The addition of ubiquitin to a substrate protein is called ubiquitination or ubiquitylation. Ubiquitination can affect proteins in many ways: it can signal for their degradation via the proteasome, alter their cellular location, affect their activity, and promote or prevent protein interactions. Ubiquitination is carried out in three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Multi-monoubiquitination can mark transmembrane proteins for removal from membranes and fulfil several signalling roles within the cell.
INT-747是FXR高效选择性激动剂,EC50值为99 nM。
MoreFenofibrate是PPARα激动剂,对小鼠和人的PPARα的EC50分别为18 μM和30 μM。
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。
MoreXL335是一种有效的,选择性的FXR激动剂,EC50为4 nM,高选择性作用于其他核受体,如LXR, PPAR, ER等。
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