Phenotypic Screen Identifies JAK2 as a Major Regulator of FAT10 Expression.

abstract：:Thermodynamics and kinetics of protein-ligand binding are both important aspects for the design of novel drug molecules. Presently, thermodynamic data are collected with isothermal titration calorimetry, while kinetic data are mostly derived from surface plasmon resonance. The new method of kinITC provides both thermo...

journal_title：ACS chemical biology

authors： Glöckner S,Ngo K,Sager CP,Hüfner-Wulsdorf T,Heine A,Klebe G

更新日期：2020-03-20 00:00:00

abstract：:HIV infection is pandemic in humans and is responsible for millions of deaths every year. The discovery of new cellular targets that can be used to prevent the infection process represents a new opportunity for developing more effective antiviral drugs. In this context, dendritic cell-specific ICAM-3 grabbing non-inte...

journal_title：ACS chemical biology

authors： Sattin S,Daghetti A,Thépaut M,Berzi A,Sánchez-Navarro M,Tabarani G,Rojo J,Fieschi F,Clerici M,Bernardi A

更新日期：2010-03-19 00:00:00

abstract：:Recent advances in mass spectrometry (MS)-based proteomics allow the identification and quantitation of thousands of posttranslational modification (PTM) sites in a single experiment. This follows from the development of more effective class enrichment strategies, new high performance instrumentation and bioinformatic...

journal_title：ACS chemical biology

authors： Doll S,Burlingame AL

更新日期：2015-01-16 00:00:00

abstract：:G protein-coupled receptors (GPCRs) are an ubiquitously expressed class of transmembrane proteins involved in the signal transduction of neurotransmitters, hormones and various other ligands. Their signaling output is desensitized by mechanisms involving phosphorylation, internalization, and dissociation from G protei...

journal_title：ACS chemical biology

authors： Gehret AU,Hinkle PM

更新日期：2013-03-15 00:00:00

abstract：:Inducible modulation is often required for precise investigations and manipulations of dynamic biological processes. Transcription activator-like effectors (TALEs) provide a powerful tool for targeted gene editing and transcriptional programming. We designed a series of chemical inducible systems by coupling TALEs wit...

journal_title：ACS chemical biology

authors： Zhao C,Zhang Y,Zhao Y,Ying Y,Ai R,Zhang J,Wang Y

更新日期：2018-03-16 00:00:00

abstract：:Nearly one-third of the encoded proteome is comprised of secretory proteins that enable communication between cells and organ systems, playing a ubiquitous role in human health and disease. High-throughput detection of secreted proteins would enhance efforts to identify therapies for secretion-related diseases. Using ...

journal_title：ACS chemical biology

authors： Iannotti MJ,MacArthur R,Jones R,Tao D,Singeç I,Michael S,Inglese J

更新日期：2019-03-15 00:00:00

abstract：:Flavin-containing monooxygenases (FMOs) are emerging as effective players in oxidative drug metabolism. Until recently, the functions of the five human FMO isoforms were mostly linked to their capability of oxygenating molecules containing soft N- and S-nucleophiles. However, the human FMO isoform 5 was recently shown...

journal_title：ACS chemical biology

authors： Fiorentini F,Romero E,Fraaije MW,Faber K,Hall M,Mattevi A

更新日期：2017-09-15 00:00:00

abstract：:Cocaine esterase (CocE) is known as the most efficient natural enzyme for cocaine hydrolysis. The major obstacle to the clinical application of wild-type CocE is the thermoinstability with a half-life of only ∼12 min at 37 °C. The previously designed T172R/G173Q mutant (denoted as enzyme E172-173) with an improved in ...

journal_title：ACS chemical biology

authors： Fang L,Chow KM,Hou S,Xue L,Chen X,Rodgers DW,Zheng F,Zhan CG

更新日期：2014-08-15 00:00:00

abstract：:Available crystal structures of opioid receptors provide a high-resolution picture of ligand binding at the primary ("orthosteric") site, that is, the site targeted by endogenous ligands. Recently, positive allosteric modulators of opioid receptors have also been discovered, but their modes of binding and action remai...

journal_title：ACS chemical biology

authors： Shang Y,Yeatman HR,Provasi D,Alt A,Christopoulos A,Canals M,Filizola M

更新日期：2016-05-20 00:00:00

abstract：:Protein dimerization provides a mechanism for the modulation of cellular signaling events. In α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors, the rapidly desensitizing, activated state has been correlated with a weakly dimeric, glutamate-binding domain conformation. Allosteric modulators can fo...

journal_title：ACS chemical biology

authors： Ptak CP,Hsieh CL,Weiland GA,Oswald RE

更新日期：2014-01-17 00:00:00

abstract：:The arabinosyltransferases responsible for the biosynthesis of the arabinan domains of two abundant heteropolysaccharides of the cell envelope of all mycobacterial species, lipoarabinomannan and arabinogalactan, are validated drug targets. Using a cell envelope preparation from Mycobacterium smegmatis as the enzyme so...

journal_title：ACS chemical biology

authors： Angala SK,McNeil MR,Zou L,Liav A,Zhang J,Lowary TL,Jackson M

更新日期：2016-06-17 00:00:00

abstract：:C-methylation of aromatic small molecules by C-methyltransferases (C-MTs) is an important biological transformation that involves C-C bond formation using S-adenosyl-l-methionine (SAM) as the methyl donor. Here, two advances in the mechanistic understanding of C-methylation of the 8-position of coumarin substrates cat...

journal_title：ACS chemical biology

authors： Sadler JC,Chung CH,Mosley JE,Burley GA,Humphreys LD

更新日期：2017-02-17 00:00:00

abstract：:Membrane proteins perform their functions within or on the lipid membrane, and lipid compositions are known to affect membrane protein integration and activity. Recently, the geometric aspect of membrane curvature was shown to play an important role in membrane protein behavior. Certain membrane proteins are known to ...

journal_title：ACS chemical biology

authors： Fujii S,Matsuura T,Yomo T

更新日期：2015-07-17 00:00:00

abstract：:Siderophores are iron-chelating molecules produced by microorganisms and plants to acquire exogenous iron. Siderophore biosynthetic enzymology often produces elaborate and unique molecules through unusual reactions to enable specific recognition by the producing organisms. Herein, we report the structure of two sidero...

journal_title：ACS chemical biology

authors： Vinnik V,Zhang F,Park H,Cook TB,Throckmorton K,Pfleger BF,Bugni TS,Thomas MG

更新日期：2021-01-15 00:00:00

abstract：:The flavo-enzyme DprE1 catalyzes a key epimerization step in the decaprenyl-phosphoryl d-arabinose (DPA) pathway, which is essential for mycobacterial cell wall biogenesis and targeted by several new tuberculosis drug candidates. Here, using differential radiolabeling with DPA precursors and high-resolution fluorescen...

journal_title：ACS chemical biology

authors： Brecik M,Centárová I,Mukherjee R,Kolly GS,Huszár S,Bobovská A,Kilacsková E,Mokošová V,Svetlíková Z,Šarkan M,Neres J,Korduláková J,Cole ST,Mikušová K

更新日期：2015-07-17 00:00:00

abstract：:Integrins play myriad and vital roles in development and disease. They connect a cell with its surroundings and transmit chemical and mechanical signals across the plasma membrane to the cell's interior. Dissecting their roles in cell behavior is complicated by their overlapping ligand specificity and shared downstrea...

journal_title：ACS chemical biology

authors： Klim JR,Fowler AJ,Courtney AH,Wrighton PJ,Sheridan RT,Wong ML,Kiessling LL

更新日期：2012-03-16 00:00:00

abstract：:Although protein kinase inhibitors present excellent pharmaceutical opportunities, lack of selectivity and associated therapeutic side effects are common. Bisubstrate-based inhibitors targeting both the high-selectivity peptide substrate binding groove and the high-affinity ATP pocket address this. However, they are t...

journal_title：ACS chemical biology

authors： van Wandelen LT,van Ameijde J,Ismail-Ali AF,van Ufford HC,Vijftigschild LA,Beekman JM,Martin NI,Ruijtenbeek R,Liskamp RM

更新日期：2013-07-19 00:00:00

abstract：:Creation of an artificial oscillating gene expression system is one of the most challenging issues in synthetic biology. Here, we constructed a simple system to manipulate gene expression patterns to be circadian, reflecting the intrinsic cellular clock, by fusing a core clock protein, BMAL1 or CLOCK, with a zinc fing...

journal_title：ACS chemical biology

authors： Imanishi M,Yamamoto K,Yamada H,Hirose Y,Okamura H,Futaki S

更新日期：2012-11-16 00:00:00

abstract：:Large-scale quantification of protein O-linked β- N-acetylglucosamine (O-GlcNAc) modification in a site-specific manner remains a key challenge in studying O-GlcNAc biology. Herein, we developed an isotope-tagged cleavable linker (isoTCL) strategy, which enabled isotopic labeling of O-GlcNAc through bioorthogonal conj...

journal_title：ACS chemical biology

authors： Qin K,Zhu Y,Qin W,Gao J,Shao X,Wang YL,Zhou W,Wang C,Chen X

更新日期：2018-08-17 00:00:00

abstract：:Various potential G-quadruplex forming sequences present in the genome offer a platform to modulate their function by means of stabilizing molecules. Though G-quadruplex structures exhibit diverse structural topologies, the presence of G-quartets as a common structural element makes the design of topology specific lig...

journal_title：ACS chemical biology

authors： Dhamodharan V,Harikrishna S,Bhasikuttan AC,Pradeepkumar PI

更新日期：2015-03-20 00:00:00

abstract：:Zinc plays both physiological and pathological roles in biology, making it of increasing interest. To date, intracellular free zinc has been measured in cell types supplemented with or enriched in zinc, such as hippocampal neurons. Here we quantitatively image intracellular exchangeable zinc in an ordinary resting cel...

journal_title：ACS chemical biology

authors： Bozym RA,Thompson RB,Stoddard AK,Fierke CA

更新日期：2006-03-17 00:00:00

abstract：:Originally discovered as part of an adaptive bacterial defense system against the invasion of foreign phages, programmable CRISPR-Cas nucleases have emerged as remarkable enzymes with transformative potential for both biological research and clinical application. CRISPR-Cas nucleases likely evolved in their natural co...

journal_title：ACS chemical biology

authors： Tsai SQ

更新日期：2018-02-16 00:00:00

abstract：:Ca(II) ions are critical for the proper function of neurons by contributing to synaptic signaling and regulating neuronal plasticity. Dysregulation of Ca(II) is associated with a number of pathologies that cause neurodegeneration; therefore the ability to monitor Ca(II) intracellularly is an important target for molec...

journal_title：ACS chemical biology

authors： Adams CJ,Krueger R,Meade TJ

更新日期：2020-02-21 00:00:00

abstract：:Tumor heterogeneity has hampered the development of novel effective therapeutic options for aggressive cancers, including the deadly primary adult brain tumor glioblastoma (GBM). Intratumoral heterogeneity is partially attributed to the tumor initiating cell (TIC) subset that contains highly tumorigenic, stem-like cel...

journal_title：ACS chemical biology

authors： Libby CJ,Zhang S,Benavides GA,Scott SE,Li Y,Redmann M,Tran AN,Otamias A,Darley-Usmar V,Napierala M,Zhang J,Augelli-Szafran CE,Zhang W,Hjelmeland AB

更新日期：2018-08-17 00:00:00

abstract：:Angucyclines are a structurally diverse class of actinobacterial natural products defined by their varied polycyclic ring systems, which display a wide range of biological activities. We recently discovered lugdunomycin (1), a highly rearranged polyketide antibiotic derived from the angucycline backbone that is synthe...

journal_title：ACS chemical biology

authors： Xiao X,Elsayed SS,Wu C,van der Heul HU,Metsä-Ketelä M,Du C,Prota AE,Chen CC,Liu W,Guo RT,Abrahams JP,van Wezel GP

更新日期：2020-09-18 00:00:00

abstract：:The anxiolytic, anticonvulsant, muscle-relaxant, and sedative-hypnotic effects of benzodiazepine site ligands are mainly elicited by allosteric modulation of GABAA receptors via their extracellular αx+/γ2- ( x = 1, 2, 3, 5) interfaces. In addition, a low affinity binding site at the homologous α+/β- interfaces was rep...

journal_title：ACS chemical biology

authors： Siebert DCB,Bampali K,Puthenkalam R,Varagic Z,Sarto-Jackson I,Scholze P,Sieghart W,Mihovilovic MD,Schnürch M,Ernst M

更新日期：2018-08-17 00:00:00

abstract：:Reactive oxygen species (ROS) play an important role in the onset of Parkinson's disease (PD), and deciphering protective mechanisms is a major goal for therapeutic development. Here, DJ-1 (PARK7) gained major attention when a conserved cysteine residue with a putative role in oxidative stress sensing/protection was l...

journal_title：ACS chemical biology

authors： Drechsel J,Mandl FA,Sieber SA

更新日期：2018-08-17 00:00:00

abstract：:Sugar aminotransferases (SATs) are an important class of tailoring enzymes that catalyze the 5'-pyridoxal phosphate (PLP)-dependent stereo- and regiospecific installation of an amino group from an amino acid donor (typically L-Glu or L-Gln) to a corresponding ketosugar nucleotide acceptor. Herein we report the strateg...

journal_title：ACS chemical biology

authors： Wang F,Singh S,Xu W,Helmich KE,Miller MD,Cao H,Bingman CA,Thorson JS,Phillips GN Jr

更新日期：2015-09-18 00:00:00

abstract：:Reporter gene assays (RGAs) are commonly used to measure biological pathway modulation by small molecules. Understanding how such compounds interact with the reporter enzyme is critical to accurately interpret RGA results. To improve our understanding of reporter enzymes and to develop optimal RGA systems, we investig...

journal_title：ACS chemical biology

authors： Ho PI,Yue K,Pandey P,Breault L,Harbinski F,McBride AJ,Webb B,Narahari J,Karassina N,Wood KV,Hill A,Auld DS

更新日期：2013-05-17 00:00:00

abstract：:Understanding the complex biochemical mechanisms that underlie the regulation, toxicity, and protein binding of metal ions requires the ability to analyze the metal content of individual proteins in complex mixtures. In this issue of ACS Chemical Biology, a technique combining gel electrophoresis with synchrotron X-ra...

journal_title：ACS chemical biology

authors： Zahler NH

更新日期：2010-06-18 00:00:00