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Signal Pathway


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.

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    Avagacestat是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。

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  • TMP269 EY1073

    TMP269是IIa型HDAC选择性抑制剂，对于HDAC4、5、7、9的IC50分别为126、80、36、9nM。相对于1型HDAC有20-400倍的选择性。

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    PH-797804是一种新型吡啶酮抑制剂，作用于p38α，IC50为26 nM；比作用于p38β选择性高4倍以上，不抑制JNK2。

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  • Luminespib EY1021

    AUY922 (NVP-AUY922)是高活性HSP90α和β抑制剂，IC50为13 nM和21 nM，对GRP94和 TRAP-1的活性较低。

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  • RG2833 EY1030

    RG2833(RGFP109)是可通过血脑屏障的HDAC抑制剂，对HDAC1和HDAC3的IC50分别为60nM和50nM。

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