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.
Pracinostat是广泛的HDAC抑制剂,对HDAC1,3,4,5,9,和10的IC50分别是49 nM,43 nM,56 nM,47 nM,70 nM和40 nM。
MoreWHI-P154是JAK3抑制剂,IC50为1.8 μM,还能抑制EGFR,Src,Abl,VEGFR和MAPK,对JAK1和JAK2无活性。
MoreParthenolide(PTL)能诱导癌细胞凋亡,并杀灭癌症干细胞,还能特异地抑制HDAC1活性而不影响别的I/II类HDAC。
MoreTrilostane (曲洛司坦; Win 24540; Modrastane) 是3 β-羟化类固醇脱氢酶抑制剂,可作用于库兴氏综合症。
MoreCH5138303 是一种口服有效的Hsp90抑制剂,其Kd为 0.48 nM。
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