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.
LAQ824 (Dacinostat)是新型HDAC抑制剂,IC50为32 nM,且激活p21启动子。
MoreTelbivudine 是一种抗病毒药,用于治疗乙型肝炎感染。
MoreSolifenacin Succinate (琥珀酸索利那新; YM905; Vesicare) 是毒蕈碱受体拮抗剂。
MoreNifuroxazide是一种可渗透细胞的,口服有效的硝基呋喃类止泻药,有效地抑制细胞内STAT1/3/5转录活性的激活,IC50为3 µM。
MorePCI-24781是一种新型的pan-HDAC抑制剂,靶向作用于HDAC1,Ki为7 nM,对HDACs 2, 3, 6,和10有适中的抑制性,但比作用于HDAC8选择性强40倍。
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