Chemical Biology and Therapeutics Science
Phenotypic Screening for Small Molecules that Protect β-Cells from Glucolipotoxicity. ACS Chem Biol. 2022. doi:10.1021/acschembio.2c00052.
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.
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. .
Targeting a Therapy-Resistant Cancer Cell State Using Masked Electrophiles as GPX4 Inhibitors. bioRxiv. 2018. doi:10.1101/376764.
A programmable Cas9-serine recombinase fusion protein that operates on DNA sequences in mammalian cells. Nucleic Acids Res. 2016;44(20):9758-9770. doi:10.1093/nar/gkw707. .
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. Nature. 2016;538(7625):344-349. doi:10.1038/nature19804.
Inhibition of DYRK1A Stimulates Human β-Cell Proliferation. Diabetes. 2016;65(6):1660-71. doi:10.2337/db15-1127.
Programmable editing of a target base in genomic DNA without double-stranded DNA cleavage. Nature. 2016;533(7603):420-4. doi:10.1038/nature17946. .
Continuous evolution of Bacillus thuringiensis toxins overcomes insect resistance. Nature. 2016;533(7601):58-63. doi:10.1038/nature17938.
Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Nat Chem Biol. 2016;12(2):109-16. doi:10.1038/nchembio.1986.
Discovery and characterization of a peptide that enhances endosomal escape of delivered proteins in vitro and in vivo. J Am Chem Soc. 2015;137(44):14084-93. doi:10.1021/jacs.5b05694.
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.
Development of potent in vivo mutagenesis plasmids with broad mutational spectra. Nat Commun. 2015;6:8425. doi:10.1038/ncomms9425. .
Continuous directed evolution of DNA-binding proteins to improve TALEN specificity. Nat Methods. 2015;12(10):939-42. doi:10.1038/nmeth.3515.
KRAS Genomic Status Predicts the Sensitivity of Ovarian Cancer Cells to Decitabine. Cancer Res. 2015;75(14):2897-906. doi:10.1158/0008-5472.CAN-14-2860.
Small molecule-triggered Cas9 protein with improved genome-editing specificity. Nat Chem Biol. 2015;11(5):316-8. doi:10.1038/nchembio.1793. .
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.
Synthesis of oxazocenones via gold(I)-catalyzed 8-endo-dig hydroalkoxylation of alkynamides. Org Lett. 2015;17(3):418-21. doi:10.1021/ol503273v. .
Cationic lipid-mediated delivery of proteins enables efficient protein-based genome editing in vitro and in vivo. Nat Biotechnol. 2015;33(1):73-80. doi:10.1038/nbt.3081.
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.
Electrophilic activity-based RNA probes reveal a self-alkylating RNA for RNA labeling. Nat Chem Biol. 2014;10(12):1049-54. doi:10.1038/nchembio.1655. .
A system for the continuous directed evolution of proteases rapidly reveals drug-resistance mutations. Nat Commun. 2014;5:5352. doi:10.1038/ncomms6352. .
Diversity-oriented synthesis-facilitated medicinal chemistry: toward the development of novel antimalarial agents. J Med Chem. 2014;57(20):8496-502. doi:10.1021/jm500994n.
NAMPT is the cellular target of STF-31-like small-molecule probes. ACS Chem Biol. 2014;9(10):2247-54. doi:10.1021/cb500347p.
Reprogramming the specificity of sortase enzymes. Proc Natl Acad Sci U S A. 2014;111(37):13343-8. doi:10.1073/pnas.1411179111. .
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.
Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones. Nature. 2014;511(7507):94-8. doi:10.1038/nature13297.
Automated Structure-Activity Relationship Mining: Connecting Chemical Structure to Biological Profiles. J Biomol Screen. 2014;19(5):738-48. doi:10.1177/1087057114530783.
Connecting Small Molecules with Similar Assay Performance Profiles Leads to New Biological Hypotheses. J Biomol Screen. 2014;19(5):771-81. doi:10.1177/1087057113520226.
Fusion of catalytically inactive Cas9 to FokI nuclease improves the specificity of genome modification. Nat Biotechnol. 2014;32(6):577-82. doi:10.1038/nbt.2909. .
Broad specificity profiling of TALENs results in engineered nucleases with improved DNA-cleavage specificity. Nat Methods. 2014;11(4):429-35. doi:10.1038/nmeth.2845.
Negative selection and stringency modulation in phage-assisted continuous evolution. Nat Chem Biol. 2014;10(3):216-22. doi:10.1038/nchembio.1453. .
Identification of ligand-target pairs from combined libraries of small molecules and unpurified protein targets in cell lysates. J Am Chem Soc. 2014;136(8):3264-70. doi:10.1021/ja412934t. .
Quantitative-proteomic comparison of alpha and Beta cells to uncover novel targets for lineage reprogramming. PLoS One. 2014;9(4):e95194. doi:10.1371/journal.pone.0095194.
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.
Synthesis of piperlogs and analysis of their effects on cells. Tetrahedron. 2013;69(36). doi:10.1016/j.tet.2013.05.080. .
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.
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. 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. 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. ACS Med Chem Lett. 2012;3(10):808-813. doi:10.1021/ml300172p.
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. ACS Chem Biol. 2012;7(7):1152-7. doi:10.1021/cb300139y.
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. J Biomol Screen. 2012;17(4):509-18. doi:10.1177/1087057111430253.
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. PLoS One. 2012;7(1):e28808. doi:10.1371/journal.pone.0028808.
Roscovitine inhibits EBNA1 serine 393 phosphorylation, nuclear localization, transcription, and episome maintenance. J Virol. 2011;85(6):2859-68. doi:10.1128/JVI.01628-10.
Small molecule microarrays enable the discovery of compounds that bind the Alzheimer's Aβ peptide and reduce its cytotoxicity. J Am Chem Soc. 2010;132(47):17015-22. doi:10.1021/ja107552s. .
Distinct biological network properties between the targets of natural products and disease genes. J Am Chem Soc. 2010;132(27):9259-61. doi:10.1021/ja102798t. .
A complex task? Direct modulation of transcription factors with small molecules. Curr Opin Chem Biol. 2010;14(3):331-40. doi:10.1016/j.cbpa.2010.03.022. .
Detecting protein-small molecule interactions using fluorous small-molecule microarrays. Methods Mol Biol. 2010;669:43-55. doi:10.1007/978-1-60761-845-4_4. .
Binding affinity and kinetic analysis of targeted small molecule-modified nanoparticles. Bioconjug Chem. 2010;21(1):14-9. doi:10.1021/bc900438a.
A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009;5(3):154-6. doi:10.1038/nchembio.142.
Small-molecule microarrays as tools in ligand discovery. Chem Soc Rev. 2008;37(7):1385-94. doi:10.1039/b703568n. .
Identification of the molecular target of small molecule inhibitors of HDL receptor SR-BI activity. Biochemistry. 2008;47(1):460-72. doi:10.1021/bi701277x.
Detecting binding interactions using microarrays of natural product extracts. J Am Chem Soc. 2007;129(37):11346-7. doi:10.1021/ja073965s. .
Influence of HDL-cholesterol-elevating drugs on the in vitro activity of the HDL receptor SR-BI. J Lipid Res. 2007;48(8):1832-45. doi:10.1194/jlr.M700209-JLR200.
A pipeline for ligand discovery using small-molecule microarrays. Curr Opin Chem Biol. 2007;11(1):74-82. doi:10.1016/j.cbpa.2006.11.031. .
Ring-opening and ring-closing reactions of a shikimic acid-derived substrate leading to diverse small molecules. J Comb Chem. 2007;9(2):245-53. doi:10.1021/cc060135m.
Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors. Angew Chem Int Ed Engl. 2007;46(42):7960-4. doi:10.1002/anie.200703198.
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.
A robust small-molecule microarray platform for screening cell lysates. Chem Biol. 2006;13(5):493-504. doi:10.1016/j.chembiol.2006.03.004.
A method for the covalent capture and screening of diverse small molecules in a microarray format. Nat Protoc. 2006;1(5):2344-52. doi:10.1038/nprot.2006.282. .
The role of lysine 55 in determining the specificity of the purine repressor for its operators through minor groove interactions. J Mol Biol. 1999;291(2):347-61. doi:10.1006/jmbi.1999.2946. .