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Stanley Center Therapeutics

FDG-PET imaging reveals local brain glucose utilization is altered by class I histone deacetylase inhibitors.

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Schroeder FA, Chonde DB, Riley MM, et al. FDG-PET imaging reveals local brain glucose utilization is altered by class I histone deacetylase inhibitors. Neurosci Lett. 2013;550:119-24. doi:10.1016/j.neulet.2013.06.016.

Validating therapeutic targets through human genetics.

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Plenge RM, Scolnick EM, Altshuler D. Validating therapeutic targets through human genetics. Nat Rev Drug Discov. 2013;12(8):581-94. doi:10.1038/nrd4051.

Working memory impairment in calcineurin knock-out mice is associated with alterations in synaptic vesicle cycling and disruption of high-frequency synaptic and network activity in prefrontal cortex.

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Cottrell JR, Levenson JM, Kim SH, et al. Working memory impairment in calcineurin knock-out mice is associated with alterations in synaptic vesicle cycling and disruption of high-frequency synaptic and network activity in prefrontal cortex. J Neurosci. 2013;33(27):10938-49. doi:10.1523/JNEUROSCI.5362-12.2013.

Discovery of the first histone deacetylase 6/8 dual inhibitors.

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Olson DE, Wagner FF, Kaya T, et al. Discovery of the first histone deacetylase 6/8 dual inhibitors. J Med Chem. 2013;56(11):4816-20. doi:10.1021/jm400390r.

Signal-dependent repression of DUSP5 by class I HDACs controls nuclear ERK activity and cardiomyocyte hypertrophy.

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Ferguson BS, Harrison BC, Jeong MY, et al. Signal-dependent repression of DUSP5 by class I HDACs controls nuclear ERK activity and cardiomyocyte hypertrophy. Proc Natl Acad Sci U S A. 2013;110(24):9806-11. doi:10.1073/pnas.1301509110.

Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation.

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Frumm SM, Fan ZP, Ross KN, et al. Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation. Chem Biol. 2013;20(5):713-25. doi:10.1016/j.chembiol.2013.03.020.

Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.

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Wagner FF, Olson DE, Gale JP, et al. Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. J Med Chem. 2013;56(4):1772-6. doi:10.1021/jm301355j.

Design, synthesis, and evaluation of hydroxamic acid-based molecular probes for in vivo imaging of histone deacetylase (HDAC) in brain.

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Wang C, Eessalu TE, Barth VN, et al. Design, synthesis, and evaluation of hydroxamic acid-based molecular probes for in vivo imaging of histone deacetylase (HDAC) in brain. Am J Nucl Med Mol Imaging. 2013;4(1):29-38.

A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and alters mouse behavior in two mood-related tests.

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Schroeder FA, Lewis MC, Fass DM, et al. A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and alters mouse behavior in two mood-related tests. PLoS One. 2013;8(8):e71323. doi:10.1371/journal.pone.0071323.

Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries.

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Lowe JT, Lee MD, Akella LB, et al. Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries. J Org Chem. 2012;77(17):7187-211. doi:10.1021/jo300974j.