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Page 1
Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors.
Konicek BW, Capen AR, Credille KM, Ebert PJ, Falcon BL, Heady GL, Patel BKR, Peek VL, Stephens JR, Stewart JA, Stout SL, Timm DE, Um SL, Willard MD, Wulur IH, Zeng Y, Wang Y, Walgren RA, Betty Yan SC. Konicek BW, et al. Among authors: timm de. Oncotarget. 2018 Feb 13;9(17):13796-13806. doi: 10.18632/oncotarget.24488. eCollection 2018 Mar 2. Oncotarget. 2018. PMID: 29568395 Free PMC article.
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: timm de. 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 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: timm de. 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
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: timm de. 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
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: timm de. 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.
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: timm de. 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
The discovery of a new structural class of cyclin-dependent kinase inhibitors, aminoimidazo[1,2-a]pyridines.
Hamdouchi C, Keyser H, Collins E, Jaramillo C, De Diego JE, Spencer CD, Dempsey JA, Anderson BD, Leggett T, Stamm NB, Schultz RM, Watkins SA, Cocke K, Lemke S, Burke TF, Beckmann RP, Dixon JT, Gurganus TM, Rankl NB, Houck KA, Zhang F, Vieth M, Espinosa J, Timm DE, Campbell RM, Patel BK, Brooks HB. Hamdouchi C, et al. Among authors: de diego je, timm de. Mol Cancer Ther. 2004 Jan;3(1):1-9. Mol Cancer Ther. 2004. PMID: 14749470
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.
Jaramillo C, de Diego JE, Hamdouchi C, Collins E, Keyser H, Sánchez-Martínez C, del Prado M, Norman B, Brooks HB, Watkins SA, Spencer CD, Dempsey JA, Anderson BD, Campbell RM, Leggett T, Patel B, Schultz RM, Espinosa J, Vieth M, Zhang F, Timm DE. Jaramillo C, et al. Among authors: de diego je, timm de. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6095-9. doi: 10.1016/j.bmcl.2004.09.053. Bioorg Med Chem Lett. 2004. PMID: 15546737
45 results