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33 results

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Page 1
Down-regulation of the Notch pathway mediated by a gamma-secretase inhibitor induces anti-tumour effects in mouse models of T-cell leukaemia.
Tammam J, Ware C, Efferson C, O'Neil J, Rao S, Qu X, Gorenstein J, Angagaw M, Kim H, Kenific C, Kunii K, Leach KJ, Nikov G, Zhao J, Dai X, Hardwick J, Scott M, Winter C, Bristow L, Elbi C, Reilly JF, Look T, Draetta G, Van der Ploeg L, Kohl NE, Strack PR, Majumder PK. Tammam J, et al. Among authors: kenific c. Br J Pharmacol. 2009 Nov;158(5):1183-95. doi: 10.1111/j.1476-5381.2009.00389.x. Epub 2009 Sep 23. Br J Pharmacol. 2009. PMID: 19775282 Free PMC article.
Purine derivatives as potent gamma-secretase modulators.
Rivkin A, Ahearn SP, Chichetti SM, Hamblett CL, Garcia Y, Martinez M, Hubbs JL, Reutershan MH, Daniels MH, Siliphaivanh P, Otte KM, Li C, Rosenau A, Surdi LM, Jung J, Hughes BL, Crispino JL, Nikov GN, Middleton RE, Moxham CM, Szewczak AA, Shah S, Moy LY, Kenific CM, Tanga F, Cruz JC, Andrade P, Angagaw MH, Shomer NH, Miller T, Munoz B, Shearman MS. Rivkin A, et al. Among authors: kenific cm. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2279-82. doi: 10.1016/j.bmcl.2010.02.008. Epub 2010 Feb 6. Bioorg Med Chem Lett. 2010. PMID: 20207146
Inhibition of gamma-secretase activity inhibits tumor progression in a mouse model of pancreatic ductal adenocarcinoma.
Plentz R, Park JS, Rhim AD, Abravanel D, Hezel AF, Sharma SV, Gurumurthy S, Deshpande V, Kenific C, Settleman J, Majumder PK, Stanger BZ, Bardeesy N. Plentz R, et al. Among authors: kenific c. Gastroenterology. 2009 May;136(5):1741-9.e6. doi: 10.1053/j.gastro.2009.01.008. Epub 2009 Jan 14. Gastroenterology. 2009. PMID: 19208345 Free PMC article.
Fluorinated piperidine acetic acids as gamma-secretase modulators.
Stanton MG, Hubbs J, Sloman D, Hamblett C, Andrade P, Angagaw M, Bi G, Black RM, Crispino J, Cruz JC, Fan E, Farris G, Hughes BL, Kenific CM, Middleton RE, Nikov G, Sajonz P, Shah S, Shomer N, Szewczak AA, Tanga F, Tudge MT, Shearman M, Munoz B. Stanton MG, et al. Among authors: kenific cm. Bioorg Med Chem Lett. 2010 Jan 15;20(2):755-8. doi: 10.1016/j.bmcl.2009.11.034. Epub 2009 Nov 13. Bioorg Med Chem Lett. 2010. PMID: 20005099
Triazoles as γ-secretase modulators.
Fischer C, Zultanski SL, Zhou H, Methot JL, Brown WC, Mampreian DM, Schell AJ, Shah S, Nuthall H, Hughes BL, Smotrov N, Kenific CM, Cruz JC, Walker D, Bouthillette M, Nikov GN, Savage DF, Jeliazkova-Mecheva VV, Diaz D, Szewczak AA, Bays N, Middleton RE, Munoz B, Shearman MS. Fischer C, et al. Among authors: kenific cm. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4083-7. doi: 10.1016/j.bmcl.2011.04.089. Epub 2011 May 4. Bioorg Med Chem Lett. 2011. PMID: 21616665
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.
Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Hayashi I, Hughes BL, Moxham CM, Bays NW, Smotrov N, Hill AD, Pan BS, Wu Z, Moy LY, Tanga F, Kenific C, Cruz JC, Walker D, Bouthillette M, Nikov GN, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Michener MS, Cook JJ, Munoz B, Shearman MS. Fischer C, et al. Among authors: kenific c. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3488-94. doi: 10.1016/j.bmcl.2015.07.003. Epub 2015 Jul 9. Bioorg Med Chem Lett. 2015. PMID: 26212776
Potent benzoazepinone γ-secretase modulators with improved bioavailability.
Methot JL, Fischer C, Li C, Rivkin A, Ahearn SP, Brown WC, Kattar S, Kelley E, Mampreian DM, Schell A, Rosenau A, Zhou H, Ball R, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Moy LY, Kenific CM, Moxham C, Shah S, Nuthall H, Szewczak AA, Hill A, Hughes B, Smotrov N, Munoz B, Miller TA, Shearman MS. Methot JL, et al. Among authors: kenific cm. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3495-500. doi: 10.1016/j.bmcl.2015.06.032. Epub 2015 Jun 15. Bioorg Med Chem Lett. 2015. PMID: 26142947
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.
Methot JL, Hoffman DM, Witter DJ, Stanton MG, Harrington P, Hamblett C, Siliphaivanh P, Wilson K, Hubbs J, Heidebrecht R, Kral AM, Ozerova N, Fleming JC, Wang H, Szewczak AA, Middleton RE, Hughes B, Cruz JC, Haines BB, Chenard M, Kenific CM, Harsch A, Secrist JP, Miller TA. Methot JL, et al. Among authors: kenific cm. ACS Med Chem Lett. 2014 Jan 2;5(4):340-5. doi: 10.1021/ml4004233. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900838 Free PMC article.
SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Methot JL, Hamblett CL, Mampreian DM, Jung J, Harsch A, Szewczak AA, Dahlberg WK, Middleton RE, Hughes B, Fleming JC, Wang H, Kral AM, Ozerova N, Cruz JC, Haines B, Chenard M, Kenific CM, Secrist JP, Miller TA. Methot JL, et al. Among authors: kenific cm. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. doi: 10.1016/j.bmcl.2008.10.052. Epub 2008 Oct 14. Bioorg Med Chem Lett. 2008. PMID: 18951790
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.
Kattar SD, Surdi LM, Zabierek A, Methot JL, Middleton RE, Hughes B, Szewczak AA, Dahlberg WK, Kral AM, Ozerova N, Fleming JC, Wang H, Secrist P, Harsch A, Hamill JE, Cruz JC, Kenific CM, Chenard M, Miller TA, Berk SC, Tempest P. Kattar SD, et al. Among authors: kenific cm. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1168-72. doi: 10.1016/j.bmcl.2008.12.083. Epub 2008 Dec 25. Bioorg Med Chem Lett. 2009. PMID: 19138845
33 results