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Center for the Development of Therapeutics

Point mutations at the catalytic site of PCSK9 inhibit folding, autoprocessing, and interaction with the LDL receptor.

Garvie CW, Fraley CV, Elowe NH, et al. Point mutations at the catalytic site of PCSK9 inhibit folding, autoprocessing, and interaction with the LDL receptor. Protein Sci. 2016;25(11):2018-2027. doi:10.1002/pro.3019

Diversity-oriented synthesis yields novel multistage antimalarial inhibitors.

Kato N, Comer E, Sakata-Kato T, et al. Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. Nature. 2016;538(7625):344-349. doi:10.1038/nature19804

Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1.

Law JM, Stark SC, Liu K, et al. Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1. ACS Med Chem Lett. 2016;7(10):944-949. doi:10.1021/acsmedchemlett.6b00264

Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia.

Sykes DB, Kfoury YS, Mercier FE, et al. Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia. Cell. 2016;167(1):171-186.e15. doi:10.1016/j.cell.2016.08.057

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.

Wagner FF, Weïwer M, Steinbacher S, et al. Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. Bioorg Med Chem. 2016;24(18):4008-4015. doi:10.1016/j.bmc.2016.06.040

Cell Painting, a high-content image-based assay for morphological profiling using multiplexed fluorescent dyes.

Bray MA, Singh S, Han H, et al. Cell Painting, a high-content image-based assay for morphological profiling using multiplexed fluorescent dyes. Nat Protoc. 2016;11(9):1757-74. doi:10.1038/nprot.2016.105

Genomic Copy Number Dictates a Gene-Independent Cell Response to CRISPR/Cas9 Targeting.

Aguirre AJ, Meyers RM, Weir BA, et al. Genomic Copy Number Dictates a Gene-Independent Cell Response to CRISPR/Cas9 Targeting. Cancer Discov. 2016;6(8):914-29. doi:10.1158/2159-8290.CD-16-0154

Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects.

Wagner FF, Bishop JA, Gale JP, et al. Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects. ACS Chem Biol. 2016;11(7):1952-63. doi:10.1021/acschembio.6b00306

Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.

Bošković ŽV, Kemp MM, Freedy AM, et al. Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile. ACS Chem Biol. 2016;11(7):1844-51. doi:10.1021/acschembio.6b00012

Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors.

Huang F, Goyal N, Sullivan K, et al. Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors. Nucleic Acids Res. 2016;44(9):4189-99. doi:10.1093/nar/gkw087