In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.
Artemisinin, a potent antimalarial, can be used to cure multidrug-resistant Plasmodium falciparum infections.
MoreMasitinib, a novel phenylaminothiazole-type derivative, is an inhibitor of the class III receptor tyrosine kinase stem-cell growth factor receptor (c-Kit) with IC50 of 200 nM, platelet-derived growth factor receptor α and β and the non-receptor tyrosine kinase Lyn(PDGFRα/β with IC50 of 540 nM/800 nM).
MoreQuisinostat (JNJ-26481585) is a novel second-generation HDACi inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. , in NSCLC cells. In vitro, quisinostat has shown anti-proliferative activity against NSCLC cell lines. quisinostat extremely changed protein acetylation patterns of A549 cells and inhibited epithelial-mesenchymal transition (EMT) process.
MoreMalotilate is a new drug suggested for use in chronic liver diseases. It is shown here to prevent liver damage caused by CCl4. It has been shown to inhibit 5-1ipoxygenase in human macrophages selectively.
MoreOrteronel (TAK-700) is an inhibitor of the steroidogenic enzyme CYP17A1. It has higher specificity for the 17,20 lyase activity of CYP17A1 with IC50 of 38 nM. Phase III.
More