Results 21 to 30 of about 2,739,450 (298)

Modulation of nongenomic activation of PI3K signalling by tetramerization of N-terminally-cleaved RXRα

Nature Communications, 2017
The transcription factor retinoid X receptor-alpha (RXRα) can also form homotetramers. Here the authors show that the anti-cancer agent K-80003 selectively inhibits the nongenomic action of N-terminally-cleaved RXRα in tumour cells by stabilizing its ...
Liqun Chen, Alexander E. Aleshin, Gulimiran Alitongbieke, Yuqi Zhou, Xindao Zhang, Xiaohong Ye, Mengjie Hu, Gaoang Ren, Ziwen Chen, Yue Ma, Duo Zhang, Shuai Liu, Weiwei Gao, Lijun Cai, Lingjuan Wu, Zhiping Zeng, Fuquan Jiang, Jie Liu, Hu Zhou, Gregory Cadwell, Robert C. Liddington, Ying Su, Xiao-kun Zhang   +22 more
doaj   +1 more source

Norlichexanthone purified from plant endophyte prevents postmenopausal osteoporosis by targeting ERα to inhibit RANKL signaling

Acta Pharmaceutica Sinica B, 2021
Although different types of drugs are available for postmenopausal osteoporosis, the limitations of the current therapies including drug resistances and adverse effects require identification of novel anti-osteoporosis agents.
Keqi Wang, Yongyan Chen, Shuo Gao, Maosi Wang, Mengmeng Ge, Qian Yang, Mingkai Liao, Lin Xu, Junjie Chen, Zhiping Zeng, Haifeng Chen, Xiao-kun Zhang, Ting Lin, Hu Zhou   +13 more
doaj   +1 more source

The benefits of in silico modeling to identify possible small-molecule drugs and their off-target interactions [PDF]

, 2018
Accepted for publication in a future issue of Future Medicinal Chemistry.The research into the use of small molecules as drugs continues to be a key driver in the development of molecular databases, computer-aided drug design software and collaborative ...
Blomberg N, Choi SH, Hastings J, Hirschey J, Mire Zloh, Stewart B Kirton, Wang X   +6 more
core   +2 more sources

Antihyperuricemic effect of mangiferin aglycon derivative J99745 by inhibiting xanthine oxidase activity and urate transporter 1 expression in mice

Acta Pharmaceutica Sinica B, 2018
A mangiferin aglycon derivative J99745 has been identified as a potent xanthine oxidase (XOD) inhibitor by previous in vitro study. This study aimed to evaluate the hypouricemic effects of J99745 in experimental hyperuricemia mice, and explore the ...
Zhizhen Qin, Shoubao Wang, Yihuang Lin, Ying Zhao, Shengqian Yang, Junke Song, Tao Xie, Jinlong Tian, Song Wu, Guanhua Du   +9 more
doaj   +1 more source

Computational structure‐based drug design: Predicting target flexibility [PDF]

, 2018
The role of molecular modeling in drug design has experienced a significant revamp in the last decade. The increase in computational resources and molecular models, along with software developments, is finally introducing a competitive advantage in early
Ding X., Dreher J., Khago D., Li Y., Samuel G.   +4 more
core   +2 more sources

Industry-scale application and evaluation of deep learning for drug target prediction [PDF]

, 2019
Artificial intelligence (AI) is undergoing a revolution thanks to the breakthroughs of machine learning algorithms in computer vision, speech recognition, natural language processing and generative modelling.
Ashby, Thomas J., Böhm, Stanislav, Ceulemans, Hugo, Chen, Hongming, Chupakhin, Vladimir, Cima, Vojtěch, Engkvist, Ola, Golib-Dzib, Jose-Felipe, Greene, Nigel, Hochreiter, Sepp, Jeliazkova, Nina, Klambauer, Günter, Martinovič, Jan, Mayr, Andreas, Sturm, Noe, Van, Thanh Le, Vander Aa, Tom, Vandriessche, Yves, Wegner, Joerg   +18 more
core   +2 more sources

Oncogenic potential of truncated RXRα during colitis-associated colorectal tumorigenesis by promoting IL-6-STAT3 signaling

Nature Communications, 2019
The truncated form of retinoid X receptor-alpha is found in cancer. Here, the authors show that this mutant receptor promotes colorectal tumorigenesis by activation of NF-κB in myeloid cells, leading to subsequent IL-6-induced STAT3 activation in ...
Xiaohong Ye, Hua Wu, Luoyan Sheng, Yi-xin Liu, Fang Ye, Mo Wang, Hu Zhou, Ying Su, Xiao-kun Zhang   +8 more
doaj   +1 more source

miR-218 targets survivin and regulates resistance to chemotherapeutics in breast cancer [PDF]

, 2015
Multidrug resistance (MDR) remains one of the most significant obstacles in breast cancer treatment, and this process often involves dysregulation of a great number of microRNAs (miRNAs).
Hu, Y, Xu, K, Yagüe, E
core   +1 more source

Knockout of Nur77 Leads to Amino Acid, Lipid, and Glucose Metabolism Disorders in Zebrafish

Frontiers in Endocrinology, 2022
Orphan nuclear receptor Nur77 has been reported to be implicated in a diverse range of metabolic processes, including carbohydrate metabolism and lipid metabolism.
Yang Xu, Juanjuan Tian, Qi Kang, Qi Kang, Hang Yuan, Chengdong Liu, Zhehui Li, Jie Liu, Mingyu Li   +8 more
doaj   +1 more source

The efficiency of multi-target drugs: the network approach might help drug design

, 2005
Despite considerable progress in genome- and proteome-based high-throughput screening methods and rational drug design, the number of successful single target drugs did not increase appreciably during the past decade.
Agoston, Vilmos, Csermely, Peter, Pongor, Sandor   +2 more
core   +1 more source