Abstract:
:Modern visualization techniques are affording a peek into complex cellular processes. A recent paper describes an automated fluorescence microscopy method to map the subcellular localization of up to 100 different proteins in the same sample.
journal_name
ACS Chem Bioljournal_title
ACS chemical biologyauthors
Jacquier V,Michnick SWdoi
10.1021/cb600461vsubject
Has Abstractpub_date
2006-12-15 00:00:00pages
744-6issue
12eissn
1554-8929issn
1554-8937journal_volume
1pub_type
杂志文章abstract::Bacterial resistance to conventional antibiotics is of major concern. Antimicrobial peptides (AMPs) are considered excellent alternatives. Among them, D-cateslytin (D-Ctl, derivative of a host defense peptide) has shown high efficiency against a broad spectrum of bacteria. The first target of AMPs is the outer membran...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00622
更新日期:2020-10-16 00:00:00
abstract::Kinetic parameters of protein-ligand interactions are progressively acknowledged as valuable information for rational drug discovery. However, a targeted optimization of binding kinetics is not easy to achieve, and further systematic studies are necessary to increase the understanding about molecular mechanisms involv...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.6b00979
更新日期:2017-01-20 00:00:00
abstract::Mutations that constitutively activate the phosphatidyl-inositol-3-kinase (PI3K) signaling pathway, including alterations in PI3K, PTEN, and AKT, are found in a variety of human cancers, implicating the PI3K lipid kinase as an attractive target for the development of therapeutic agents to treat cancer and other relate...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb800039y
更新日期:2008-05-16 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
pub_type: 杂志文章
doi:10.1021/cb300432s
更新日期:2012-11-16 00:00:00
abstract::We report here an isatin derivative 45 (ID45) against coxsackievirus B3 (CVB3) replication, which was synthesized based on a high-throughput screen of a unique natural product library. ID45 showed the most potent anti-CVB3 activity among the four synthesized compounds. Treatment of cells with ID45 before or after infe...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb400775z
更新日期:2014-04-18 00:00:00
abstract::The expansion of the genetic code with noncanonical amino acids (ncAA) enables the function of proteins to be tailored with high molecular precision. In this approach, the ncAA is charged to an orthogonal nonsense suppressor tRNA by an aminoacyl-tRNA-synthetase (aaRS) and incorporated into the target protein in vivo b...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb5006273
更新日期:2014-12-19 00:00:00
abstract::The ATP site of kinases displays remarkable conformational flexibility when accommodating chemically diverse small molecule inhibitors. The so-called activation segment, whose conformation controls catalytic activity and access to the substrate binding pocket, can undergo a large conformational change with the active ...
journal_title:ACS chemical biology
pub_type: 杂志文章,评审
doi:10.1021/cb500129t
更新日期:2014-06-20 00:00:00
abstract::Methicillin resistance in Staphylococcus aureus depends on the production of mecA, which encodes penicillin-binding protein 2A (PBP2A), an acquired peptidoglycan transpeptidase (TP) with reduced susceptibility to β-lactam antibiotics. PBP2A cross-links nascent peptidoglycan when the native TPs are inhibited by β-lacta...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb100269f
更新日期:2011-01-21 00:00:00
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
pub_type: 杂志文章
doi:10.1021/acschembio.9b00895
更新日期:2020-03-20 00:00:00
abstract::The Akt kinase family, consisting of three isoforms in humans, is a well-validated class of drug target. Through various screening campaigns in academics and pharmaceutical industries, several promising inhibitors have been developed to date. However, due to the mechanistic and structural similarities of Akt kinases, ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb200388k
更新日期:2012-03-16 00:00:00
abstract::In type-2 diabetes (T2D), islet amyloid polypeptide (IAPP) self-associates into toxic assemblies causing islet β-cell death. Therefore, preventing IAPP toxicity is a promising therapeutic strategy for T2D. The molecular tweezer CLR01 is a supramolecular tool for selective complexation of K residues in (poly)peptides. ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.5b00146
更新日期:2015-06-19 00:00:00
abstract::Despite being extensively characterized structurally and biochemically, the functional role of histone deacetylase 8 (HDAC8) has remained largely obscure due in part to a lack of known cellular substrates. Herein, we describe an unbiased approach using chemical tools in conjunction with sophisticated proteomics method...
journal_title:ACS chemical biology
pub_type: 信件
doi:10.1021/cb500492r
更新日期:2014-10-17 00:00:00
abstract::RUVBL1 and RUVBL2 are ATPases associated with diverse cellular activities (AAAs) that form a complex involved in a variety of cellular processes, including chromatin remodeling and regulation of gene expression. RUVBLs have a strong link to oncogenesis, where overexpression is correlated with tumor growth and poor pro...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.8b00904
更新日期:2019-02-15 00:00:00
abstract::The genetic integrity of each organism depends on the faithful segregation of its genome during mitosis. To meet this challenge, a cellular surveillance mechanism, termed the spindle assembly checkpoint (SAC), evolved that monitors the correct attachment of chromosomes and blocks progression through mitosis if correct...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.5b00121
更新日期:2015-07-17 00:00:00
abstract::Elevation of reactive oxygen species (ROS) levels has been observed in many cancer cells relative to nontransformed cells, and recent reports have suggested that small-molecule enhancers of ROS may selectively kill cancer cells in various in vitro and in vivo models. We used a high-throughput screening approach to ide...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb300653v
更新日期:2013-05-17 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
pub_type: 杂志文章
doi:10.1021/acschembio.5b00237
更新日期:2015-07-17 00:00:00
abstract::Hydrogen sulfide (H2S) is an endogenously produced gas that is toxic at high concentrations. It is eliminated by a dedicated mitochondrial sulfide oxidation pathway, which connects to the electron transfer chain at the level of complex III. Direct reduction of cytochrome c (Cyt C) by H2S has been reported previously b...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.8b00463
更新日期:2018-08-17 00:00:00
abstract::Bacteria use small molecules to assess the density and identity of nearby organisms and formulate a response. This process, called quorum sensing (QS), commonly regulates bioluminescence, biofilm formation, and virulence. Vibrio harveyi have three described QS circuits. Each involves the synthesis of a molecule that r...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb300215t
更新日期:2012-08-17 00:00:00
abstract::BRD4, a member of the bromodomain and extraterminal domain (BET) family, has emerged as a promising epigenetic target in cancer and inflammatory disorders. All reported BET family ligands bind within the bromodomain acetyl-lysine binding sites and competitively inhibit BET protein interaction with acetylated chromatin...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00058
更新日期:2020-04-17 00:00:00
abstract::The ubiquitin proteasome system is widely postulated to be a new and important field of drug discovery for the future, with the ubiquitin specific proteases (USPs) representing one of the more attractive target classes within the area. Many USPs have been linked to critical axes for therapeutic intervention, and the f...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.7b00334
更新日期:2017-12-15 00:00:00
abstract::Unrelated ligands, often found in drug discovery campaigns, can bind to the same receptor, even with the same protein residues. To investigate how this might occur, and whether it might be typically possible to find unrelated ligands for the same drug target, we sought examples of topologically unrelated ligands that ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.8b00443
更新日期:2018-09-21 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
pub_type: 评论,杂志文章
doi:10.1021/cb100145z
更新日期:2010-06-18 00:00:00
abstract::The oxidative addition of nitric oxide (NO) to a thiol, S-nitrosation, is a focus of studies on cyclic guanosine monophosphate (cGMP)-independent NO signaling. S-Nitrosation of the catalytic cysteine of the caspase proteases has important effects on apoptosis and consequently has received attention. Here we report on ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb600393x
更新日期:2006-11-21 00:00:00
abstract::Our immune system constantly samples peptides found inside the body as a means to detect foreign pathogens, infected cells, and tumorous cells. T cells, which carry out the critical task of distinguishing self from nonself peptides, can only survey peptides that are presented by the major histocompatibility complex pr...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb400594q
更新日期:2013-11-15 00:00:00
abstract::The emergence of multidrug-resistant Staphylococcus aureus strains has become a serious clinical problem. Iron is absolutely required for the bacterial growth, virulence associated with colonization, and survival from the host immune system. The FeoB protein is a major iron permease in bacterial ferrous iron transport...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00842
更新日期:2021-01-15 00:00:00
abstract::N-Acetylneuraminic acid lyase (NAL) is a Class I aldolase that catalyzes the reversible condensation of pyruvate with N-acetyl-d-mannosamine (ManNAc) to yield the sialic acid N-acetylneuraminic acid (Neu5Ac). Aldolases are finding increasing use as biocatalysts for the stereospecific synthesis of complex molecules. In...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb500067z
更新日期:2014-04-18 00:00:00
abstract::Chloropupukeananin and chloropestolides are novel metabolites of the plant endophyte Pestalotiopsis fici, showing antimicrobial, antitumor, and anti-HIV activities. Their highly complex and unique skeletons were generated from the coisolated pestheic acid (1) and iso-A82775C (10) based on our previous studies. Here, w...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.7b01059
更新日期:2018-03-16 00:00:00
abstract::Fatty acylation or lipid modification of proteins controls their cellular activation and diverse roles in physiology. It mediates protein-protein and protein-membrane interactions and plays an important role in regulating cellular signaling pathways. Currently, there is need for visualizing lipid modifications of prot...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb900085z
更新日期:2009-07-17 00:00:00
abstract::A strategy has been established for the synthesis of a family of bifunctional HIV-1 inhibitor covalent conjugates with the potential to bind simultaneously to both the gp120 and gp41 subunits of the HIV-1 envelope glycoprotein trimeric complex (Env). One component of the conjugates is derived from BNM-III-170, a small...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00888
更新日期:2021-01-15 00:00:00
abstract::The cell utilizes the Keap1/Nrf2-ARE signaling pathway to detoxify harmful chemicals in order to protect itself from oxidative stress and to maintain its reducing environment. When exposed to oxidative stress and xenobiotic inducers, the redox sensitive Keap1 is covalently modified at specific cysteine residues. Conse...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb4000103
更新日期:2013-08-16 00:00:00