Results 71 to 80 of about 69,829 (264)

Studies in molecular modeling, in vitro CDK2 inhibition and antimetastatic activity of some synthetic flavones

Frontiers in Bioscience-Landmark, 2020
Naturally occurring flavonoids have been shown to possess anticancer activity. We have previously shown that certain synthetic flavonoids also exert significant antiproliferative potential in MOLT-4, MCF-7, and HepG2 cell lines. To this end, we evaluated
Ojas S.Wagal, Akshada J. Joshi, Urmila J. Joshi, Heena R. Bhojwani, Khushboo V. Begwani, Harshank A. Dawne, Rajiv P. Gude, Sadhana S. Sathaye, Divya M. Kanchan   +8 more
doaj   +1 more source

Phosphorylation‐Facilitated CKB Lactylation At K11 By GCN5 Enhances Creatine Kinase Activity and Mitigates Neuronal Damage After Cerebral Ischemia‐Reperfusion

Advanced Science, EarlyView.
This study uncovers hierarchical coordination between K11 lactylation and S199 phosphorylation of CKB in cerebral ischemia‐reperfusion injury. Such dual modifications potentiate CKB enzymatic function, remodel energy metabolism, alleviate oxidative stress and neuronal damage, and represent a viable therapeutic target for stroke treatment.
Chao Duan, Ruolin Zhang, Shihui Ding, Ying Feng, Tao Shen, Ziwei Wang, Wendai Bao, Ke Shui, Jun Qin, Jun Chen, Min Zhang, Zijing Ren, Dongmei Zhao, Xingrong Guo, Zhibing Ai, Xin Yang, Peiyang Zhou, Zhiqiang Dong   +17 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

Covalent Inhibition of SHMT2 by Gambogic Acid Induces Ferroptosis Through Mitochondrial Collapse in Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
In this study, chemoproteomics combined with genetic and functional analyses was integrated to identify SHMT2 as a covalent and functional target of gambogic acid (GA) in triple‐negative breast cancer (TNBC). Further validation demonstrated that GA selectively modifies the Cys241 site of SHMT2, triggering mitochondrial dysfunction, activating the Nrf2 ...
Tong Yang, Chong Qiu, Yulei Li, Ying Zhang, Chen Wang, Jie Zhou, Zheng Chu, Ang Ma, Ling Huang, Yin Kwan Wong, Junzhe Zhang, Peng Gao, Cui Liu, Junhua Zhang, Huan Tang, Jigang Wang   +15 more
wiley   +1 more source

TSPYL5 Promotes Triple‐Negative Breast Cancer Metastasis by Antagonizing USP10‐Mediated PTEN Stabilization to Unleash a ZEB1‐Dependent EMT Program

Advanced Science, EarlyView.
The hyperactivation of PI3K/AKT signaling in PTEN wild‐type triple‐negative breast cancer represents a clinical paradox. We delineate a novel post‐translational regulatory axis wherein the oncogene TSPYL5 competitively antagonizes the deubiquitinase USP10.
Jiaying Shi, Ming Yi, Shengyu Xie, Zhaokun Wang, Xinyue Zhang, Yangwei Zhang, Rui Tang, Yuan Yang, Yunqiang Liu   +8 more
wiley   +1 more source

Subtractive proteomics-based vaccine targets annotation and reverse vaccinology approaches to identify multiepitope vaccine against Plesiomonas shigelloides

Heliyon
Plesiomonas shigelloides, an aquatic bacterium belonging to the Enterobacteriaceae family, is a frequent cause of gastroenteritis with diarrhea and gastrointestinal severe disease.
Danish Rasool, Sohail Ahmad Jan, Sumra Umer Khan, Nazia Nahid, Usman Ali Ashfaq, Ahitsham Umar, Muhammad Qasim, Fatima Noor, Abdur Rehman, Kiran Shahzadi, Abdulrahman Alshammari, Metab Alharbi, Muhammad Atif Nisar   +12 more
doaj   +1 more source

The Development and Pilot Clinical Study of CD147 Targeted Antagonistic Peptide Probe for Tumor Imaging

Advanced Science, EarlyView.
This study establishes [68Ga]Ga‐DOTA‐AP9 as a first‐in‐human CD147‐targeted PET tracer with favorable safety and specific tumor uptake. Tracer accumulation correlates with CD147 expression in patients, enabling noninvasive quantification of CD147‐positive malignancies.
Xiaokun Ma, Rui Guo, Dongfeng Niu, Yufei Song, Zhenyao Zhang, Xiangxi Meng, Lili Mao, Haifeng Huang, Hua Zhu, Zhi Yang, Teli Liu   +10 more
wiley   +1 more source

High Selectivity of Dipeptidyl Peptidase 4 Receptor Towards 13 Aromatic Compounds in Cinnamomi ramulus Extract: Molecular Docking and Molecular Dynamics

Engineering Proceedings
Dipeptidyl peptidase 4 (DPP4) plays a pivotal role in the treatment of type 2 diabetes as an important glucose-regulating enzyme. We evaluated the molecular interactions between 13 major aromatic compounds from Cinnamomi ramulus and DPP4 enzyme through ...
Vo Van On, Ho Anh Kiet, Nguyen Thi Thanh Thao, Nguyen Thi Lien Thuong   +3 more
doaj   +1 more source

ANKS1B in the Nucleus Accumbens Controls Escalated Cocaine Self‐Administration via Regulating CBP‐FoxO3 Complex

Advanced Science, EarlyView.
ANKS1B in the nucleus accumbens plays a critical role in the transition from controlled to escalated cocaine intake. Mechanistically, ANKS1B interacts with CBP to epigenetically suppress FoxO3 through H3K27 acetylation. The ANKS1B‐CBP‐FoxO3 signaling cascade presents a novel theraputic target for the treatment of cocaine addiction.
Liping Yang, Xiaoxuan Wu, Xuan Chen, Chao Peng, Zihang Li, Shumin Gao, Shiqiu Meng, Jing Dong, Dong Wu, Liying Lv, Ying Han, Yanxue Xue, Lin Lu, Jie Shi, Jianfeng Liu, Yan Sun   +15 more
wiley   +1 more source

Harnessing MDM2‐Mediated Targeted Degradation of Transcriptional and Epigenetic Machinery to Disrupt Oncogenic Addictions in Pediatric Sarcoma

Advanced Science, EarlyView.
MDM2 dependency in pediatric sarcomas is driven by a novel p53‐independent oncogenic cistrome alongside canonical p53 pathway suppression. This study introduces MDM2‐recruiting transcriptional and epigenetic machinery degraders (MDM2‐TEMADs) as a novel precision oncology modality.
Jiawei Zhou, Xian Guan, Nan Li, Ying Zhang, Long Xie, Xingze Huang, Zhipeng Zhu, Zhuolin Ren, Xiaoyan Yu, Hanjun Guo, Yuanfang Wu, Lin Ma, Suya Zheng, Jingyao Zhang, Jiyang Liu, Victor Kuanmin Lee, Wenhao Chen, H. Phillip Koeffler, Jinhu Wang, Xin Han, Ye Chen, Liang Xu   +21 more
wiley   +1 more source