Abstract:
:Using light to control cellular processes is one of the attractive areas of research. Here, availability of different, light-responsive caged compounds has played a critical role. In this issue of Cell Chemical Biology, Hövelmann et al. (2016) give us an example of how to design and use caged lipids to guide chemotaxis at the single cell level.
journal_name
Cell Chem Bioljournal_title
Cell chemical biologyauthors
Dore TMdoi
10.1016/j.chembiol.2016.05.003subject
Has Abstractpub_date
2016-05-19 00:00:00pages
531-532issue
5eissn
2451-9456issn
2451-9448pii
S2451-9456(16)30134-9journal_volume
23pub_type
评论,杂志文章abstract::Activation of innate immune signaling in the tumor microenvironment is central to a successful anti-tumor immune response, and it is in large part mediated by cytosolic double-stranded DNA sensing. Here, Carozza et al. (2020b) report potent and selective inhibitors of ENPP1, a negative regulator of innate immune signa...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.11.001
更新日期:2020-11-19 00:00:00
abstract::Reactivation of mutant p53 has emerged as a promising approach for cancer therapy. Recent studies have identified several mutant p53-reactivating compounds that target thiol groups in mutant p53. Here we have investigated the relationship between thiol reactivity, p53 thermostabilization, mutant p53 refolding, mutant ...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.06.013
更新日期:2018-10-18 00:00:00
abstract::Kinase inhibitors are effective cancer therapies. Unfortunately, drug resistance emerges in response to kinase inhibition leading to loss of drug efficacy. In this issue of Cell Chemical Biology, Peh et al. (2018) demonstrate that caspase activators effectively delay onset of resistance to kinase inhibitors and are ex...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2018.08.001
更新日期:2018-08-16 00:00:00
abstract::The Precision Medicine Initiative aims to use advances in basic and clinical research to develop therapeutics that selectively target and kill cancer cells. Under the same doctrine of precision medicine, there is an equally important need to visualize these diseased cells to enable diagnosis, facilitate surgical resec...
journal_title:Cell chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.chembiol.2015.12.003
更新日期:2016-01-21 00:00:00
abstract::Polo-like kinase 1 has hundreds of substrates and multiple functions that operate within the ∼60 min of mitosis. Herein, we describe a chemical-genetic system that allows particular substrates to be "toggled" into or out of chemical control using engineered phosphoacceptor selectivity. Biochemical assays and phosphopr...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.01.007
更新日期:2020-03-19 00:00:00
abstract::Eicosanoids and related oxylipins are critical, small bioactive mediators of human physiology and inflammation. While ∼1,100 distinct species have been predicted to exist, to date, less than 150 of these molecules have been measured in humans, limiting our understanding of their role in human biology. Using a directed...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.11.015
更新日期:2019-03-21 00:00:00
abstract::USP7 is a deubiquitinating enzyme that plays a pivotal role in multiple oncogenic pathways and therefore is a desirable target for new anti-cancer therapies. However, the lack of structural information about the USP7-inhibitor interactions has been a critical gap in the development of potent inhibitors. USP7 is unique...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2017.09.004
更新日期:2017-12-21 00:00:00
abstract::Owing to their structural flexibility, most serpins inhibit the cognate proteases in a fast and specific manner and also are susceptible to pathogenic misfolding. In this issue of Cell Chemical Biology, Madsen et al. (2016) report on the selection and characterization of an RNA aptamer that stabilizes α1-antichymotryp...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2016.06.002
更新日期:2016-06-23 00:00:00
abstract::The spliceosome mediates precursor mRNA splicing in eukaryotes, including the model organism Saccharomyces cerevisiae (yeast). Despite decades of study, no chemical inhibitors of yeast splicing in vivo are available. We have developed a system to efficiently inhibit splicing and block proliferation in living yeast cel...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.11.008
更新日期:2019-03-21 00:00:00
abstract::In this issue of Cell Chemical Biology, Olson et al. (2019) develop the first selective CDK7 irreversible inhibitor. Elegant cell-based studies using a CDK7 mutant that is not covalently engaged by the probe helped decipher the effects of inhibiting the kinase on the cell cycle and gene transcription. ...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2019.05.012
更新日期:2019-06-20 00:00:00
abstract::The cysteine prodrug N-acetyl cysteine (NAC) is widely used as a pharmacological antioxidant and cytoprotectant. It has been reported to lower endogenous oxidant levels and to protect cells against a wide range of pro-oxidative insults. As NAC itself is a poor scavenger of oxidants, the molecular mechanisms behind the...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.01.011
更新日期:2018-04-19 00:00:00
abstract::Numerous near-infrared (NIR) fluorescent proteins (FPs) were recently engineered from bacterial photoreceptors but lack of their systematic comparison makes researcher's choice rather difficult. Here we evaluated side-by-side several modern NIR FPs, such as blue-shifted smURFP and miRFP670, and red-shifted mIFP and mi...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2017.05.018
更新日期:2017-06-22 00:00:00
abstract::Non-ribosomal peptides (NRPs) are biosynthesized on non-ribosomal peptides synthetase (NRPS) complexes, of which a C-terminal releasing domain commonly offloads the products. Interestingly, a dedicated releasing domain is absent in surugamides (SGM) NRPS, which directs the biosynthesis of cyclic octapeptides, SGM-A to...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2019.02.010
更新日期:2019-05-16 00:00:00
abstract::Interfacial inhibitors exert their biological effects through co-association with two macromolecules. The pateamine A (PatA) class of molecules function by stabilizing eukaryotic initiation factor (eIF) 4A RNA helicase onto RNA, resulting in translation initiation inhibition. Here, we present the crystal structure of ...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.12.006
更新日期:2021-01-05 00:00:00
abstract::Ubiquinone (UQ) is a conserved polyprenylated lipid essential to cellular respiration. Two papers, one in this issue of Cell Chemical Biology (Hajj Chehade et al., 2019) and another in Molecular Cell (Lohman et al., 2019), identify lipid-binding proteins that play crucial roles in chaperoning UQ-intermediates. ...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2019.04.005
更新日期:2019-04-18 00:00:00
abstract::Identification and validation of the targets of bioactive small molecules identified in cell-based screening is challenging and often meets with failure, calling for the development of new methodology. We demonstrate that a combination of chemical proteomics with in silico target prediction employing the SPiDER method...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.05.016
更新日期:2018-09-20 00:00:00
abstract::Recent advances in induced pluripotent stem cell technologies and phenotypic screening shape the future of bioactive small-molecule discovery. In this review we analyze the impact of small-molecule phenotypic screens on drug discovery as well as on the investigation of human development and disease biology. We further...
journal_title:Cell chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.chembiol.2019.05.007
更新日期:2019-08-15 00:00:00
abstract::In this issue of Cell Chemical Biology, Shah et al. (2019) report an in vitro, high-throughput assay that predicts the ability of compounds to suppress peroxidation of phospholipids. This approach provides a way to design and optimize targeted antioxidants that suppress specific oxidative event in cells, potentially o...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2019.11.003
更新日期:2019-11-21 00:00:00
abstract::In this issue of Cell Chemical Biology, Ortega et al. (2016) determine the structure of another lantibiotic dehydratase with a tRNA(Glu)-dependent mechanism of modification. Moreover, they identify a common recognition motif involved in leader peptide binding in a number of different peptide-modification enzymes. Thes...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2016.03.001
更新日期:2016-03-17 00:00:00
abstract::The natural product cepafungin I was recently reported to be one of the most potent covalent inhibitors of the 20S proteasome core particle through a series of in vitro activity assays. Here, we report a short chemoenzymatic total synthesis of cepafungin I featuring the use of a regioselective enzymatic oxidation to p...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.07.012
更新日期:2020-10-15 00:00:00
abstract::Pharmacophore-focused chemical libraries are continuously being created in drug discovery programs, yet screening assays to maximize the usage of such libraries are not fully explored. Here, we report a chemical proteomics approach to reutilizing a focused chemical library of 1,800 indole-containing molecules for disc...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.04.007
更新日期:2020-06-18 00:00:00
abstract::Proper functioning of organelles such as the ER or the Golgi apparatus requires luminal accumulation of Ca(2+) at high concentrations. Here we describe a ratiometric low-affinity Ca(2+) sensor of the GFP-aequorin protein (GAP) family optimized for measurements in high-Ca(2+) concentration environments. Transgenic anim...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2016.05.010
更新日期:2016-06-23 00:00:00
abstract::Protein kinases are attractive therapeutic targets because their dysregulation underlies many diseases, including cancer. The high conservation of the kinase domain and the evolution of drug resistance, however, pose major challenges to the development of specific kinase inhibitors. We recently discovered selective Sr...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2016.07.017
更新日期:2016-09-22 00:00:00
abstract::Alport syndrome is a hereditary glomerular disease caused by mutation in type IV collagen α3-α5 chains (α3-α5(IV)), which disrupts trimerization, leading to glomerular basement membrane degeneration. Correcting the trimerization of α3/α4/α5 chain is a feasible therapeutic approach, but is hindered by lack of informati...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.02.003
更新日期:2018-05-17 00:00:00
abstract::The rise of antibiotic resistance threatens modern medicine; to combat it new diagnostic methods are required. Sequencing the whole genome of a pathogen offers the potential to accurately determine which antibiotics will be effective to treat a patient. A key limitation of this approach is that it cannot classify rare...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2017.12.009
更新日期:2018-03-15 00:00:00
abstract::In the nematode Caenorhabditis elegans, inactivating mutations in the insulin/IGF-1 receptor, DAF-2, result in a 2-fold increase in lifespan mediated by DAF-16, a FOXO-family transcription factor. Downstream protein activities that directly regulate longevity during impaired insulin/IGF-1 signaling (IIS) are poorly ch...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2016.06.015
更新日期:2016-08-18 00:00:00
abstract::In this issue of Cell Chemical Biology, Cook et al. (2019) report a new small-molecule activator that enhances osteogenesis and skeletal regeneration in developmental and adult animal models, respectively. This discovery has therapeutic potential for healing following traumatic bone injury, as well as bone remodeling ...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2019.06.007
更新日期:2019-07-18 00:00:00
abstract::New opportunities to advance small-molecule kinase ligands that downregulate their cognate target binding proteins are discussed. Rationally designed heterobifunctional kinase degraders are compared with ATP site ligands that were serendipitously found to cause kinase downregulation. These approaches could be particul...
journal_title:Cell chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.chembiol.2017.10.011
更新日期:2018-01-18 00:00:00
abstract::Disease sites in atherosclerosis and cancer feature cell masses (e.g., plaques/tumors), a low pH extracellular microenvironment, and various pro-inflammatory cytokines such as tumor necrosis factor α (TNFα). The ability to engineer a cell to seek TNFα sources allows for targeted therapeutic delivery. To accomplish thi...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2017.05.008
更新日期:2017-06-22 00:00:00
abstract::In this issue of Cell Chemical Biology, Harvey et al. (2020) identify 4E14, a sulfhydryl-containing N-acetyltryptophan analog that selectively disrupts binding to the previously undruggable anti-apoptotic BCL2 paralog BFL1, and elucidate a BFL1 conformational change that facilitates 4E14 interaction. These results pro...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.05.014
更新日期:2020-06-18 00:00:00