Results 71 to 80 of about 803,380 (297)

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
FAK mediated tumour cell migration, invasion, survival, proliferation and regulation of tumour stem cells through its kinase-dependent enzymatic functions and kinase-independent scaffolding functions. At present, the development of FAK PROTACs has become
Qiaohua Qin, Ruifeng Wang, Qinglin Fu, Guoqi Zhang, Tianxiao Wu, Nian Liu, Ruicheng Lv, Wenbo Yin, Yin Sun, Yixiang Sun, Dongmei Zhao, Maosheng Cheng   +11 more
doaj   +1 more source

Drug-gene interactions of antihypertensive medications and risk of incident cardiovascular disease: a pharmacogenomics study from the CHARGE consortium [PDF]

, 2015
Background Hypertension is a major risk factor for a spectrum of cardiovascular diseases (CVD), including myocardial infarction, sudden death, and stroke.
Arnett, Donna, Avery, Christy L., Bis, Joshua C., Boerwinkle, Eric, Brody, Jennifer A., Buckley, Brendan M., Chen, Yii-Der Ida, Cummings, Steven R., Cupples, L. Adrienne, Davis, Barry R., de Craen, Anton J. M., Demissie, Serkalem, Eckfeldt, John H., Evans, Daniel S., Ford, Ian, Franco, Oscar H., Gudnason, Vilmundur, Harris, Tamara B., Heckbert, Susan R., Hofman, Albert, Ikram, M. Arfan, Irvin, Ryan, Jukema, J. Wouter, Krijthe, Bouwe P., Lange, Leslie A., Launer, Lenore J., Li, Xiaohui, Liu, Yongmei, Lumley, Thomas, Musani, Solomon K., Post, Wendy, Psaty, Bruce M., Quibrera, P. Miguel, Rotter, Jerome I., Sattar, Naveed, Sitlani, Colleen, Slagboom, P. Eline, Smith, Albert Vernon, Smith, Nicholas L., Sotoodehnia, Nona, Stott, David J., Stricker, Bruno H., Stürmer, Til, Sun, Fangui, Taylor, Herman A., Taylor, Kent D., Tranah, Gregory J., Trompet, Stella, Uitterlinden, Andre G., Vasan, Ramachandran S., Westendorp, Rudi, Whitsel, Eric A., Wiggins, Kerri L., Wilson, James G.   +53 more
core   +4 more sources

Structural biology of ferritin nanocages

FEBS Letters, EarlyView.
Ferritin is a conserved iron‐storage protein that sequesters iron as a ferric mineral core within a nanocage, protecting cells from oxidative damage and maintaining iron homeostasis. This review discusses ferritin biology, structure, and function, and highlights recent cryo‐EM studies revealing mechanisms of ferritinophagy, cellular iron uptake, and ...
Eloise Mastrangelo, Flavio Di Pisa
wiley   +1 more source

Zinc (II)-Mediated Selective O-Benzylation of 2-Oxo-1,2-Dihydropyridines Systems

Molecules, 2018
The selective O-benzylation of 2-oxo-1,2-dihydropyridines plays a critical role in organic synthesis of natural products and biological active molecules.
Qifan Zhou, Fangyu Du, Xinjie Liang, Wenqiang Liu, Ting Fang, Guoliang Chen   +5 more
doaj   +1 more source

Organ‐specific redox imbalances in spinal muscular atrophy mice are partially rescued by SMN antisense oligonucleotides

FEBS Letters, EarlyView.
We identified a systemic, progressive loss of protein S‐glutathionylation—detected by nonreducing western blotting—alongside dysregulation of glutathione‐cycle enzymes in both neuronal and peripheral tissues of Taiwanese SMA mice. These alterations were partially rescued by SMN antisense oligonucleotide therapy, revealing persistent redox imbalance as ...
Sofia Vrettou, Brunhilde Wirth
wiley   +1 more source

Tau acetylation at K331 has limited impact on tau pathology in vivo

FEBS Letters, EarlyView.
We mapped tau post‐translational modifications in humanized MAPT knock‐in mice and in amyloid‐bearing double knock‐in mice. Acetylation within the repeat domain, particularly around K331, showed modest increases under amyloid pathology. To test functional relevance, we generated MAPTK331Q knock‐in mice.
Shoko Hashimoto, Yukio Matsuba, Mika Takahashi, Takaomi C. Saido   +3 more
wiley   +1 more source

Design, Synthesis and Biological Evaluation of N,N-Substituted Amine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors

Molecules, 2017
N,N-Substituted amine derivatives were designed by utilizing a bioisosterism strategy. Consequently, twenty-two compounds were synthesized and evaluated for their inhibitory activity against CETP.
Xinran Wang, Lijuan Hao, Xuanqi Xu, Wei Li, Chunchi Liu, Dongmei Zhao, Maosheng Cheng   +6 more
doaj   +1 more source

Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system

FEBS Letters, EarlyView.
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley   +1 more source

Identification of structural features of surface modifiers in engineered nanostructured metal oxides regarding cell uptake through ML-based classification

Beilstein Journal of Nanotechnology
Nanoparticles (NPs) are considered as versatile tools in various fields including medicine, electronics, and environmental science. Understanding the structural aspects of surface modifiers in nanoparticles that govern their cellular uptake is crucial ...
Indrasis Dasgupta, Totan Das, Biplab Das, Shovanlal Gayen   +3 more
doaj   +1 more source