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Chemical Biology and Therapeutics Science Program

Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells.

Yuan Y, Tang AJ, Castoreno AB, et al. Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells. Cell Death Dis. 2013;4:e690. doi:10.1038/cddis.2013.191

Small-molecule inhibitors of cytokine-mediated STAT1 signal transduction in β-cells with improved aqueous solubility.

Scully SS, Tang AJ, Lundh M, Mosher CM, Perkins KM, Wagner BK. Small-molecule inhibitors of cytokine-mediated STAT1 signal transduction in β-cells with improved aqueous solubility. J Med Chem. 2013;56(10):4125-9. doi:10.1021/jm400397x

Discovery of small-molecule enhancers of reactive oxygen species that are nontoxic or cause genotype-selective cell death.

Adams DJ, Bošković Žarko V, Theriault JR, et al. Discovery of small-molecule enhancers of reactive oxygen species that are nontoxic or cause genotype-selective cell death. ACS Chem Biol. 2013;8(5):923-9. doi:10.1021/cb300653v

Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies.

Dockendorff C, Nagiec MM, Weïwer M, et al. Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies. ACS Med Chem Lett. 2012;3(10):808-813. doi:10.1021/ml300172p

Synthesis, cellular evaluation, and mechanism of action of piperlongumine analogs.

Adams DJ, Dai M, Pellegrino G, et al. Synthesis, cellular evaluation, and mechanism of action of piperlongumine analogs. Proc Natl Acad Sci U S A. 2012;109(38):15115-20. doi:10.1073/pnas.1212802109

A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma.

Yuan Y, Wang Q, Paulk J, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012;7(7):1152-7. doi:10.1021/cb300139y

Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis.

Chou DHC, Holson EB, Wagner FF, et al. Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis. Chem Biol. 2012;19(6):669-73. doi:10.1016/j.chembiol.2012.05.010

A human islet cell culture system for high-throughput screening.

Walpita D, Hasaka T, Spoonamore J, et al. A human islet cell culture system for high-throughput screening. J Biomol Screen. 2012;17(4):509-18. doi:10.1177/1087057111430253

Unbiased binding assays for discovering small-molecule probes and drugs.

Kemp MM, Weïwer M, Koehler AN. Unbiased binding assays for discovering small-molecule probes and drugs. Bioorg Med Chem. 2012;20(6):1979-89. doi:10.1016/j.bmc.2011.11.071

GW8510 increases insulin expression in pancreatic alpha cells through activation of p53 transcriptional activity.

Fomina-Yadlin D, Kubicek S, Vetere A, et al. GW8510 increases insulin expression in pancreatic alpha cells through activation of p53 transcriptional activity. PLoS One. 2012;7(1):e28808. doi:10.1371/journal.pone.0028808