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Establishment of LCMS Based Platform for Discovery of Quorum Sensing Inhibitors: Signal Detection in Pseudomonas aeruginosa PAO1
10.1021/acschembio.7b00875 2018-01-18 Targeting the main three networking systems, viz. Las, RhI, and PQS, via natural quenchers is a new ray of hope for combating the persistent behavior of Pseudomonas aeruginosa. In the bacterial chemical vocabulary pyocyanin, N-AHLs and rhamnolipids are the ma... |
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Dual Allosteric Inhibition of SHP2 Phosphatase
10.1021/acschembio.7b00980 2018-01-18 SHP2 is a cytoplasmic protein tyrosine phosphatase encoded by the PTPN11 gene and is involved in cell proliferation, differentiation, and survival. Recently, we reported an allosteric mechanism of inhibition that stabilizes the auto-inhibited conformation of ... |
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Chemical Control of a CRISPR-Cas9 Acetyltransferase
10.1021/acschembio.7b00883 2018-01-17 Lysine acetyltransferases (KATs) play a critical role in the regulation of transcription and other genomic functions. However, a persistent challenge is the development of assays capable of defining KAT activity directly in living cells. Toward this goal, her... |
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Hsp70 Inhibits the Nucleation and Elongation of Tau and Sequesters Tau Aggregates with High Affinity
10.1021/acschembio.7b01039 2018-01-17 As a key player of the protein quality control network of the cell, the molecular chaperone Hsp70 inhibits the aggregation of the amyloid protein tau. To date, the mechanism of this inhibition and the tau species targeted by Hsp70 remain unknown. This is part... |
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Oxidatively Generated Lesions as Internal Photosensitizers for Pyrimidine Dimerization in DNA
10.1021/acschembio.7b01097 2018-01-17 In this work, the attention is focused on UVA-photosensitized reactions triggered by a DNA chromophore-containing lesion, namely 5-formyluracil. This is a major oxidatively generated lesion that exhibits an enhanced light absorption in the UVB–UVA region. The... |
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Protein Inhibitors of CRISPR-Cas9
10.1021/acschembio.7b00831 2018-01-17 Bacteria are under constant predation from viruses, called bacteriophages (phages). This threat has driven the evolution of multiple defense systems, including the CRISPR-Cas (clustered regularly interspaced short palindromic repeats and CRISPR associated gen... |
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Generation of Optogenetically Modified Adenovirus Vector for Spatiotemporally Controllable Gene Therapy
10.1021/acschembio.7b01058 2018-01-12 Gene therapy is expected to be utilized for the treatment of various diseases. However, the spatiotemporal resolution of current gene therapy technology is not high enough. In this study, we generated a new technology for spatiotemporally controllable gene th... |
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Investigation of Amide Bond Formation during Dehydrophos Biosynthesis
10.1021/acschembio.7b00949 2018-01-12 Dehydrophos is a tripeptide phosphonate antibiotic produced by Streptomyces luridus. Its biosynthetic pathway involves the use of aminoacyl-tRNA (aa-tRNA) for amide bond formation. The first amide bond during biosynthesis is formed by DhpH-C, a peptidyltransf... |
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Live Cell Visualization of Multiple Protein–Protein Interactions with BiFC Rainbow
10.1021/acschembio.7b00931 2018-01-11 As one of the most powerful tools to visualize PPIs in living cells, bimolecular fluorescence complementation (BiFC) has gained great advancement during recent years, including deep tissue imaging with far-red or near-infrared fluorescent proteins or super-re... |
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Development of Stabilized Peptide-Based PROTACs against Estrogen Receptor α
10.1021/acschembio.7b00985 2018-01-11 Peptide modulators targeting protein–protein interactions (PPIs) exhibit greater potential than small-molecule drugs in several important aspects including facile modification and relative large contact surface area. Stabilized peptides constructed by variabl... |