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.
Miltefosine作用于癌细胞系A431和HeLa,抑制PI3K/Akt活性,ED50分别为17.2 μM和8.1 μM,是第一个用于治疗内脏利什曼病的口服药物,有效对抗前鞭毛体和无鞭毛体。
MoreDipyridamole是磷酸二酯酶抑制剂,能阻断红细胞和血管内皮细胞对腺苷的吸收和代谢。
MoreGSK923295是首创的,特异的CENP-E驱动蛋白ATPase变构抑制剂,Ki为3.2 nM,对突变型I182和T183抑制活性较低。
MoreLFM-A13是Btk激酶选择性抑制剂,IC50值为17.2uM,也对PLK3有抑制作用。
MoreAtazanavir sulfate (硫酸阿扎那韦) 是HIV-1蛋白酶高活性抑制剂。
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