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Center for the Development of Therapeutics

Hydroxamate-based histone deacetylase inhibitors can protect neurons from oxidative stress via a histone deacetylase-independent catalase-like mechanism.

Olson DE, Sleiman SF, Bourassa MW, et al. Hydroxamate-based histone deacetylase inhibitors can protect neurons from oxidative stress via a histone deacetylase-independent catalase-like mechanism. Chem Biol. 2015;22(4):439-445. doi:10.1016/j.chembiol.2015.03.014

Niche-Based Screening in Multiple Myeloma Identifies a Kinesin-5 Inhibitor with Improved Selectivity over Hematopoietic Progenitors.

Chattopadhyay S, Stewart AL, Mukherjee S, et al. Niche-Based Screening in Multiple Myeloma Identifies a Kinesin-5 Inhibitor with Improved Selectivity over Hematopoietic Progenitors. Cell Rep. 2015;10(5):755-770. doi:10.1016/j.celrep.2015.01.017

Target-based identification of whole-cell active inhibitors of biotin biosynthesis in Mycobacterium tuberculosis.

Park SW, Casalena DE, Wilson DJ, et al. Target-based identification of whole-cell active inhibitors of biotin biosynthesis in Mycobacterium tuberculosis. Chem Biol. 2015;22(1):76-86. doi:10.1016/j.chembiol.2014.11.012

Kinetically Selective Inhibitors of Histone Deacetylase 2 (HDAC2) as Cognition Enhancers.

Wagner FF, Zhang YL, Fass DM, et al. Kinetically Selective Inhibitors of Histone Deacetylase 2 (HDAC2) as Cognition Enhancers. Chem Sci. 2015;6(1):804-815. doi:10.1039/C4SC02130D

Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression.

Nagiec MM, Skepner AP, Negri J, et al. Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression. PLoS One. 2015;10(3):e0120295. doi:10.1371/journal.pone.0120295

BioAssay Research Database (BARD): chemical biology and probe-development enabled by structured metadata and result types.

Howe EA, De Souza A, Lahr DL, et al. BioAssay Research Database (BARD): chemical biology and probe-development enabled by structured metadata and result types. Nucleic Acids Res. 2015;43(Database issue):D1163-70. doi:10.1093/nar/gku1244

Benzo-fused lactams from a diversity-oriented synthesis (DOS) library as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake.

Dockendorff C, Faloon PW, Pu J, et al. Benzo-fused lactams from a diversity-oriented synthesis (DOS) library as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake. Bioorg Med Chem Lett. 2015;25(10):2100-5. doi:10.1016/j.bmcl.2015.03.073

Identification of ATR-Chk1 pathway inhibitors that selectively target p53-deficient cells without directly suppressing ATR catalytic activity.

Kawasumi M, Bradner JE, Tolliday N, et al. Identification of ATR-Chk1 pathway inhibitors that selectively target p53-deficient cells without directly suppressing ATR catalytic activity. Cancer Res. 2014;74(24):7534-45. doi:10.1158/0008-5472.CAN-14-2650

Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1).

Fang C, D’Souza B, Thompson CF, et al. Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1). ACS Med Chem Lett. 2014;5(12):1308-12. doi:10.1021/ml500388q

Hydroxamic acid-based histone deacetylase (HDAC) inhibitors can mediate neuroprotection independent of HDAC inhibition.

Sleiman SF, Olson DE, Bourassa MW, et al. Hydroxamic acid-based histone deacetylase (HDAC) inhibitors can mediate neuroprotection independent of HDAC inhibition. J Neurosci. 2014;34(43):14328-37. doi:10.1523/JNEUROSCI.1010-14.2014