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 excellent co-therapeutics for a number of tumor types.
journal_name
Cell Chem Bioljournal_title
Cell chemical biologyauthors
Hardy JAdoi
10.1016/j.chembiol.2018.08.001subject
Has Abstractpub_date
2018-08-16 00:00:00pages
927-928issue
8eissn
2451-9456issn
2451-9448pii
S2451-9456(18)30267-8journal_volume
25pub_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::The engineered ascorbate peroxidase (APEX) is a powerful tool for the proximity-dependent labeling of proteins and RNAs in live cells. Although widely use in mammalian cells, APEX applications in microorganisms have been hampered by the poor labeling efficiency of its biotin-phenol (BP) substrate. In this study, we so...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.05.006
更新日期:2020-07-16 00:00:00
abstract::Acyl-coenzyme A (CoA)/protein interactions are essential for life. Despite this importance, their global scope and selectivity remains undefined. Here, we describe CATNIP (CoA/AcetylTraNsferase Interaction Profiling), a chemoproteomic platform for the high-throughput analysis of acyl-CoA/protein interactions in endoge...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2019.11.011
更新日期:2020-03-19 00:00:00
abstract::Mycobacterium tuberculosis synthesizes a wide variety of complex lipids that can serve as antigens in immune recognition of the bacterium. In this issue of Cell Chemical Biology, Gilleron et al. (2016) identify key enzymes essential for lipid antigen processing, which is required for CD1b-restricted T cell activation....
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2016.09.005
更新日期:2016-09-22 00:00:00
abstract::While the wound healing property of the macrolide FK506 is well known, the underlying mechanism has been elusive. In this issue of Cell Chemical Biology, Peiffer et al. (2019) utilize FKBP12 ligand to demonstrate that wound healing effects of FK506 occur via activation of the BMP (bone morphogenic protein) signaling p...
journal_title:Cell chemical biology
pub_type: 评论,杂志文章
doi:10.1016/j.chembiol.2019.05.001
更新日期:2019-05-16 00:00:00
abstract::Chemical strategies to block quorum sensing (QS) could provide a route to attenuate virulence in bacterial pathogens. Considerable research has focused on this approach in Pseudomonas aeruginosa, which uses the LuxR-type receptor LasR to regulate much of its QS network. Non-native ligands that antagonize LasR have bee...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.06.007
更新日期:2018-09-20 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::Increased telomerase activity is associated with malignancy and poor prognosis in human cancer, but the development of targeted agents has not yet provided clinical benefit. Here we report that, instead of targeting the telomerase enzyme directly, small molecules that bind to the G-hairpin of the hTERT G-quadruplex-fo...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2019.04.009
更新日期:2019-08-15 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::A protein-fragment complementation assay (PCA) for detecting and localizing intracellular protein-protein interactions (PPIs) was built by bisection of miniSOG, a fluorescent flavoprotein derived from the light, oxygen, voltage (LOV)-2 domain of Arabidopsis phototropin. When brought together by interacting proteins, t...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2019.07.007
更新日期:2019-10-17 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::Clostridium difficile causes increasing numbers of life-threatening intestinal infections. Symptoms associated with C. difficile infection (CDI) are mediated by secreted protein toxins, whose virulence is modulated by intracellular auto-proteolysis following allosteric activation of their protease domains by inositol ...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2018.10.002
更新日期:2019-01-17 00:00:00
abstract::Phenotypic drug discovery offers some advantages over target-based methods, mainly because it allows drug leads to be tested in systems that more closely model distinct disease states. However, a potential disadvantage is the difficulty of linking the observed phenotype to a specific cellular target. To address this p...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2016.08.011
更新日期:2016-10-20 00:00:00
abstract::The mechanisms by which cancer cell-intrinsic CYP monooxygenases promote tumor progression are largely unknown. CYP3A4 was unexpectedly associated with breast cancer mitochondria and synthesized arachidonic acid (AA)-derived epoxyeicosatrienoic acids (EETs), which promoted the electron transport chain/respiration and ...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2017.08.009
更新日期:2017-10-19 00:00:00
abstract::Despite the urgent need for assays to visualize insulin secretion there is to date no reliable method available for measuring insulin release from single cells. To address this need, we developed a genetically encoded reporter termed RINS1 based on proinsulin superfolder GFP (sfGFP) and mCherry fusions for monitoring ...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2017.03.001
更新日期:2017-04-20 00:00:00
abstract::In this issue of Cell Chemical Biology, Sakin et al. (2017) investigate the nanoscale behavior of the HIV-1 envelope (Env) glycoprotein complex by using genetic code expansion, bioorthogonal amino acids, synthetic dyes, and click chemistry. This minimally invasive approach allows the measurement of native Env cellular...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2017.05.006
更新日期:2017-05-18 00:00:00
abstract::Electron microscopy (EM) remains the primary method for imaging cellular and tissue ultrastructure, although simultaneous localization of multiple specific molecules continues to be a challenge for EM. We present a method for obtaining multicolor EM views of multiple subcellular components. The method uses sequential,...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2016.10.006
更新日期:2016-11-17 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::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::This month: Lysosomal iron linked to cell death in cancer stem cells, non-enzymatic catalyst SynCAc for histone acylation, cytotoxins ivermectin and etoposide bring new anti-fungals out of the crypt, and 2'-deoxy-ADPR as second messenger activating TRPM2. ...
journal_title:Cell chemical biology
pub_type:
doi:10.1016/j.chembiol.2017.07.016
更新日期:2017-08-17 00:00:00
abstract::Because small-molecule activators of adenylyl cyclases (AC) affect ACs cell-wide, it is challenging to explore the signaling consequences of AC activity emanating from specific intracellular compartments. We explored this issue using a series of engineered, optogenetic, spatially restricted, photoactivable adenylyl cy...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2019.07.004
更新日期:2019-10-17 00:00:00
abstract::ATP is an important energy metabolite and allosteric signal in health and disease. ATP-interacting proteins, such as P2 receptors, control inflammation, cell death, migration, and wound healing. However, identification of allosteric ATP sites remains challenging, and our current inventory of ATP-controlled pathways is...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.05.010
更新日期:2020-08-20 00:00:00
abstract::Epidermal growth factor receptor (EGFR) is a target of signal-derived H2O2, and oxidation of active-site cysteine 797 to sulfenic acid enhances kinase activity. Although a major class of covalent drugs targets C797, nothing is known about its catalytic importance or how S-sulfenylation leads to activation. Here, we re...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2016.05.017
更新日期:2016-07-21 00:00:00
abstract::The rapid emergence of extensively drug-resistant A. baumannii has posed a major threat to global public health, emphasizing the desperate need for novel therapeutic strategies. We report the development of a highly efficient genome-engineering platform in A. baumannii by coupling a Cas9 nuclease-mediated genome cleav...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2019.09.003
更新日期:2019-12-19 00:00:00
abstract::Tumor suppressor genes represent a major class of oncogenic drivers. However, direct targeting of loss-of-function tumor suppressors remains challenging. To address this gap, we explored a variant-directed chemical biology approach to reverse the lost function of tumor suppressors using SMAD4 as an example. SMAD4, a c...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.11.010
更新日期:2020-12-04 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
abstract::Despite widespread interest for understanding how modified bases have evolved their contemporary functions, limited experimental evidence exists for measuring how close an organism is to accidentally creating a new, modified base within the framework of its existing genome. Here, we describe the biochemical and struct...
journal_title:Cell chemical biology
pub_type: 杂志文章
doi:10.1016/j.chembiol.2020.09.006
更新日期:2021-01-21 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::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