Abstract:
:Polyalkoxybenzenes are plant components displaying a wide range of biological activities. In these studies, we synthesized apiol and dillapiol isoxazoline analogues of combretastatins and evaluated their effect on sea urchin embryos. We have shown that p-methoxyphenyl isoxazoline caused sea urchin embryo immobilization due to the selective excision of motile cilia, whereas long immotile sensory cilia of apical tuft remained intact. This effect was completely reversed by washing the embryos. The compound did not alter cell division, blastulae hatching, and larval morphogenesis. In our hands, the molecule would serve as a convenient tool for in vivo studying morphogenetic processes in the sea urchin embryo. We anticipate that both the assay and the described derivative could be used for studies in ciliary function in embryogenesis.
journal_name
ACS Chem Bioljournal_title
ACS chemical biologyauthors
Semenova MN,Tsyganov DV,Yakubov AP,Kiselyov AS,Semenov VVdoi
10.1021/cb700163qsubject
Has Abstractpub_date
2008-02-15 00:00:00pages
95-100issue
2eissn
1554-8929issn
1554-8937journal_volume
3pub_type
信件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::Ubc13 is an E2 ubiquitin conjugating enzyme that functions in nuclear DNA damage signaling and cytoplasmic NF-κB signaling. Here, we present the structures of complexes of Ubc13 with two inhibitors, NSC697923 and BAY 11-7082, which inhibit DNA damage and NF-κB signaling in human cells. NSC697923 and BAY 11-7082 both i...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.5b00222
更新日期:2015-07-17 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::Allosteric inhibitors can be more difficult to optimize without an understanding of how their binding influences the conformational motions of the target. Here, we used an integrated computational and experimental approach to probe the molecular mechanism of an allosteric inhibitor of heat shock protein 70 (Hsp70). Th...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.8b00712
更新日期:2018-11-16 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::Many oncogenic mutants of the tumor suppressor p53 are conformationally unstable, including the frequently occurring Y220C mutant. We have previously developed several small-molecule stabilizers of this mutant. One of these molecules, PhiKan083, 1-(9-ethyl-9H-carbazole-3-yl)-N-methylmethanamine, binds to a mutation-in...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.6b00315
更新日期:2016-08-19 00:00:00
abstract::Extracellular expression of heat shock protein 90 (eHsp90) by tumor cells is correlated with malignancy. Development of small molecule probes that can detect eHsp90 in vivo may therefore have utility in the early detection of malignancy. We synthesized a cell impermeable far-red fluorophore-tagged Hsp90 inhibitor to t...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.7b00006
更新日期:2017-04-21 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::Glycosylphosphatidylinositol (GPI)-anchored proteins are abundant in the protozoan parasite Trypanosoma brucei, the causative agent of African sleeping sickness in humans and the related disease Nagana in cattle, and disruption of GPI biosynthesis is genetically and chemically validated as a drug target. Here, we exam...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb800143w
更新日期:2008-10-17 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
pub_type: 杂志文章
doi:10.1021/acschembio.9b00001
更新日期:2019-03-15 00:00:00
abstract::Designed second mitochondrial activator of caspases (Smac) mimetics based on an accessible [7,5]-bicyclic scaffold bind to and antagonize protein interactions involving the inhibitor of apoptosis (IAP) proteins, X-chromosome-linked IAP (XIAP), melanoma IAP (ML-IAP), and c-IAPs 1 and 2 (cIAP1 and cIAP2). The design rat...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb600276q
更新日期:2006-09-19 00:00:00
abstract::Histo-blood group epitopes are fucosylated branched oligosaccharides with well-defined conformations in solution that are recognized by receptors, such as lectins from pathogens. We report here the results of a series of experimental and computational endeavors revealing the unusual distortion of histo-blood group ant...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.6b00333
更新日期:2016-07-15 00:00:00
abstract::The innate immune system provides the first line of defense against pathogens through the recognition of nonspecific patterns in RNA to protect the cell in a generalized way. The human RNA-activated protein kinase, PKR, is a dsRNA binding protein and an essential sensor in the innate immune response, which recognizes ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.6b00081
更新日期:2016-04-15 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
pub_type: 杂志文章
doi:10.1021/acschembio.7b00606
更新日期:2018-03-16 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::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::RNA modifications play important roles in RNA structures and regulation of gene expression and translation. We report the first RNA modification on the phosphate, the RNA phosphorothioate (PS) modification, discovered in both prokaryotes and eukaryotes. The PS modification is also first reported on nucleic acids of eu...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00163
更新日期:2020-06-19 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::Activation by glycosaminoglycans (GAGs) is an emerging trend among extracellular proteases important in disease. ProMMP-7, the zymogen of a matrix metalloproteinase secreted by mucosal epithelial and tumor cells, is activated at their surfaces by sulfated GAGs, but how? ProMMP-7 is activated in trans by representative...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb400898t
更新日期:2014-04-18 00:00:00
abstract::Terpene synthases (TS) are classified into two broad types, Class I and II, based on the chemical strategy for initial carbocation formation and motif sequences of the catalytic site. We have recently identified a new class of enzymes, Class IB, showing the acceptability of long (C20-C35) prenyl-diphosphates as substr...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00145
更新日期:2020-06-19 00:00:00
abstract::The ever-growing drug resistance problem worldwide highlights the urgency to discover and develop new drugs. Microbial natural products are a prolific source of drugs. Genome sequencing has revealed a tremendous amount of uncharacterized natural product biosynthetic gene clusters (BGCs) encoded within microbial genome...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.0c00581
更新日期:2020-09-18 00:00:00
abstract::Dysregulated activity of the protease matriptase is a key contributor to aggressive tumor growth, cancer metastasis, and osteoarthritis. Methods for the detection and quantification of matriptase activity and inhibition would be useful tools. To address this need, we developed a matriptase-sensitive protein biosensor ...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.7b00715
更新日期:2018-01-19 00:00:00
abstract::Histone post-translational modifications (PTMs) are crucial for many cellular processes including mitosis, transcription, and DNA repair. The cellular readout of histone PTMs is dependent on both the chemical modification and histone site, and the array of histone PTMs on chromatin is dynamic throughout the eukaryotic...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.9b00651
更新日期:2020-01-17 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::The limited clinical success of therapeutics targeting cellular signaling processes is due to multiple factors, including off-target effects and complex feedback regulation encoded within the signaling network. To understand these effects, chemical proteomics and chemical genetics tools have been developed to map the ...
journal_title:ACS chemical biology
pub_type: 杂志文章,评审
doi:10.1021/cb1002834
更新日期:2011-01-21 00:00:00
abstract::The use of nitric oxide (NO) as a signal for biofilm dispersal has been shown to increase the susceptibility of many biofilms to antibiotics, promoting their eradication. The delivery of NO to biofilms can be achieved by using NO donors with different kinetics and properties of NO release that can influence their effi...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/acschembio.7b00256
更新日期:2017-08-18 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::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::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
pub_type: 杂志文章
doi:10.1021/acschembio.0c00809
更新日期:2021-01-15 00:00:00
abstract::Caenorhabditis elegans lives in compost and decaying fruit, eats bacteria and is exposed to pathogenic microbes. We show that C. elegans is able to modify diverse microbial small-molecule toxins via both O- and N-glucosylation as well as unusual 3'-O-phosphorylation of the resulting glucosides. The resulting glucosyla...
journal_title:ACS chemical biology
pub_type: 杂志文章
doi:10.1021/cb300520u
更新日期:2013-02-15 00:00:00