Center for the Development of Therapeutics
Three million images and morphological profiles of cells treated with matched chemical and genetic perturbations. Submitted. doi:10.1101/2022.01.05.475090.
Single-nucleus profiling of human dilated and hypertrophic cardiomyopathy. Nature. 2022. doi:10.1038/s41586-022-04817-8.
Protein Flexibility and Dissociation Pathway Differentiation Can Explain Onset Of Resistance Mutations in Kinases. Angew Chem Int Ed Engl. 2022. doi:10.1002/anie.202200983. .
High-Throughput Assay to Screen Small Molecules for Their Ability to Prevent Sickling of Red Blood Cells. ACS Omega. 2022;7(16):14009-14016. doi:10.1021/acsomega.2c00541.
Phenotypic Screening for Small Molecules that Protect β-Cells from Glucolipotoxicity. ACS Chem Biol. 2022. doi:10.1021/acschembio.2c00052.
Phosphate dysregulation via the XPR1-KIDINS220 protein complex is a therapeutic vulnerability in ovarian cancer. Nat Cancer. 2022. doi:10.1038/s43018-022-00360-7.
A screen of repurposed drugs identifies AMHR2/MISR2 agonists as potential contraceptives. Proc Natl Acad Sci U S A. 2022;119(15):e2122512119. doi:10.1073/pnas.2122512119.
Circuit topology predicts pathogenicity of missense mutations. Proteins. 2022. doi:10.1002/prot.26342. .
TAILS Identifies Candidate Substrates and Biomarkers of ADAMTS7, a Therapeutic Protease Target in Coronary Artery Disease. Mol Cell Proteomics. 2022;21(4):100223. doi:10.1016/j.mcpro.2022.100223.
Novel Fluorescence-Based High-Throughput FLIPR Assay Utilizing Membrane-Tethered Genetic Calcium Sensors to Identify T-Type Calcium Channel Modulators. ACS Pharmacol Transl Sci. 2022;5(3):156-168. doi:10.1021/acsptsci.1c00233.
Characterization of intrinsically disordered regions in proteins informed by human genetic diversity. PLoS Comput Biol. 2022;18(3):e1009911. doi:10.1371/journal.pcbi.1009911.
Biophysical analysis of the Mycobacteria tuberculosis peptide binding protein DppA reveals a stringent peptide binding pocket. Tuberculosis (Edinb). 2022;132:102157. doi:10.1016/j.tube.2021.102157.
Identification of Inhibitors of Fungal Fatty Acid Biosynthesis. ACS Infect Dis. 2021;7(12):3210-3223. doi:10.1021/acsinfecdis.1c00404.
Paralog knockout profiling identifies DUSP4 and DUSP6 as a digenic dependence in MAPK pathway-driven cancers. Nat Genet. 2021;53(12):1664-1672. doi:10.1038/s41588-021-00967-z.
Control of osteocyte dendrite formation by Sp7 and its target gene osteocrin. Nat Commun. 2021;12(1):6271. doi:10.1038/s41467-021-26571-7.
Rare, Damaging DNA Variants in and Risk of Coronary Artery Disease: Insights From Functional Genomics and Large-Scale Sequencing Analyses. Circ Genom Precis Med. 2021;14(5):e003399. doi:10.1161/CIRCGEN.121.003399.
Molecular basis for substrate recruitment to the PRMT5 methylosome. Mol Cell. 2021;81(17):3481-3495.e7. doi:10.1016/j.molcel.2021.07.019.
Coronary Disease Association With ADAMTS7 Is Due to Protease Activity. Circ Res. 2021;129(4):458-470. doi:10.1161/CIRCRESAHA.121.319163.
SARS-CoV spike proteins can compete for electrolytes in physiological fluids according to structure-based quantum-chemical calculations. Comput Theor Chem. 2021:113392. doi:10.1016/j.comptc.2021.113392. .
Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. J Med Chem. 2021. doi:10.1021/acs.jmedchem.1c00507.
The Use of Informer Sets in Screening: Perspectives on an Efficient Strategy to Identify New Probes.
The Use of Informer Sets in Screening: Perspectives on an Efficient Strategy to Identify New Probes. SLAS Discov. 2021;26(7):855-861. doi:10.1177/24725552211019410.
PRICKLE2 revisited-further evidence implicating PRICKLE2 in neurodevelopmental disorders. Eur J Hum Genet. 2021;29(8):1235-1244. doi:10.1038/s41431-021-00912-y.
Structure of PDE3A-SLFN12 complex reveals requirements for activation of SLFN12 RNase. Nat Commun. 2021;12(1):4375. doi:10.1038/s41467-021-24495-w.
Inhibition of Histone Deacetylases 1, 2, and 3 Enhances Clearance of Cholesterol Accumulation in Niemann-Pick C1 Fibroblasts. ACS Pharmacol Transl Sci. 2021;4(3):1136-1148. doi:10.1021/acsptsci.1c00033.
Oculocutaneous albinism type 1B associated with a functionally significant tyrosinase gene polymorphism detected with Whole Exome Sequencing. Ophthalmic Genet. 2021;42(3):291-295. doi:10.1080/13816810.2021.1888129.
Critical assessment of protein intrinsic disorder prediction. Nat Methods. 2021;18(5):472-481. doi:10.1038/s41592-021-01117-3. .
Multidose evaluation of 6,710 drug repurposing library identifies potent SARS-CoV-2 infection inhibitors and . bioRxiv. 2021. doi:10.1101/2021.04.20.440626.
Selective modulation of a pan-essential protein as a therapeutic strategy in cancer. Cancer Discov. 2021. doi:10.1158/2159-8290.CD-20-1213.
Predicting cell health phenotypes using image-based morphology profiling. Mol Biol Cell. 2021;32(9):995-1005. doi:10.1091/mbc.E20-12-0784.
Multigram Preparation of BRD4780 Enantiomers and Assignment of Absolute Stereochemistry. J Org Chem. 2021;86(5):4281-4289. doi:10.1021/acs.joc.0c02520. .
Characterization of the GABRB2-Associated Neurodevelopmental Disorders. Ann Neurol. 2021;89(3):573-586. doi:10.1002/ana.25985.
Targeting a Braf/Mapk pathway rescues podocyte lipid peroxidation in CoQ-deficiency kidney disease. J Clin Invest. 2021;131(5). doi:10.1172/JCI141380.
Assessing optimal: inequalities in codon optimization algorithms. BMC Biol. 2021;19(1):36. doi:10.1186/s12915-021-00968-8. .
Regulation of purine metabolism connects KCTD13 to a metabolic disorder with autistic features. iScience. 2021;24(1):101935. doi:10.1016/j.isci.2020.101935.
GSK3α, not GSK3β, drives hippocampal NMDAR-dependent LTD via tau-mediated spine anchoring. EMBO J. 2021;40(2):e105513. doi:10.15252/embj.2020105513.
Synthetic Lethal Interaction between the ESCRT Paralog Enzymes VPS4A and VPS4B in Cancers Harboring Loss of Chromosome 18q or 16q. Cell Rep. 2020;33(11):108493. doi:10.1016/j.celrep.2020.108493.
A High-Content Screen for Mucin-1-Reducing Compounds Identifies Fostamatinib as a Candidate for Rapid Repurposing for Acute Lung Injury. Cell Rep Med. 2020;1(8):100137. doi:10.1016/j.xcrm.2020.100137.
TFEB Transcriptional Responses Reveal Negative Feedback by BHLHE40 and BHLHE41. Cell Rep. 2020;33(6):108371. doi:10.1016/j.celrep.2020.108371.
Comprehensive characterization of amino acid positions in protein structures reveals molecular effect of missense variants. Proc Natl Acad Sci U S A. 2020;117(45):28201-28211. doi:10.1073/pnas.2002660117.
Predicting functional effects of missense variants in voltage-gated sodium and calcium channels. Sci Transl Med. 2020;12(556). doi:10.1126/scitranslmed.aay6848.
Multimodal small-molecule screening for human prion protein binders. J Biol Chem. 2020. doi:10.1074/jbc.RA120.014905.
MISCAST: MIssense variant to protein StruCture Analysis web SuiTe. Nucleic Acids Res. 2020;48(W1):W132-W139. doi:10.1093/nar/gkaa361.
A High Content Screen for Mucin-1-Reducing Compounds Identifies Fostamatinib as a Candidate for Rapid Repurposing for Acute Lung Injury during the COVID-19 pandemic. bioRxiv. 2020. doi:10.1101/2020.06.30.180380.
Cationic zinc is required for factor XII recruitment and activation by stimulated platelets and for thrombus formation in vivo. J Thromb Haemost. 2020. doi:10.1111/jth.14964.
Autism-Associated Shank3 Is Essential for Homeostatic Compensation in Rodent V1. Neuron. 2020;106(5):769-777.e4. doi:10.1016/j.neuron.2020.02.033.
Selective inhibition of glycogen synthase kinase 3α corrects pathophysiology in a mouse model of fragile X syndrome. Sci Transl Med. 2020;12(544). doi:10.1126/scitranslmed.aam8572.
Mechanistic insights into cancer cell killing through interaction of phosphodiesterase 3A and schlafen family member 12. J Biol Chem. 2020;295(11):3431-3446. doi:10.1074/jbc.RA119.011191.
Discovering the anti-cancer potential of non-oncology drugs by systematic viability profiling. Nat Cancer. 2020;1(2):235-248. doi:10.1038/s43018-019-0018-6.
Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1. J Med Chem. 2020;63(1):103-121. doi:10.1021/acs.jmedchem.9b00293.
Defining the landscape of ATP-competitive inhibitor resistance residues in protein kinases. Nat Struct Mol Biol. 2020;27(1):92-104. doi:10.1038/s41594-019-0358-z.
Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35. ACS Medicinal Chemistry Letters. 2020;11(11):2131-2138.
Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35. ACS Medicinal Chemistry Letters. 2020;11(11):2131-2138.
Current knowledge of SLC6A1-related neurodevelopmental disorders. Brain Commun. 2020;2(2):fcaa170. doi:10.1093/braincomms/fcaa170.
Histone deacetylases 1 and 2 inhibition suppresses cytokine production and osteoclast bone resorption in vitro. J Cell Biochem. 2020;121(1):244-258. doi:10.1002/jcb.29137.
Roles of glycogen synthase kinase 3 alpha and calcineurin in regulating the ability of sperm to fertilize eggs. FASEB J. 2020;34(1):1247-1269. doi:10.1096/fj.201902163R. .
Characterization of the Prion Protein Binding Properties of Antisense Oligonucleotides. Biomolecules. 2019;10(1). doi:10.3390/biom10010001.
Single cell census of human kidney organoids shows reproducibility and diminished off-target cells after transplantation. Nat Commun. 2019;10(1):5462. doi:10.1038/s41467-019-13382-0.
Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing. ACS Med Chem Lett. 2019;10(11):1537-1542. doi:10.1021/acsmedchemlett.9b00360.
Structural basis for the docking of mTORC1 on the lysosomal surface. Science. 2019;366(6464):468-475. doi:10.1126/science.aay0166.
Chasing Tails: Cathepsin-L Improves Structural Analysis of Histones by HX-MS. Mol Cell Proteomics. 2019;18(10):2089-2098. doi:10.1074/mcp.RA119.001325.
The novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies. Leukemia. 2019;33(10):2403-2415. doi:10.1038/s41375-019-0461-5.
Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers. Cell Rep. 2019;29(1):118-134.e8. doi:10.1016/j.celrep.2019.08.090.
Small Molecule Targets TMED9 and Promotes Lysosomal Degradation to Reverse Proteinopathy. Cell. 2019;178(3):521-535.e23. doi:10.1016/j.cell.2019.07.002.
Conservation of the structure and function of bacterial tryptophan synthases. IUCrJ. 2019;6(Pt 4):649-664. doi:10.1107/S2052252519005955.
Discovering metabolic disease gene interactions by correlated effects on cellular morphology. Mol Metab. 2019;24:108-119. doi:10.1016/j.molmet.2019.03.001.
Stabilization of the Max Homodimer with a Small Molecule Attenuates Myc-Driven Transcription. Cell Chem Biol. 2019;26(5):711-723.e14. doi:10.1016/j.chembiol.2019.02.009.
Genome-Wide Interrogation of Human Cancers Identifies EGLN1 Dependency in Clear Cell Ovarian Cancers. Cancer Res. 2019;79(10):2564-2579. doi:10.1158/0008-5472.CAN-18-2674.
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. 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. Cancer Cell. 2019;35(4):664-676.e7. doi:10.1016/j.ccell.2019.03.004.
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.
WRN helicase is a synthetic lethal target in microsatellite unstable cancers. Nature. 2019;568(7753):551-556. doi:10.1038/s41586-019-1102-x.
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. 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. PLoS One. 2019;14(4):e0213831. doi:10.1371/journal.pone.0213831.
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. 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. 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.
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. 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. Sci Transl Med. 2018;10(431). doi:10.1126/scitranslmed.aam8460.
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. Biochemistry. 2017;56(51):6639-6651. doi:10.1021/acs.biochem.7b00936.
Genomic Activation of 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. 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. 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. 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. 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. Nat Genet. 2017;49(9):1392-1397. doi:10.1038/ng.3914.
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. 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. Nat Med. 2017;23(4):405-408. doi:10.1038/nm.4306.
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. Royal Society of Chemistry; 2017. doi:10.1039/9781782626770. .
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. Nat Chem Biol. 2016;12(12):1023-1030. doi:10.1038/nchembio.2194.
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. 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. Protein Sci. 2016;25(11):2018-2027. doi:10.1002/pro.3019.
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. 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. 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. 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. 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. 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. 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. ACS Chem Biol. 2016;11(7):1952-63. doi:10.1021/acschembio.6b00306.
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. ACS Chem Biol. 2016;11(2):363-74. doi:10.1021/acschembio.5b00640.
Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nat Chem Biol. 2016;12(2):102-8. doi:10.1038/nchembio.1984.
Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Nat Chem Biol. 2016;12(2):109-16. doi:10.1038/nchembio.1986.
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. Immunity. 2015;43(4):715-26. doi:10.1016/j.immuni.2015.10.005.
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. 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. 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. 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. 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. 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. 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. 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. 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). 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. 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. 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. 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. Nature. 2014;510(7506):547-51. doi:10.1038/nature13267.
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. J Med Chem. 2014;57(6):2746-54. doi:10.1021/jm500059t.
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. PLoS One. 2014;9(8):e102684. doi:10.1371/journal.pone.0102684.
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. 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.
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. 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. Neurosci Lett. 2013;550:119-24. doi:10.1016/j.neulet.2013.06.016.
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. J Med Chem. 2013;56(11):4816-20. doi:10.1021/jm400390r.
Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation. Chem Biol. 2013;20(5):713-25. doi:10.1016/j.chembiol.2013.03.020.
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.
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.
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.
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.
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.
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.
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. 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. 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. 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. 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. PLoS One. 2012;7(3):e33755. doi:10.1371/journal.pone.0033755.
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