PCNA degradation exhibits superior pharmacological effects over stoichiometric inhibition [0.03%]
PCNA的降解在药理作用上优于当量抑制效应
Ananya A Basu,Isabella A Riha,Xiaoyu Zhang
Ananya A Basu
In this issue of Cell Chemical Biology, Chang et al. report that a PCNA-targeting bioPROTAC, an engineered E3 ligase linked to a PCNA-binding peptide, has superior pharmacological effects over inhibition of PCNA. Their findings demonstrate ...
Malia B Potts
Malia B Potts
In this issue of Cell Chemical Biology, You et al. demonstrate that selective degradation of ERK5 exhibits neither anti-proliferative nor anti-inflammatory activities previously attributed to ERK5 inactivation. This settles a longstanding d...
Chemoproteomic profiling to identify activity changes and functional inhibitors of DNA-binding proteins [0.03%]
化学蛋白质组学分析以识别DNA结合蛋白的活性变化及其功能抑制剂
Benjamin Ruprecht,Lan Wei,Li Zheng et al.
Benjamin Ruprecht et al.
DNA-binding proteins are promising therapeutic targets but are notoriously difficult to drug. Here, we evaluate a chemoproteomic DNA interaction platform as a complementary strategy for parallelized compound profiling. To enable this approa...
Bortezomib inhibits ZIKV/DENV by interfering with viral polyprotein cleavage via the ERAD pathway [0.03%]
硼替佐米通过干扰病毒多蛋白的切割经ERAD通路抑制ZIKV / DENV病毒感染
Yali Ci,Bin Yao,Kun Yue et al.
Yali Ci et al.
Flaviviruses have posed a serious threat to human health in the past decades, and effective therapeutic drugs are lacking; thus, treatment of flavivirus infection is a great challenge. The flavivirus protease NS2B3 is an attractive target f...
Addressing the Enzyme-independent tumor-promoting function of NAMPT via PROTAC-mediated degradation [0.03%]
通过 PROTAC 介导降解针对NAMPT的非酶促促肿瘤功能
Xiaotong Zhu,Haixia Liu,Li Chen et al.
Xiaotong Zhu et al.
Aberrant overexpression of nicotinamide phosphoribosyltransferase (NAMPT) has been reported in a variety of tumor cells and is a poor prognosis factor for patient survival. It plays an important role in tumor cell proliferation, acting conc...
Targeted degradation of PCNA outperforms stoichiometric inhibition to result in programed cell death [0.03%]
靶向降解PCNA优于剂量限制性抑制诱导肿瘤选择性的程序化癌细胞死亡
Shih Chieh Chang,Pooja Gopal,Shuhui Lim et al.
Shih Chieh Chang et al.
Biodegraders are targeted protein degradation constructs composed of mini-proteins/peptides linked to E3 ligase receptors. We gained deeper insights into their utility by studying Con1-SPOP, a biodegrader against proliferating cell nuclear ...
Ferroptosis inhibition by lysosome-dependent catabolism of extracellular protein [0.03%]
溶酶体依赖性降解细胞外蛋白抑制铁死亡
David A Armenta,Nouf N Laqtom,Grace Alchemy et al.
David A Armenta et al.
Cancer cells need a steady supply of nutrients to evade cell death and proliferate. Depriving cancer cells of the amino acid cystine can trigger the non-apoptotic cell death process of ferroptosis. Here, we report that cancer cells can evad...
Mechanistic insights into cancer drug resistance through optogenetic PI3K signaling hyperactivation [0.03%]
通过光遗传学活化PI3K信号研究癌症药物耐药性的机制
Yoshibumi Ueda,Yuri Miura,Nario Tomishige et al.
Yoshibumi Ueda et al.
Hyperactivation of phosphatidylinositol 3-kinase (PI3K) signaling is a prominent feature in cancer cells. However, the mechanism underlying malignant behaviors in the state remains unknown. Here, we describe a mechanism of cancer drug resis...
Multiplexed bioluminescence imaging with a substrate unmixing platform [0.03%]
一种采用底物分离平台的多重生物发光成像技术
Caroline K Brennan,Zi Yao,Anastasia A Ionkina et al.
Caroline K Brennan et al.
Bioluminescent tools can illuminate cellular features in whole organisms. Multi-component tracking remains challenging, though, owing to a lack of well-resolved probes and long imaging times. To address the need for more rapid, quantitative...
Identification of proteomic landscape of drug-binding proteins in live cells by proximity-dependent target ID [0.03%]
用于识别活细胞中与药物结合蛋白的邻近依赖性目标识别技术
Chulhwan Kwak,Cheolhun Park,Minjeong Ko et al.
Chulhwan Kwak et al.
Direct identification of the proteins targeted by small molecules can provide clues for disease diagnosis, prevention, and drug development. Despite concentrated attempts, there are still technical limitations associated with the elucidatio...