Metabolic targeting of cancer by a ubiquinone uncompetitive inhibitor of mitochondrial complex I [0.03%]
通过泛醌抑制线粒体复合物I来代谢性靶向癌症的非竞争性抑制剂
Shashi Jain,Cheng Hu,Jerome Kluza et al.
Shashi Jain et al.
SMIP004-7 is a small molecule inhibitor of mitochondrial respiration with selective in vivo anti-cancer activity through an as-yet unknown molecular target. We demonstrate here that SMIP004-7 targets drug-resistant cancer cells with stem-li...
Temporal proteomics reveal specific cell cycle oncoprotein downregulation by p97/VCP inhibition [0.03%]
时间蛋白质组学揭示p97/VCP抑制通过特异性的细胞周期癌蛋白下调作用
Feng Wang,Shan Li,Nadia Houerbi et al.
Feng Wang et al.
Targeting protein quality control (PQC) pathways using proteasome or p97/VCP inhibition can effectively treat blood tumors. However, in solid tumors, only p97/VCP inhibitors are effective. To probe this difference in efficacy, we tracked HC...
Identification of Pax protein inhibitors that suppress target gene expression and cancer cell proliferation [0.03%]
能够抑制目标基因表达和肿瘤细胞增殖的Pax蛋白抑制物的识别
Shayna T J Bradford,Edward Grimley,Ann M Laszczyk et al.
Shayna T J Bradford et al.
The Pax family of developmental control genes are frequently deregulated in human disease. In the kidney, Pax2 is expressed in developing nephrons but not in adult proximal and distal tubules, whereas polycystic kidney epithelia or renal ce...
An allosteric inhibitor of bacterial Hsp70 chaperone potentiates antibiotics and mitigates resistance [0.03%]
细菌Hsp70分子伴娘的变构抑制剂可增强抗生素功效并缓解抗药性
Jordan Hosfelt,Aweon Richards,Meng Zheng et al.
Jordan Hosfelt et al.
DnaK is the bacterial homolog of Hsp70, an ATP-dependent chaperone that helps cofactor proteins to catalyze nascent protein folding and salvage misfolded proteins. In the pathogen Mycobacterium tuberculosis, the causative agent of tuberculo...
PALP: A rapid imaging technique for stratifying ferroptosis sensitivity in normal and tumor tissues in situ [0.03%]
PALP:一种快速成像技术,用于原位分层正常和肿瘤组织中的铁死亡敏感性
Fengxiang Wang,Emily T Graham,Nathchar Naowarojna et al.
Fengxiang Wang et al.
Ferroptosis is an emerging cancer suppression strategy. However, how to select cancer patients for treating with ferroptosis inducers remains challenging. Here, we develop photochemical activation of membrane lipid peroxidation (PALP), whic...
Sweet sensation: Developing a single-cell fluorescent reporter of glycolytic heterogeneity [0.03%]
甜蜜的感知:研发单细胞荧光报道剂来报告糖酵解的异质性
Diane B Karloff,Jennifer M Heemstra
Diane B Karloff
Conversion of in vitro selected aptamers into functional metabolic sensors is hampered by reduced in vivo aptamer binding and limited tunability of cellular metabolite levels. In this issue of Cell Chemical Biology, Ortega et al. (2021) con...
Systemic delivery of a targeted synthetic immunostimulant transforms the immune landscape for effective tumor regression [0.03%]
系统性递送靶向人工免疫刺激物改变免疫格局以实现有效的肿瘤消退
Caitlyn L Miller,Idit Sagiv-Barfi,Patrick Neuhöfer et al.
Caitlyn L Miller et al.
Promoting immune activation within the tumor microenvironment (TME) is a promising therapeutic strategy to reverse tumor immunosuppression and elicit anti-tumor immunity. To enable tumor-localized immunotherapy following intravenous adminis...
Identification of a highly efficient dual type I/II FMS-like tyrosine kinase inhibitor that disrupts the growth of leukemic cells [0.03%]
一种高效双作用I / II型FMS样酪氨酸激酶抑制剂的识别,可破坏白血病细胞的生长
Mandy Beyer,Sven J Henninger,Patricia S Haehnel et al.
Mandy Beyer et al.
Internal tandem duplications (ITDs) in the FMS-like tyrosine kinase-3 (FLT3) are causally linked to acute myeloid leukemia (AML) with poor prognosis. Available FLT3 inhibitors (FLT3i) preferentially target inactive or active conformations o...
ND3 Cys39 in complex I is exposed during mitochondrial respiration [0.03%]
复合物I中的ND3 Cys39在线粒体呼吸过程中暴露出来
Nils Burger,Andrew M James,John F Mulvey et al.
Nils Burger et al.
Mammalian complex I can adopt catalytically active (A-) or deactive (D-) states. A defining feature of the reversible transition between these two defined states is thought to be exposure of the ND3 subunit Cys39 residue in the D-state and ...
Live-cell imaging to analyze intracellular aggregation of recombinant IgG in CHO cells [0.03%]
使用活细胞成像分析CHO细胞中重组IgG的胞内聚集情况
Yukako Senga,Motomichi Doi,Masayoshi Onitsuka et al.
Yukako Senga et al.
Recombinant immunoglobulin G (IgG) aggregates are formed during their production. However, the process underlying intracellular/extracellular aggregation in cell culture conditions is not well understood, and no effective method exists to a...