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The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.
Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH. Burton CR, et al. Among authors: grafstrom rh. J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23. J Biol Chem. 2008. PMID: 18574238 Free article.
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.
Markwalder JA, Arnone MR, Benfield PA, Boisclair M, Burton CR, Chang CH, Cox SS, Czerniak PM, Dean CL, Doleniak D, Grafstrom R, Harrison BA, Kaltenbach RF 3rd, Nugiel DA, Rossi KA, Sherk SR, Sisk LM, Stouten P, Trainor GL, Worland P, Seitz SP. Markwalder JA, et al. J Med Chem. 2004 Nov 18;47(24):5894-911. doi: 10.1021/jm020455u. J Med Chem. 2004. PMID: 15537345
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).
Yue EW, Higley CA, DiMeo SV, Carini DJ, Nugiel DA, Benware C, Benfield PA, Burton CR, Cox S, Grafstrom RH, Sharp DM, Sisk LM, Boylan JF, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Seitz SP, Trainor GL. Yue EW, et al. Among authors: grafstrom rh. J Med Chem. 2002 Nov 21;45(24):5233-48. doi: 10.1021/jm0201722. J Med Chem. 2002. PMID: 12431051
Quinazolines as cyclin dependent kinase inhibitors.
Sielecki TM, Johnson TL, Liu J, Muckelbauer JK, Grafstrom RH, Cox S, Boylan J, Burton CR, Chen H, Smallwood A, Chang CH, Boisclair M, Benfield PA, Trainor GL, Seitz SP. Sielecki TM, et al. Among authors: grafstrom rh. Bioorg Med Chem Lett. 2001 May 7;11(9):1157-60. doi: 10.1016/s0960-894x(01)00185-8. Bioorg Med Chem Lett. 2001. PMID: 11354366
Identification of selective inhibitors of cyclin dependent kinase 4.
Carini DJ, Kaltenbach RF, Liu J, Benfield PA, Boylan J, Boisclair M, Brizuela L, Burton CR, Cox S, Grafstrom R, Harrison BA, Harrison K, Akamike E, Markwalder JA, Nakano Y, Seitz SP, Sharp DM, Trainor GL, Sielecki TM. Carini DJ, et al. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2209-11. doi: 10.1016/s0960-894x(01)00416-4. Bioorg Med Chem Lett. 2001. PMID: 11514172
32 results