Results 291 to 300 of about 379,625 (351)

Resolvin D5 Inhibits CXCL8 Expression in Colonic Epithelial Cells Through Activating GPR101 to Impede Neutrophil Recruitment and Consequently Alleviate Ulcerative Colitis

Advanced Science, EarlyView.
RvD5 effectively alleviates UC by inhibiting STAT1 signaling to reduce CXCL8 expression in colonic epithelial cells via activation of GPR101, which subsequently decreases the infiltration of neutrophils in the colonic mucosal epithelium. Epimedin A1, a natural allosteric inhibitor of 5‐LOX, demonstrates potential as a therapeutic agent for UC by ...
Pengxiang Guo, Yilei Guo, Yanrong Zhu, Ke Yan, Yulai Fang, Jiafeng Zhang, Yue He, Zhifeng Wei, Yufeng Xia, Yue Dai   +9 more
wiley   +1 more source

Targeting Lactate and Lactylation in Cancer Metabolism and Immunotherapy

Advanced Science, EarlyView.
Lactate, once deemed a metabolic waste, emerges as a central regulator of cancer progression. This review elucidates how lactate and its epigenetic derivative, protein lactylation, orchestrate tumor metabolism, immune suppression, and therapeutic resistance.
Jiajing Gong, Yuhang Xie, Zhijie Weng, Yongzhi Wu, Longjiang Li, Bo Li   +5 more
wiley   +1 more source

IL‐4/STAT6‐signaling Influences Local Inflammation and Regeneration Processes During Acute Pancreatitis and Promotes Fibrosis by a Direct Activation of Pancreatic Fibroblasts During Chronic Pancreatitis

Advanced Science, EarlyView.
IL‐4/IL‐13/STAT6 signaling plays a crucial for the suppression of pro‐inflammation during acute pancreatitis and supports acinar cell regeneration but has only minor impact on fibrogenesis during chronic form of the disease. IL‐4/IL‐13 induce the expression of certain collagens directly in pancreatic fibroblasts via STAT6 activation, whereas ...
ElSheikh H, Salvers A, Piesker J, Buchholz S, Lange R, Ameling S, Steil L, Hammer E, Homuth G, Völker U, Bröker BM, Weiss FU, Sendler M, Glaubitz J   +13 more
wiley   +1 more source

AI‐Driven Acceleration of Fluorescence Probe Discovery

Advanced Science, EarlyView.
We present PROBY, an AI model trained on large‐scale datasets to predict key photophysical properties and accelerate the discovery of target‐specific fluorescent probes. By screening a target‐annotated library, PROBY identifies candidate probes for diverse targets and could guide probe optimization, enabling a range of in vitro and in vivo imaging ...
Xuefeng Jiang, Yanbo Li, Xue Tian, Sen Yang, Ruina Luo, Cenxing Zhou, Yuxuan Liu, Jingying Hu, Sen Feng, Lu Gan, Chongzhao Ran, Kun‐Hsing Yu, Junhan Zhao, Xiao Han, Xuan Zhai, Yuntao Jia, Jiapei Dai, Xiyue Wang, Biyue Zhu   +18 more
wiley   +1 more source

DNA Nanoflower LYTACs Enable Efficient VEGF Degradation and Verteporfin Loading for Combined Therapy of Wet Age‐Related Macular Degeneration

Advanced Science, EarlyView.
An integrated approach that combines a DNA nanoflower VEGF degrader with photodynamic therapy is developed for the treatment of wet age‐related macular degeneration, which reduces the risk of VEGF reactivation‐induced CNV recurrence and minimizes the systemic side effects associated with photodynamic therapy.
Mengxuan Li, Yan Yue, Sijin Wu, Xinyu He, Jiayi Song, Shuwen Ma, Haokun Zhang, Chenyu Xu, Song Chen, Yanming Huang, Songbo Xie, Hua Yan   +11 more
wiley   +1 more source

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Transient Receptor Potential A1 Modulators

Current Topics in Medicinal Chemistry, 2011
TRPA1 is a member of a superfamily of non-selective cation channels that is known to be involved in multiple physiological functions. TRPA1 is activated by a broad spectrum of chemical irritants and endogenous inflammatory compounds. An emerging role for TRPA1 in mediating pain and inflammation raises the possibility that compounds targeting TRPA1 ...
Tim, Strassmaier, Rajagopal, Bakthavatchalam   +1 more
openaire   +2 more sources

Adenosine A1-receptor occupancy predicts A1-receptor antagonist effects of N-0861*

Clinical Pharmacology & Therapeutics, 1998
To evaluate the relationship between dose of N-0861 ([+/-]N6-endo-norbornan-2-yl-9-methyladenine), N-0861 plasma concentrations, and antagonism of adenosine-induced slowing of atrioventricular nodal conduction and to evaluate A1-receptor occupancy by antagonist present in plasma of subjects after administration of N-0861 to determine A1-selectivity of ...
S U, Yasuda, S, Nagashima, E, Douyon, R E, Benton, R L, Woosley, J T, Barbey   +5 more
openaire   +2 more sources

Adenosine A1 receptors and erythropoietin production

American Journal of Physiology-Cell Physiology, 1993
N6-cyclopentyladenosine (CPA), a selective adenosine A1 receptor agonist, in a concentration range of 10(-9) to 10(-7) M, produced a significant decrease in erythropoietin (EPO) levels in a human hepatocellular carcinoma (Hep G2) cell culture (medium levels of EPO, 91.81 +/- 1.61 and 94.36 +/- 0.97% of control, respectively) after 24 h incubation in a
T, Ohigashi, J, Brookins, J W, Fisher
openaire   +2 more sources

Adenosine receptor modelling. A1/A2a selectivity

European Journal of Medicinal Chemistry, 2006
Three-dimensional models of the A(1) and A(2a) adenosine receptors (AR) were constructed by means of a homology procedure, using bovine rhodopsin as a template. In order to validate the two models, a docking analysis of selective agonists was carried out.
TUCCINARDI, TIZIANO, ORTORE, GABRIELLA MARIA PIA, MANERA, CLEMENTINA, SACCOMANNI, GIUSEPPE, MARTINELLI, ADRIANO   +4 more
openaire   +3 more sources

Allosteric modulators for the A1 adenosine receptor

Expert Opinion on Therapeutic Patents, 2004
A review. Allosteric modulators of endogenous adenosine represent an alternative to direct acting adenosine agonists and nucleoside uptake blockers. These compds. can selectively enhance the response to adenosine in only those organs or localized areas of a given organ in which prodn. of adenosine is increased. The present article is an overview of the
BARALDI, Pier Giovanni, MOORMAN ALLAN R., AGHAZADEH TABRIZI, Mojgan, PAVANI, Maria Giovanna, ROMAGNOLI, Romeo   +4 more
openaire   +2 more sources