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.
Sodium Butyrate (丁酸钠) 被报道证实为HDAC抑制剂,从而导致组蛋白过乙酰化。
MoreAZD4547是一种新型选择性的FGFR抑制剂,靶向作用于FGFR1/2/3,IC50为0.2 nM/2.5 nM/1.8 nM,对FGFR4, VEGFR2(KDR)具有微弱的作用活性,但对IGFR, CDK2和p38几乎没有作用活性。
MoreLovastatin (洛伐他汀) 是高效HMG-CoA还原酶抑制剂,IC50为3.4 nM,有降血脂作用。
MoreDAPT (GSI-IX)是新型γ-分泌酶抑制剂,抑制HEK 293细胞中全部Aβ, IC50为20 nM。
MoreSB525334是一种有效的,选择性的TGFβ receptor I (ALK5)抑制剂,IC50为14.3 nM,作用于ALK4比作用于ALK5效果低4倍,可抑制ALK2, 3,和6活性。
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