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.
Quisinostat (JNJ-26481585)是一种新型的,二代HDAC抑制剂,对HDAC作用最有效,IC50为0.11 nM,适度有效作用于HDACs 2, 4, 10,和11;比作用于HDACs 3, 5, 8,和9选择性强30倍,对HDACs 6和7作用效果最弱。
MoreCI-994 (Tacedinaline)是抗癌化合物,能抑制HDAC1,IC50为0.57 μM,能促使细胞周期停滞于G1期。
MoreURB597是口服生物相容性的FAAH抑制剂,IC50为4.6 nM,对其它的cannabinoid-相关靶点无活性。
MoreAG-1478 (Tyrphostin AG-1478)是一种选择性的EGFR抑制剂,IC50为3 nM,对HER2-Neu, PDGFR, Trk, Bcr-Abl和InsR几乎没有抑制作用。
MoreTrichostatin A (TSA)是一种HDAC抑制剂,IC50为1.8 nM左右,HDAC8是HDAC家族中唯一不受TSA影响的成员。
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