Jhee SS, Komjathy SF, Li L, Lindstrom TD, Mathes BM, Martényi F, Sheehan SM, Stout SL, Timm DE, Vaught GM, Watson BM, Winneroski LL, Yang Z, Mergott DJ. May PC, et al. Among authors: stout sl. J Neurosci. 2015 Jan 21;35(3):1199-210. doi: 10.1523/JNEUROSCI.4129-14.2015. J Neurosci. 2015. PMID: 25609634 Free PMC article. Clinical Trial.
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Winneroski LL, Schiffler MA, Erickson JA, May PC, Monk SA, Timm DE, Audia JE, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hudziak KJ, Klimkowski VJ, Garcia Losada P, Mathes BM, Stout SL, Watson BM, Mergott DJ. Winneroski LL, et al. Among authors: stout sl. Bioorg Med Chem. 2015 Jul 1;23(13):3260-8. doi: 10.1016/j.bmc.2015.04.062. Epub 2015 May 6. Bioorg Med Chem. 2015. PMID: 26001341
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
McKinzie DL, Winneroski LL, Green SJ, Hembre EJ, Erickson JA, Willis BA, Monk SA, Aluise CD, Baker TK, Lopez JE, Hendle J, Beck JP, Brier RA, Boggs LN, Borders AR, Cocke PJ, Garcia-Losada P, Lowe SL, Mathes BM, May PC, Porter WJ, Stout SL, Timm DE, Watson BM, Yang Z, Mergott DJ. McKinzie DL, et al. Among authors: stout sl. J Med Chem. 2021 Jun 24;64(12):8076-8100. doi: 10.1021/acs.jmedchem.1c00489. Epub 2021 Jun 3. J Med Chem. 2021. PMID: 34081466
Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt).
Lugar CW, Clarke CA, Morphy R, Rudyk H, Sapmaz S, Stites RE, Vaught GM, Furness K, Broughton HB, Durst GL, Clawson DK, Stout SL, Guo SY, Durbin JD, Stayrook KR, Edmondson DD, Kikly K, New NE, Bina HA, Chambers MG, Shetler P, Chang WY, Chang VC, Barr R, Gough WH, Steele JP, Getman B, Patel N, Mathes BM, Richardson TI. Lugar CW, et al. Among authors: stout sl. J Med Chem. 2021 May 13;64(9):5470-5484. doi: 10.1021/acs.jmedchem.0c01918. Epub 2021 Apr 14. J Med Chem. 2021. PMID: 33852312
Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.
Parthasarathy S, Henry K, Pei H, Clayton J, Rempala M, Johns D, De Frutos O, Garcia P, Mateos C, Pleite S, Wang Y, Stout S, Condon B, Ashok S, Lu Z, Ehlhardt W, Raub T, Lai M, Geeganage S, Burkholder TP. Parthasarathy S, et al. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1887-1891. doi: 10.1016/j.bmcl.2018.03.092. Epub 2018 Apr 2. Bioorg Med Chem Lett. 2018. PMID: 29655979
Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design.
Hughes NE, Bleisch TJ, Jones SA, Richardson TI, Doti RA, Wang Y, Stout SL, Durst GL, Chambers MG, Oskins JL, Lin C, Adams LA, Page TJ, Barr RJ, Zink RW, Osborne H, Montrose-Rafizadeh C, Norman BH. Hughes NE, et al. Among authors: stout sl. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-3277. doi: 10.1016/j.bmcl.2016.05.056. Epub 2016 May 20. Bioorg Med Chem Lett. 2016. PMID: 27261179
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.
Durham TB, Klimkowski VJ, Rito CJ, Marimuthu J, Toth JL, Liu C, Durbin JD, Stout SL, Adams L, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR. Durham TB, et al. Among authors: stout sl. J Med Chem. 2014 Dec 26;57(24):10476-85. doi: 10.1021/jm501522n. Epub 2014 Dec 5. J Med Chem. 2014. PMID: 25415648
16 results