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.
BMN 673是一种新型的PARP抑制剂,IC50为0.58 nM,也有效抑制PARP-2,但不抑制PARG,对PTEN突变型高度敏感。
MoreSNX-2112选择性结合到HSP90α和HSP90β的ATP结合袋中,Ka分别为30 nM和30 nM,比17-AAG更有效。
MoreBIIB021是口服活性的HSP90抑制剂,Ki和EC50分别为1.7 nM和38 nM。
MoreTopiramate 是镇痉化合物,能拮抗GluR5受体,还可作为GABA受体介导的电流阳性变构调节剂。
MoreSunitinib 是多靶点RTK抑制剂,对VEGFR2(Flk-1)和PDGFRβ的IC50分别为80nM和2nM。
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