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Center for the Development of Therapeutics

A High-Throughput Platform to Identify Small-Molecule Inhibitors of CRISPR-Cas9.
Maji B, Gangopadhyay SA, Lee M, et al. A High-Throughput Platform to Identify Small-Molecule Inhibitors of CRISPR-Cas9. Cell. 2019;177(4):1067-1079.e19. doi:10.1016/j.cell.2019.04.009.
Publisher Correction: Side chain determinants of biopolymer function during selection and replication.
Lichtor PA, Chen Z, Elowe NH, Chen JC, Liu DR. Publisher Correction: Side chain determinants of biopolymer function during selection and replication. Nat Chem Biol. 2019;15(5):550. doi:10.1038/s41589-019-0254-1.
Synthetic Lethality of Wnt Pathway Activation and Asparaginase in Drug-Resistant Acute Leukemias.
Hinze L, Pfirrmann M, Karim S, et al. Synthetic Lethality of Wnt Pathway Activation and Asparaginase in Drug-Resistant Acute Leukemias. Cancer Cell. 2019;35(4):664-676.e7. doi:10.1016/j.ccell.2019.03.004.
WRN helicase is a synthetic lethal target in microsatellite unstable cancers.
Chan EM, Shibue T, McFarland JM, et al. WRN helicase is a synthetic lethal target in microsatellite unstable cancers. Nature. 2019. doi:10.1038/s41586-019-1102-x.
A GPX4-dependent cancer cell state underlies the clear-cell morphology and confers sensitivity to ferroptosis.
Zou Y, Palte MJ, Deik AA, et al. A GPX4-dependent cancer cell state underlies the clear-cell morphology and confers sensitivity to ferroptosis. Nat Commun. 2019;10(1):1617. doi:10.1038/s41467-019-09277-9.
The novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies.
Christian S, Merz C, Evans L, et al. The novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies. Leukemia. 2019. doi:10.1038/s41375-019-0461-5.
Genome-wide interrogation of human cancers identifies EGLN1 dependency in clear cell ovarian cancers.
Price C, Gill S, Ho ZV, et al. Genome-wide interrogation of human cancers identifies EGLN1 dependency in clear cell ovarian cancers. Cancer Res. 2019. doi:10.1158/0008-5472.CAN-18-2674.
Crystal structure of MICU2 and comparison with MICU1 reveal insights into the uniporter gating mechanism.
Kamer KJ, Jiang W, Kaushik VK, Mootha VK, Grabarek Z. Crystal structure of MICU2 and comparison with MICU1 reveal insights into the uniporter gating mechanism. Proc Natl Acad Sci U S A. 2019;116(9):3546-3555. doi:10.1073/pnas.1817759116.
Development of a novel, sensitive cell-based corin assay.
Lambertz P, Theisen L, Längst N, et al. Development of a novel, sensitive cell-based corin assay. Biochem Pharmacol. 2019;160:62-70. doi:10.1016/j.bcp.2018.12.009.
Glycogen synthase kinase 3-β inhibition induces lymphangiogenesis through β-catenin-dependent and mTOR-independent pathways.
Stump B, Shrestha S, Lamattina AM, et al. Glycogen synthase kinase 3-β inhibition induces lymphangiogenesis through β-catenin-dependent and mTOR-independent pathways. PLoS One. 2019;14(4):e0213831. doi:10.1371/journal.pone.0213831.
Novel tricyclic glycal-based inducers that reprogram LDL metabolism in hepatic cells.
Nagiec MM, Duvall JR, Skepner AP, et al. Novel tricyclic glycal-based inducers that reprogram LDL metabolism in hepatic cells. Medchemcomm. 2018;9(11):1831-1842. doi:10.1039/c8md00297e.
High Throughput Screen Identifies Interferon γ-Dependent Inhibitors of Toxoplasma gondii Growth.
Radke JB, Carey KL, Shaw S, et al. High Throughput Screen Identifies Interferon γ-Dependent Inhibitors of Toxoplasma gondii Growth. ACS Infect Dis. 2018;4(10):1499-1507. doi:10.1021/acsinfecdis.8b00135.
High-Throughput Screens To Identify Autophagy Inducers That Function by Disrupting Beclin 1/Bcl-2 Binding.
Chiang W-C, Wei Y, Kuo Y-C, et al. High-Throughput Screens To Identify Autophagy Inducers That Function by Disrupting Beclin 1/Bcl-2 Binding. ACS Chem Biol. 2018;13(8):2247-2260. doi:10.1021/acschembio.8b00421.
Second-generation DNA-templated macrocycle libraries for the discovery of bioactive small molecules.
Usanov DL, Chan AI, Maianti JPablo, Liu DR. Second-generation DNA-templated macrocycle libraries for the discovery of bioactive small molecules. Nat Chem. 2018;10(7):704-714. doi:10.1038/s41557-018-0033-8.
Functionally Biased D2R Antagonists: Targeting the β-Arrestin Pathway to Improve Antipsychotic Treatment.
Weïwer M, Xu Q, Gale JP, et al. Functionally Biased D2R Antagonists: Targeting the β-Arrestin Pathway to Improve Antipsychotic Treatment. ACS Chem Biol. 2018;13(4):1038-1047. doi:10.1021/acschembio.8b00168.
Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia.
Wagner FF, Benajiba L, Campbell AJ, et al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018;10(431). doi:10.1126/scitranslmed.aam8460.
Targeting a Therapy-Resistant Cancer Cell State Using Masked Electrophiles as GPX4 Inhibitors
Eaton JK, Furst L, Ruberto RA, et al. Targeting a Therapy-Resistant Cancer Cell State Using Masked Electrophiles as GPX4 Inhibitors. bioRxiv. 2018. doi:10.1101/376764.
The Autophagy-Related Beclin-1 Protein Requires the Coiled-Coil and BARA Domains To Form a Homodimer with Submicromolar Affinity.
Ranaghan MJ, Durney MA, Mesleh MF, et al. The Autophagy-Related Beclin-1 Protein Requires the Coiled-Coil and BARA Domains To Form a Homodimer with Submicromolar Affinity. Biochemistry. 2017;56(51):6639-6651. doi:10.1021/acs.biochem.7b00936.
Genomic Activation of PPARG Reveals a Candidate Therapeutic Axis in Bladder Cancer.
Goldstein JT, Berger AC, Shih J, et al. Genomic Activation of PPARG Reveals a Candidate Therapeutic Axis in Bladder Cancer. Cancer Res. 2017;77(24):6987-6998. doi:10.1158/0008-5472.CAN-17-1701.
A dataset of images and morphological profiles of 30 000 small-molecule treatments using the Cell Painting assay.
Bray M-A, Gustafsdottir SM, Rohban MH, et al. A dataset of images and morphological profiles of 30 000 small-molecule treatments using the Cell Painting assay. Gigascience. 2017;6(12):1-5. doi:10.1093/gigascience/giw014.
A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles.
Subramanian A, Narayan R, Corsello SM, et al. A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles. Cell. 2017;171(6):1437-1452.e17. doi:10.1016/j.cell.2017.10.049.
Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells.
Johannessen, iv L, Sundberg TB, O'Connell DJ, et al. Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nat Chem Biol. 2017;13(10):1102-1108. doi:10.1038/nchembio.2458.
Potential role of intratumor bacteria in mediating tumor resistance to the chemotherapeutic drug gemcitabine.
Geller LT, Barzily-Rokni M, Danino T, et al. Potential role of intratumor bacteria in mediating tumor resistance to the chemotherapeutic drug gemcitabine. Science. 2017;357(6356):1156-1160. doi:10.1126/science.aah5043.
Genetic analysis in UK Biobank links insulin resistance and transendothelial migration pathways to coronary artery disease.
Klarin D, Zhu QMartin, Emdin CA, et al. Genetic analysis in UK Biobank links insulin resistance and transendothelial migration pathways to coronary artery disease. Nat Genet. 2017;49(9):1392-1397. doi:10.1038/ng.3914.
A small-molecule allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase.
Wellington S, Nag PP, Michalska K, et al. A small-molecule allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase. Nat Chem Biol. 2017;13(9):943-950. doi:10.1038/nchembio.2420.
Identification of Highly Specific Diversity-Oriented Synthesis-Derived Inhibitors of Clostridium difficile.
Duvall JR, Bedard L, Naylor-Olsen AM, et al. Identification of Highly Specific Diversity-Oriented Synthesis-Derived Inhibitors of Clostridium difficile. ACS Infect Dis. 2017;3(5):349-359. doi:10.1021/acsinfecdis.6b00206.
The Drug Repurposing Hub: a next-generation drug library and information resource.
Corsello SM, Bittker JA, Liu Z, et al. The Drug Repurposing Hub: a next-generation drug library and information resource. Nat Med. 2017;23(4):405-408. doi:10.1038/nm.4306.
Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes.
Sharabi K, Lin H, Tavares CDJ, et al. Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017;169(1):148-160.e15. doi:10.1016/j.cell.2017.03.001.
High Throughput Screening Methods: Evolution and Refinement
Bittker JA, Ross NT. High Throughput Screening Methods: Evolution and Refinement. Royal Society of Chemistry; 2017. doi:10.1039/9781782626770.
Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia.
Lewis TA, Sykes DB, Law JM, et al. Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ACS Med Chem Lett. 2016;7(12):1112-1117. doi:10.1021/acsmedchemlett.6b00316.
Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cells.
Lopez-Sambrooks C, Shrimal S, Khodier C, et al. Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cells. Nat Chem Biol. 2016;12(12):1023-1030. doi:10.1038/nchembio.2194.
Structural and conformational determinants of macrocycle cell permeability.
Over B, Matsson P, Tyrchan C, et al. Structural and conformational determinants of macrocycle cell permeability. Nat Chem Biol. 2016;12(12):1065-1074. doi:10.1038/nchembio.2203.
RNF166 Determines Recruitment of Adaptor Proteins during Antibacterial Autophagy.
Heath RJ, Goel G, Baxt LA, et al. RNF166 Determines Recruitment of Adaptor Proteins during Antibacterial Autophagy. Cell Rep. 2016;17(9):2183-2194. doi:10.1016/j.celrep.2016.11.005.
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 M-A, 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.
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.
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.
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.
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.
Wagner FF, Lundh M, Kaya T, et al. An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. ACS Chem Biol. 2016;11(2):363-74. doi:10.1021/acschembio.5b00640.
Correlating chemical sensitivity and basal gene expression reveals mechanism of action.
Rees MG, Seashore-Ludlow B, Cheah JH, et al. Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Nat Chem Biol. 2016;12(2):109-16. doi:10.1038/nchembio.1986.
Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics.
de Waal L, Lewis TA, Rees MG, et al. Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nat Chem Biol. 2016;12(2):102-8. doi:10.1038/nchembio.1984.
Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset.
Seashore-Ludlow B, Rees MG, Cheah JH, et al. Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset. Cancer Discov. 2015;5(11):1210-23. doi:10.1158/2159-8290.CD-15-0235.
Ubiquitin Ligase TRIM62 Regulates CARD9-Mediated Anti-fungal Immunity and Intestinal Inflammation.
Cao Z, Conway KL, Heath RJ, et al. Ubiquitin Ligase TRIM62 Regulates CARD9-Mediated Anti-fungal Immunity and Intestinal Inflammation. Immunity. 2015;43(4):715-26. doi:10.1016/j.immuni.2015.10.005.
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
Schreiber SL, Kotz JD, Li M, et al. Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell. 2015;161(6):1252-65. doi:10.1016/j.cell.2015.05.023.
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. doi:10.1016/j.celrep.2015.01.017.
Target-based identification of whole-cell active inhibitors of biotin biosynthesis in Mycobacterium tuberculosis.
Park SWoong, 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 Y-L, 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.
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.
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.
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.
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.
An unbiased approach to identify endogenous substrates of "histone" deacetylase 8.
Olson DE, Udeshi ND, Wolfson NA, et al. An unbiased approach to identify endogenous substrates of "histone" deacetylase 8. ACS Chem Biol. 2014;9(10):2210-6. doi:10.1021/cb500492r.
Toward performance-diverse small-molecule libraries for cell-based phenotypic screening using multiplexed high-dimensional profiling.
Wawer MJ, Li K, Gustafsdottir SM, et al. Toward performance-diverse small-molecule libraries for cell-based phenotypic screening using multiplexed high-dimensional profiling. Proc Natl Acad Sci U S A. 2014;111(30):10911-6. doi:10.1073/pnas.1410933111.
Cyclin D1-Cdk4 controls glucose metabolism independently of cell cycle progression.
Lee Y, Dominy JE, Choi YJong, et al. Cyclin D1-Cdk4 controls glucose metabolism independently of cell cycle progression. Nature. 2014;510(7506):547-51. doi:10.1038/nature13267.
A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein.
Pop MS, Stransky N, Garvie CW, et al. A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein. Mol Cancer Ther. 2014;13(6):1492-502. doi:10.1158/1535-7163.MCT-13-0689.
Impact of stereospecific intramolecular hydrogen bonding on cell permeability and physicochemical properties.
Over B, McCarren P, Artursson P, et al. Impact of stereospecific intramolecular hydrogen bonding on cell permeability and physicochemical properties. J Med Chem. 2014;57(6):2746-54. doi:10.1021/jm500059t.
Phenothiazines induce PP2A-mediated apoptosis in T cell acute lymphoblastic leukemia.
Gutierrez A, Pan L, Groen RWJ, et al. Phenothiazines induce PP2A-mediated apoptosis in T cell acute lymphoblastic leukemia. J Clin Invest. 2014;124(2):644-55. doi:10.1172/JCI65093.
Selective HDAC inhibition for the disruption of latent HIV-1 infection.
Barton KM, Archin NM, Keedy KS, et al. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014;9(8):e102684. doi:10.1371/journal.pone.0102684.
A small-molecule inducer of PDX1 expression identified by high-throughput screening.
Yuan Y, Hartland K, Boskovic Z, et al. A small-molecule inducer of PDX1 expression identified by high-throughput screening. Chem Biol. 2013;20(12):1513-22. doi:10.1016/j.chembiol.2013.10.013.
Niche-based screening identifies small-molecule inhibitors of leukemia stem cells.
Hartwell KA, Miller PG, Mukherjee S, et al. Niche-based screening identifies small-molecule inhibitors of leukemia stem cells. Nat Chem Biol. 2013;9(12):840-848. doi:10.1038/nchembio.1367.
Analysis of the activities of RAD54, a SWI2/SNF2 protein, using a specific small-molecule inhibitor.
Deakyne JS, Huang F, Negri J, Tolliday N, Cocklin S, Mazin AV. Analysis of the activities of RAD54, a SWI2/SNF2 protein, using a specific small-molecule inhibitor. J Biol Chem. 2013;288(44):31567-80. doi:10.1074/jbc.M113.502195.
An interactive resource to identify cancer genetic and lineage dependencies targeted by small molecules.
Basu A, Bodycombe NE, Cheah JH, et al. An interactive resource to identify cancer genetic and lineage dependencies targeted by small molecules. Cell. 2013;154(5):1151-1161. doi:10.1016/j.cell.2013.08.003.
FDG-PET imaging reveals local brain glucose utilization is altered by class I histone deacetylase inhibitors.
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.
Class I HDAC imaging using [ (3)H]CI-994 autoradiography.
Wang Y, Zhang Y-L, Hennig K, et al. Class I HDAC imaging using [ (3)H]CI-994 autoradiography. Epigenetics. 2013;8(7):756-64. doi:10.4161/epi.25202.
Discovery of the first histone deacetylase 6/8 dual inhibitors.
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.
Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation.
Frumm SM, Fan ZPeng, 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.
An informatic pipeline for managing high-throughput screening experiments and analyzing data from stereochemically diverse libraries.
Mulrooney CA, Lahr DL, Quintin MJ, et al. An informatic pipeline for managing high-throughput screening experiments and analyzing data from stereochemically diverse libraries. J Comput Aided Mol Des. 2013;27(5):455-68. doi:10.1007/s10822-013-9641-y.
Human genetics in rheumatoid arthritis guides a high-throughput drug screen of the CD40 signaling pathway.
Li G, Diogo D, Wu D, et al. Human genetics in rheumatoid arthritis guides a high-throughput drug screen of the CD40 signaling pathway. PLoS Genet. 2013;9(5):e1003487. doi:10.1371/journal.pgen.1003487.
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
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.
ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans.
Youngsaye W, Hartland CL, Morgan BJ, et al. ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans. Beilstein J Org Chem. 2013;9:1501-7. doi:10.3762/bjoc.9.171.
A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and alters mouse behavior in two mood-related tests.
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.
Screening for inhibitors of an essential chromatin remodeler in mouse embryonic stem cells by monitoring transcriptional regulation.
Dykhuizen EC, Carmody LC, Tolliday N, Crabtree GR, Palmer MAJ. Screening for inhibitors of an essential chromatin remodeler in mouse embryonic stem cells by monitoring transcriptional regulation. J Biomol Screen. 2012;17(9):1221-30. doi:10.1177/1087057112455060.
Identification of regulators of polyploidization presents therapeutic targets for treatment of AMKL.
Wen Q, Goldenson B, Silver SJ, et al. Identification of regulators of polyploidization presents therapeutic targets for treatment of AMKL. Cell. 2012;150(3):575-89. doi:10.1016/j.cell.2012.06.032.
Overcoming fluconazole resistance in Candida albicans clinical isolates with tetracyclic indoles.
Youngsaye W, Dockendorff C, Vincent B, et al. Overcoming fluconazole resistance in Candida albicans clinical isolates with tetracyclic indoles. Bioorg Med Chem Lett. 2012;22(9):3362-5. doi:10.1016/j.bmcl.2012.02.035.
High-Throughput RT-PCR for small-molecule screening assays.
Bittker JA. High-Throughput RT-PCR for small-molecule screening assays. Curr Protoc Chem Biol. 2012;4(1):49-63. doi:10.1002/9780470559277.ch110204.
The intersection of genetic and chemical genomic screens identifies GSK-3α as a target in human acute myeloid leukemia.
Banerji V, Frumm SM, Ross KN, et al. The intersection of genetic and chemical genomic screens identifies GSK-3α as a target in human acute myeloid leukemia. J Clin Invest. 2012;122(3):935-47. doi:10.1172/JCI46465.
Development of small-molecule probes that selectively kill cells induced to express mutant RAS.
Weïwer M, Bittker JA, Lewis TA, et al. Development of small-molecule probes that selectively kill cells induced to express mutant RAS. Bioorg Med Chem Lett. 2012;22(4):1822-6. doi:10.1016/j.bmcl.2011.09.047.
A chemical screen probing the relationship between mitochondrial content and cell size.
Kitami T, Logan DJ, Negri J, et al. A chemical screen probing the relationship between mitochondrial content and cell size. PLoS One. 2012;7(3):e33755. doi:10.1371/journal.pone.0033755.
Discovery of Potent and Highly Selective Inhibitors of GSK3b
W. An F, Germain AR, Bishop J, et al. Discovery of Potent and Highly Selective Inhibitors of GSK3b. Bethesda, MD: National Center for Biotechnology Information (US); 2012. Available at: https://www.ncbi.nlm.nih.gov/books/NBK133436/.
Identification of small-molecule inhibitors of Trypansoma cruzi replication.
Germain AR, Carmody LC, Dockendorff C, et al. Identification of small-molecule inhibitors of Trypansoma cruzi replication. Bioorg Med Chem Lett. 2011;21(23):7197-200. doi:10.1016/j.bmcl.2011.09.057.
Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates.
Youngsaye W, Vincent B, Hartland CL, et al. Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. Bioorg Med Chem Lett. 2011;21(18):5502-5. doi:10.1016/j.bmcl.2011.06.105.
Selective killing of cancer cells by a small molecule targeting the stress response to ROS.
Raj L, Ide T, Gurkar AU, et al. Selective killing of cancer cells by a small molecule targeting the stress response to ROS. Nature. 2011;475(7355):231-4. doi:10.1038/nature10167.
Selective killing of K-ras mutant cancer cells by small molecule inducers of oxidative stress.
Shaw AT, Winslow MM, Magendantz M, et al. Selective killing of K-ras mutant cancer cells by small molecule inducers of oxidative stress. Proc Natl Acad Sci U S A. 2011;108(21):8773-8. doi:10.1073/pnas.1105941108.
Small-molecule inducers of insulin expression in pancreatic alpha-cells.
Fomina-Yadlin D, Kubicek S, Walpita D, et al. Small-molecule inducers of insulin expression in pancreatic alpha-cells. Proc Natl Acad Sci U S A. 2010;107(34):15099-104. doi:10.1073/pnas.1010018107.
Cell-based assays for high-throughput screening.
W An F, Tolliday N. Cell-based assays for high-throughput screening. Mol Biotechnol. 2010;45(2):180-6. doi:10.1007/s12033-010-9251-z.
Identifying the proteins to which small-molecule probes and drugs bind in cells.
Ong S-E, Schenone M, Margolin AA, et al. Identifying the proteins to which small-molecule probes and drugs bind in cells. Proc Natl Acad Sci U S A. 2009;106(12):4617-22. doi:10.1073/pnas.0900191106.
Small-molecule inhibitors of HIF-2a translation link its 5'UTR iron-responsive element to oxygen sensing.
Zimmer M, Ebert BL, Neil C, et al. Small-molecule inhibitors of HIF-2a translation link its 5'UTR iron-responsive element to oxygen sensing. Mol Cell. 2008;32(6):838-48. doi:10.1016/j.molcel.2008.12.004.
ChemBank: a small-molecule screening and cheminformatics resource database.
Seiler KPetri, George GA, Happ MPat, et al. ChemBank: a small-molecule screening and cheminformatics resource database. Nucleic Acids Res. 2008;36(Database issue):D351-9. doi:10.1093/nar/gkm843.
Small molecules, big players: the National Cancer Institute's Initiative for Chemical Genetics.
Tolliday N, Clemons PA, Ferraiolo P, et al. Small molecules, big players: the National Cancer Institute's Initiative for Chemical Genetics. Cancer Res. 2006;66(18):8935-42. doi:10.1158/0008-5472.CAN-06-2552.