Heptahelical G protein-coupled receptors (GPCRs) are arguably the most important single class of pharmaceutical drug targets in the human genome. According to Overington, of the 266 human targets for approved d...
G-protein coupled receptors in lipid rafts and caveolae: how, when and why do they go there? 来自 国家科技图书文献中心 喜欢 0 阅读量: 53 作者: Chini,B 摘要: This review describes the advances in our understanding of the role of G-protein coupled receptor (GPCR) localisation in ...
Moreover, investigators observed that transforming Ca2+ permeable receptors to impermeable ones diminished the proliferative activity and enhanced the apoptotic potentials of the glioma cells [47]. It is to be concluded from this study that Ca2+ entry through these channels may hurdle the apoptotic ...
Credit: CC0 Public Domain Many pharmaceuticals work by targeting what are known as 'G-protein-coupled receptors.' In a new study, scientists from Uppsala University describe how they have been able to predict how special molecules that can be used in new immunotherapy against cancer bind to the...
In these investigations, specific Ca2+ activation was achieved through the use of transgenic mice in which astrocytes express MrgA1 Gq-coupled receptors that respond to a specific agonist and are normally not found in the CNS. Limitations of this approach, however, include the...
We also collected the allosteric modulators of the ASD database17 or a selection of conventional inhibitors that are active in the top 100 most studied targets from BindingDB18 (version 2012), which are all conventional targets, i.e., GPCRs (G-protein coupled receptors), enzymes, kinases, ...
This is often true for multiple motifs within enhancers, suggesting that their function is coupled via AND logic (Figure 2a) [48]. To achieve such coupling, the best understood mechanism is a composite motif, that is, two motifs to which two TFs bind cooperatively through protein–protein ...
Mason JS, Bortolato A, Congreve M, Marshall FH (2012) New insights from structural biology into the druggability of G protein-coupled receptors. Trends Pharmacol Sci 33(5):249–260. doi:10.1016/j.tips.2012.02.005 CAS Google Scholar Smith RD, Dunbar JB Jr, Ung PM-U, Esposito EX, Yang...
How Do They Work? PCSK9 inhibitors are proteins made in a laboratory. They target other proteins in your body, specifically your liver. Your liver cells have receptors that sweep away excess cholesterol. But another protein called PCSK9 destroys them. That’s where inhibitors come in. They lat...
Multiprotein site within cells that mechanically interact the extracellular matrix (cell outside) with the actin cytoskeleton (cell inside). Gene transcription Process of copying a segment of DNA sequence into an RNA molecule. This process can be divided in three steps: initiation, elongation and ...