Abstract：
:Whereas the C. elegans genome was sequenced many years ago, the role of small molecule signals in its biology is still poorly understood. A recent publication reports the identification of two steroidal signaling molecules that regulate C. elegans reproductive development and dauer diapause via the nuclear receptor DAF-12. The two compounds, named dafachronic acids, represent the first endogenous ligands identified for any of the 284 nuclear receptors in C. elegans.
journal_name
ACS Chem Bioljournal_title
ACS chemical biologyauthors
Schroeder FCdoi
10.1021/cb600173tsubject
Has Abstractpub_date
2006-05-23 00:00:00pages
198-200issue
4eissn
1554-8929issn
1554-8937journal_volume
1pub_type
杂志文章,评审abstract：:Regulators of G protein signaling (RGS) proteins are key players in regulating signaling via G protein-coupled receptors. RGS proteins directly bind to the Gα-subunits of activated heterotrimeric G-proteins, and accelerate the rate of GTP hydrolysis, thereby rapidly deactivating G-proteins. Using atomistic simulations...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/cb400568g
更新日期：2013-12-20 00:00:00
abstract：:Ubiquitin specific protease 7 (USP7) regulates the protein stability of key cellular regulators in pathways ranging from apoptosis to neuronal development, making it a promising therapeutic target. Here we used an engineered, activated variant of the USP7 catalytic domain to perform structure-activity studies of elect...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.0c00031
更新日期：2020-06-19 00:00:00
abstract：:Platinum-based drugs have been used to successfully treat diverse cancers for several decades. Cisplatin, the original compound of this class, cross-links DNA, resulting in cell cycle arrest and cell death via apoptosis. Cisplatin is effective against several tumor types, yet it exhibits toxic side effects and tumors ...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/cb300320d
更新日期：2012-11-16 00:00:00
abstract：:Miniproteins have a size between that of larger biologics and small molecules and presumably possess the advantages of both; they represent an expanding class of promising scaffolds for the design of affinity reagents, enzymes, and therapeutics. Conventional strategies to promote cellular uptake of miniproteins rely o...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.8b00564
更新日期：2018-11-16 00:00:00
abstract：:Regorafenib (Stivarga) is an oral small molecule kinase inhibitor used to treat metastatic colorectal cancer, hepatocellular carcinomas, and gastrointestinal stromal tumors. Diarrhea is one of the most frequently observed adverse reactions associated with regorafenib. This toxicity may arise from the reactivation of t...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.9b00663
更新日期：2019-12-20 00:00:00
abstract：:The quest for ever more selective kinase inhibitors as potential future drugs has yielded a large repertoire of chemical probes that are selective for specific kinase conformations. These probes have been useful tools to obtain structural snapshots of kinase conformational plasticity. Similarly, kinetic and thermodyna...
journal_title：ACS chemical biology
pub_type： 杂志文章,评审
doi：10.1021/cb500870a
更新日期：2015-01-16 00:00:00
abstract：:The ubiquity of microorganisms is unparalleled in any other known organism. These creatures surround our outsides and colonize our insides, a fact that has been known for centuries. However, despite their prevalence and long study, many of their characteristics still remain largely unexplained, including how proteins ...
journal_title：ACS chemical biology
pub_type： 传,历史文章,杂志文章
doi：10.1021/cb100179t
更新日期：2010-07-16 00:00:00
abstract：:Detection of metabolites and post-translational modifications can be achieved using the azide as a bioorthogonal chemical reporter. Once introduced into target biomolecules, either metabolically or through chemical modification, the azide can be tagged with probes using one of three highly selective reactions: the Sta...
journal_title：ACS chemical biology
pub_type： 信件
doi：10.1021/cb6003228
更新日期：2006-11-21 00:00:00
abstract：:The neurotoxin saxitoxin and related paralytic shellfish toxins are produced by multiple species of cyanobacteria and dinoflagellates. This study investigates the two saxitoxin-producing strains of Scytonema crispum, CAWBG524 and CAWBG72, isolated in New Zealand. Each strain was previously reported to have a distinct ...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.8b00608
更新日期：2018-11-16 00:00:00
abstract：:Nephronectin is an extracellular matrix protein that interacts with the α8β1 integrin receptor and plays a role in tissue and organ development, though the motifs that mediate adhesion to the receptor remain unclear. This paper describes the use of self-assembled monolayers to study the adhesion of α8β1-presenting cel...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/cb200186j
更新日期：2011-10-21 00:00:00
abstract：:Hemolysis, a process by which the destruction of red blood cells leads to the release of hemoglobin, is a critical event observed during hemolytic disorders. Under oxidative stress conditions, hemoglobin can release its heme prosthetic group, which is highly cytotoxic and can catalyze the generation of reactive oxygen...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.8b00458
更新日期：2018-08-17 00:00:00
abstract：:Recent advances in understanding the relevance of noncoding RNA (ncRNA) to disease have increased interest in drugging ncRNA with small molecules. The recent discovery of ribocil, a structurally distinct synthetic mimic of the natural ligand of the flavin mononucleotide (FMN) riboswitch, has revealed the potential che...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.7b01013
更新日期：2018-03-16 00:00:00
abstract：:The endoplasmic reticulum (ER) is the initial site of biogenesis of secretory pathway proteins, including proteins localized to the ER, Golgi, lysosomes, intracellular vesicles, plasma membrane, and extracellular compartments. Proteins within the secretory pathway contain a high abundance of disulfide bonds to protect...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.9b01014
更新日期：2020-02-21 00:00:00
abstract：:There is a current and pressing need for improved cancer therapies. The use of small molecule kinase inhibitors and their application in combinatorial regimens represent an approach to personalized targeted cancer therapy. A number of AGC kinases, including atypical Protein Kinase C enzymes (PKCs), are validated drug ...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.6b00827
更新日期：2017-02-17 00:00:00
abstract：:Next-generation DNA sequencing technologies have led to a massive accumulation of genomic and transcriptomic data from patients and healthy individuals. The major challenge ahead is to understand the functional significance of the elements of the human genome and transcriptome, and implications for diagnosis and treat...
journal_title：ACS chemical biology
pub_type： 杂志文章,评审
doi：10.1021/acschembio.7b00657
更新日期：2018-02-16 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：:Bacterial tRNA-guanine transglycosylase (Tgt) is involved in the biosynthesis of the modified tRNA nucleoside queuosine present in the anticodon wobble position of tRNAs specific for aspartate, asparagine, histidine, and tyrosine. Inactivation of the tgt gene leads to decreased pathogenicity of Shigella bacteria. Ther...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.0c00700
更新日期：2020-11-20 00:00:00
abstract：:The LpxC enzyme in the lipid A biosynthetic pathway is one of the most promising and clinically unexploited antibiotic targets for treatment of multidrug-resistant Gram-negative infections. Progress in medicinal chemistry has led to the discovery of potent LpxC inhibitors with a variety of chemical scaffolds and disti...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/cb400067g
更新日期：2014-01-17 00:00:00
abstract：:WS9326A and annimycin are produced by Streptomyces asterosporus DSM 41452. WS9326A is a nonribosomal peptide synthetase-(NRPS-) derived depsipeptide containing a cinnamoyl moiety, while annimycin is a linear polyketide bearing a 2-amino-3-hydroxycyclopent-2-enone (C5N) group. Both gene clusters have been sequenced and...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.9b00351
更新日期：2019-08-16 00:00:00
abstract：:Endocytosis is a key process in cellular delivery of macromolecules by molecular transporters, although the mechanism of internalization remains unclear. Here, we probe the cellular uptake of streptavidin using biotinylated guanidinoneomycin (biotinGNeo), a low molecular weight guanidinium-rich molecular transporter. ...
journal_title：ACS chemical biology
pub_type： 信件
doi：10.1021/cb400172h
更新日期：2013-07-19 00:00:00
abstract：:Rediscovery of known compounds and time consumed in identification, especially high molecular weight compounds with complex structure, have let down interest in drug discovery. In this study, whole-genome analysis of microbe and Global Natural Products Social (GNPS) molecular networking helped in initial understanding...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.0c00026
更新日期：2020-03-20 00:00:00
abstract：:Epigenetic regulation is directed, in part, by the correlated placement of histone post-translational modifications, but the mechanisms controlling correlated modifications are incompletely understood. Correlations arise from crosstalk among modifications and are frequently attributed to protein-protein interactions t...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/cb5004527
更新日期：2015-01-16 00:00:00
abstract：:The nematode Caenorhabditis elegans is an excellent model organism for studies of glycan dynamics, a goal that requires tools for imaging glycans in vivo. Here we applied the bioorthogonal chemical reporter technique for the molecular imaging of mucin-type O-glycans in live C. elegans. We treated worms with azidosugar...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/cb900254y
更新日期：2009-12-18 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：:We report progress toward a general strategy for mimicking the recognition properties of specific α-helices within natural proteins through the use of oligomers that are less susceptible than conventional peptides to proteolysis. The oligomers contain both α- and β-amino acid residues, with the density of the β subuni...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.5b00109
更新日期：2015-07-17 00:00:00
abstract：:Bacteria harbor an immense reservoir of potentially new and therapeutic small molecules in the form of "silent" biosynthetic gene clusters (BGCs). These BGCs can be identified bioinformatically but are sparingly expressed under normal laboratory growth conditions, or not at all, and therefore do not produce significan...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.9b00049
更新日期：2019-04-19 00:00:00
abstract：:A biophysical understanding of the mechanistic, chemical, and physical origins underlying antibiotic action and resistance is vital to the discovery of novel therapeutics and the development of strategies to combat the growing emergence of antibiotic resistance. The site-specific introduction of stable-isotope labels ...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.9b01054
更新日期：2020-05-15 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：:New machine learning methods to analyze raw chemical and biological data are now widely accessible as open-source toolkits. This positions researchers to leverage powerful, predictive models in their own domains. We caution, however, that the application of machine learning to experimental research merits careful cons...
journal_title：ACS chemical biology
pub_type： 杂志文章
doi：10.1021/acschembio.8b00881
更新日期：2018-10-19 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
