Results 151 to 160 of about 537,284 (311)

Targeting UXS1‐Dependent Glucuronate Detoxification Potentiates Metformin's Anti‐Tumor Efficacy in Lung Adenocarcinoma

Advanced Science, EarlyView.
This study reveals that metformin promotes glucuronic acid metabolism in lung adenocarcinoma by activating UGDH S476 phosphorylation and enhancing the conversion of UDPG to UDPGA based on metabolomics analysis. Through compound virtual screening, it is found that plantainoside targeting UGDH downstream UXS1 leads to UDPGA toxicity accumulation ...
Qihai Sui, Zhencong Chen, Guangyao Shan, Zhengyang Hu, Xing Jin, Jiaqi Liang, Yanjun Yi, Jiacheng Yin, Haochun Shi, Xifei Jiang, Junjie Xi, Zongwu Lin, Cheng Zhan, Fenghao Sun, Wei Jiang   +14 more
wiley   +1 more source

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

Advanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel, Sofia Kokkaliari, Qiwen Gao, Jinjing Chen, Larissa Costa de Almeida, Srinivasarao Tenneti, Derek A. Leas, Eli Levit, Lewis S. Alexander, Khalil A. Abboud, Pingrong Wei, Michael D. Cameron, James R. Rocca, Ranjala Ratnayake, Donna D. Zhang, Hendrik Luesch, Robert W. Huigens III   +16 more
wiley   +1 more source

Microflow of fluorescently labelled red blood cells in tumours expressing single isoforms of VEGF and their response to VEGF-R tyrosine kinase inhibition

, 2009
This paper was presented at the 2nd Micro and Nano Flows Conference (MNF2009), which was held at Brunel University, West London, UK. The conference was organised by Brunel University and supported by the Institution of Mechanical Engineers, IPEM, the ...
Bjorndahl, MA, 2nd Micro and Nano Flows Conference (MNF2009), Tozer, GM, Evans, H, Pettyjohn, KL, Reyes-Aldasoro, CC, Akerman, S, Fisher, M   +7 more
core  

Functional Mapping of Neurodevelopmental Disease Pathways to Key Neurodevelopmental Processes Represented in the Developmental Neurotoxicity In Vitro Testing Battery

Advanced Science, EarlyView.
Human‐relevant methods are essential for modern chemical safety assessment. This study helps define the capabilities and boundaries of an in vitro testing battery for developmental neurotoxicity by exploring its biological applicability domain. By linking neurodevelopmental disease‐related pathways to key neurodevelopmental processes, the work enhances
Eliska Kuchovska, Kristina Bartmann, Georgea Raad, Mats Schade, Luiz Ladeira, Arif Dönmez, Jördis Klose, Nicolai Görts, Denis Polozij, Lynn‐Christin Saborowski, Farina Bendt, Bernard Staumont, Liesbet Geris, Katharina Koch, Ellen Fritsche   +14 more
wiley   +1 more source

O‐GlcNAcylated TAP1 Impairs Antigen Presentation and Promotes Immune Evasion in Bladder Cancer

Advanced Science, EarlyView.
This article unveils a critical mechanism of immune evasion in bladder cancer, which the O‐GlcNAc modification of TAP1 disrupts antigen presentation. This modification triggers HLA‐A degradation, shielding tumor cells from CD8+ T cell attack. The findings highlight targeting this pathway as a promising therapeutic avenue to sensitize tumors to ...
Jinpeng Wu, Xueting Ren, Zhen Zhai, Lu Wang, Liang Liang, Zengqi Tan, Jiazhen Zhao, Yuxuan Han, Yuhan Li, Feng Guan, Xiang Li   +10 more
wiley   +1 more source

Molecular Glue cc‐885 Inhibits VHL‐Deficient Clear Cell Renal Cell Carcinoma via ETS1 Degradation

Advanced Science, EarlyView.
VHL‐deficient kidney cancer lacks effective treatments. This study reveals that the molecular glue degrader cc‐885 hijacks the cellular recycling system to selectively destroy the oncogenic protein ETS1, effectively killing VHL‐mutant tumors. Combining CC‐885 with the approved drug belzutifan achieves powerful synergy, offering a promising new ...
Taowei Yang, Qihao Li, Kun Ye, Kezhi Liu, Mi Zhou, Minyu Chen, Lican Liao, Kangbo Huang, Zhu Wang, Qiong Deng, Jieyan Wang, Meiyu Jin, Xu Chen, Hui Liang, Jiaxing Zhang, Junhang Luo   +15 more
wiley   +1 more source

Bosutinib: a SRC–ABL tyrosine kinase inhibitor for treatment of chronic myeloid leukemia

, 2013
Fuad El Rassi, Hanna Jean KhouryDivision of Hematology, Department of Hematology and Medical Oncology, the Winship Cancer Institute at Emory University, Atlanta, Georgia, USAAbstract: Bosutinib is one of five tyrosine kinase inhibitors commercially ...
Khoury HJ, El Rassi F
core  

Disruption of Treg Homeostasis in Rheumatoid Arthritis via Ferroptosis‐Mediated ETC Collapse and TXK‐STAT3/PLCγ1 Activation

Advanced Science, EarlyView.
In rheumatoid arthritis, synovial Tregs accumulate but are functionally impaired due to iron overload‐induced ferroptosis. This triggers mitochondrial dysfunction and TXK tyrosine kinase‐mediated signaling, leading to Treg destabilization and inflammation.
Jingrong Chen, Xiao Guan, Kexu Xiong, Xiaoyi Shi, Luyao Wu, Chuanxin Su, Jun Zhao, Rongzhen Liang, Huimin Wang, Junlong Dang, Ye Chen, Yiding Xiong, Chi Zhou, Futao Zhao, Zhenhang Zhu, Xiaoli Fan, Li Zhou, Nancy Olsen, Yutong Jiang, Song Guo Zheng   +19 more
wiley   +1 more source

The role of receptor tyrosine kinase signalling in HER-2-positive cells and trastuzumab (Herceptin) resistance in breast cancer [PDF]

, 2009
HER-2 gene amplification or overexpression occurs in approximately 25 % of breast cancers, and trastuzumab (Tmab) is a monoclonal antibody currently used to treat patients with HER-2-overexpressing breast cancer.
Browne, Brigid
core  

An Activity‐Dependent NEPAS–PTX3 Axis Links Neurovascular and Myelin Deficits to Cognitive Impairment

Advanced Science, EarlyView.
An activity‐dependent pathway links prefrontal circuit hypoactivity to cognitive impairment. Reduced PVA–mPFC activity upregulates NEPAS, which suppresses PTX3 secretion, leading to impaired angiogenesis, myelin deficits, and memory decline. Rescue is achieved by NEPAS knockdown or chemogenetic circuit activation.
Boya Hu, Zifei Chen, Bingmei Sun, Jiale Gao, Jiale Xu, Xiaochun Guo, Fenfei Gao, Zhongsi Wang, Jie Wu, Xiaoyu Ji, Peipei Liu, Bing Huang   +11 more
wiley   +1 more source