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::The mitochondrial ADP/ATP carrier (AAC) is a prominent actor in the energetic regulation of the cell, importing ADP into the mitochondria and exporting ATP toward the cytoplasm. Severe genetic diseases have been ascribed to specific mutations in this membrane protein. How minute, well-localized modifications of the tr...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb300012j
更新日期:2012-07-20 00:00:00
abstract::A complication of diabetes is the inability of wounds to heal in diabetic patients. Diabetic wounds are refractory to healing due to the involvement of activated matrix metalloproteinases (MMPs), which remodel the tissue resulting in apoptosis. There are no readily available methods that identify active unregulated MM...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb4005468
更新日期:2014-01-17 00:00:00
abstract::Binding of the Fc domain of Immunoglobulin G (IgG) to Fcγ receptors on leukocytes can initiate a series of signaling events resulting in antibody-dependent cell-mediated cytotoxicity (ADCC) and other important immune responses. Fc domains lacking glycosylation at N297 have greatly diminished Fcγ receptor binding and l...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb300130k
更新日期:2012-09-21 00:00:00
abstract::Enzymatic plasticity, as a modern term referring to the functional conversion of an enzyme, is significant for enzymatic activity redesign. The bacterial diterpene cyclase CotB2 is a typical plastic enzyme by which its native form precisely conducts a chemical reaction while its mutants diversify the catalytic functio...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00645
更新日期:2020-10-16 00:00:00
abstract::We have developed a chemically controlled very long-acting delivery system to support once-monthly administration of a peptidic GLP-1R agonist. Initially, the prototypical GLP-1R agonist exenatide was covalently attached to hydrogel microspheres by a self-cleaving β-eliminative linker; after subcutaneous injection in ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.7b00218
更新日期:2017-08-18 00:00:00
abstract::Antivirulence strategies addressing bacterial pathogenicity without exhibiting growth inhibition effects represent a novel approach to overcome today's crisis in antibiotic development. In recent studies, we examined various inhibitors of PqsD, an enzyme involved in formation of Pseudomonas aeruginosa cell-to-cell sig...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb400530d
更新日期:2013-12-20 00:00:00
abstract::Recent studies have shown that cholesterol plays a significant role in the ability of Toxin A from Clostridium difficile to enter eukaryotic cells. The translocation process is one of three major steps during intoxication that could be targeted for intervention against the severe antibiotic-associated diarrhea caused ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb600133b
更新日期:2006-04-25 00:00:00
abstract::The complexity of the human proteome is greatly expanded by post-translational modifications. New tools capable of recognizing these modifications in a sequence-specific fashion provide a route to purify these modified proteins, to alter protein trafficking, and to visualize signal transduction in real time. Here, we ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb800069c
更新日期:2008-08-15 00:00:00
abstract::Polyhalogenated dibenzo-p-dioxins are arguably among the most toxic molecules known to man. In addition to anthropogenic sources, marine invertebrates also harbor polybrominated dibenzo-p-dioxins of as yet unknown biogenic origin. Here, we report that the bmp gene locus in marine bacteria, a recently characterized sou...
journal_title:ACS chemical biology
pub_type: 信件
doi:10.1021/cb5004338
更新日期:2014-09-19 00:00:00
abstract::Signal transducer and activator of transcription (STAT) proteins have important biological functions; however, deregulation of STAT signaling is a driving force behind the onset and progression of inflammatory diseases and cancer. While their biological roles suggest that STAT proteins would be valuable targets for de...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00046
更新日期:2020-07-17 00:00:00
abstract::Agonists and antagonists of the nicotinic acetylcholine receptor (nAChR) are used to treat nicotine addiction, neuromuscular disorders, and neurological diseases. In designing small molecule therapeutics with the nAChR as a target, it is useful to identify chemical parameters that correlate with ability to activate th...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb800189y
更新日期:2008-11-21 00:00:00
abstract::Pyrrole-imidazole alkaloids are natural products isolated from marine sponges, holobiont metazoans that are associated with symbiotic microbiomes. Pyrrole-imidazole alkaloids have attracted attention due to their chemical complexity and their favorable pharmacological properties. However, insights into how these molec...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00375
更新日期:2020-08-21 00:00:00
abstract::Establishing the relative configuration of a bioactive natural product represents the most challenging part in determining its structure. Residual dipolar couplings (RDCs) are sensitive probes of the relative spatial orientation of internuclear vectors. We adapted a force field structure calculation methodology to all...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.7b00281
更新日期:2017-08-18 00:00:00
abstract::The molecular chaperone Hsp90 requires the assistance of immunophilins, co-chaperones, and partner proteins for the conformational maturation of client proteins. Hsp90 inhibition represents a promising anticancer strategy due to the dependence of numerous oncogenic signaling pathways upon Hsp90 function. Historically,...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb400906e
更新日期:2014-04-18 00:00:00
abstract::The anticancer molecule taxol (Paclitaxel) stands as one of the most medically and economically important natural products. However, despite decades of extensive study, its biosynthesis remains poorly understood. Unpredictable behavior of the first oxygenation enzyme, taxadiene-5α-hydroxylase, which produces a range o...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.5b00767
更新日期:2016-02-19 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
pub_type: 杂志文章
doi:10.1021/acschembio.6b00093
更新日期:2016-06-17 00:00:00
abstract::The Pygo-BCL9 complex is a chromatin reader, facilitating β-catenin-mediated oncogenesis, and is thus emerging as a potential therapeutic target for cancer. Its function relies on two ligand-binding surfaces of Pygo's PHD finger that anchor the histone H3 tail methylated at lysine 4 (H3K4me) with assistance from the B...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb500585s
更新日期:2014-12-19 00:00:00
abstract::Widespread use and misuse of antibiotics has allowed for the selection of resistant bacteria capable of avoiding the effects of antibiotics. The primary mechanism for resistance to aminoglycosides, a broad-spectrum class of antibiotics, is through covalent enzymatic modification of the drug, waning their bactericidal ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.5b01070
更新日期:2016-05-20 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::The abundant observation of chemical fragment information for molecular complexities is a major advantage of biological NMR analysis. Thus, the development of a novel technique for NMR signal assignment and metabolite identification may offer new possibilities for exploring molecular complexities. We propose a new sig...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.5b00894
更新日期:2016-04-15 00:00:00
abstract::Generating highly selective probes to interrogate protein kinase function in biological studies remains a challenge, and new strategies are required. Herein, we describe the development of the first highly selective and cell-permeable inhibitor of c-Src, a key signaling kinase in cancer. Our strategy involves extensio...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb300172e
更新日期:2012-08-17 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::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::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
pub_type: 杂志文章
doi:10.1021/acschembio.0c00564
更新日期:2020-09-18 00:00:00
abstract::Combination therapies that enhance efficacy or permit reduced dosages to be administered have seen great success in a variety of therapeutic applications. More fundamentally, the discovery of epistatic pathway interactions not only informs pharmacologic intervention but can be used to better understand the underlying ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb2003225
更新日期:2011-12-16 00:00:00
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_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb600461v
更新日期:2006-12-15 00:00:00
abstract::Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chemical genetic probes of function. Cell-permeable small molecules, however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small molecules targeting RNA. As part of...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb400265y
更新日期:2013-10-18 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::Oligomeric assemblies formed from a variety of disease-associated peptides and proteins have been strongly associated with toxicity in many neurodegenerative conditions, such as Alzheimer's disease. The precise nature of the toxic agents, however, remains still to be established. We show that prefibrillar aggregates o...
journal_title:ACS chemical biology
pub_type: 信件
doi:10.1021/cb1001203
更新日期:2010-08-20 00:00:00
abstract::Drug optimization is guided by biophysical methods with increasing popularity. In the context of lead structure modifications, the introduction of methyl groups is a simple but potentially powerful approach. Hence, it is crucial to systematically investigate the influence of ligand methylation on biophysical character...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.9b00476
更新日期:2019-12-20 00:00:00