E2 enzymes
E2 enzymes (Ubiquitin-conjugating enzymes) perform the second step in the ubiquitination reaction that targets a protein for degradation via the proteasome.The ubiquitination process covalently attaches ubiquitin, a short protein of 76 amino acids, to a lysine residue on the target protein. Once a protein has been tagged with one ubiquitin molecule, additional rounds of ubiquitination form a polyubiquitin chain that is recognized by the proteasome's 19S regulatory particle, triggering the ATP-dependent unfolding of the target protein that allows passage into the proteasome's 20S core particle, where proteases degrade the target into short peptide fragments for recycling by the cell.
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Amfebutamone HCl是一种选择性去甲肾上腺素-多巴胺再摄取的抑制剂,IC50分别为6.5和3.4μM。
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Fluconazole是抗真菌化合物,可用于表面和全身性的真菌感染。
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Zolmitriptan (佐米曲普坦) 是五羟色胺受体1B和1D亚型激动剂。
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SB742457是5-HT6受体拮抗剂,pKi为9.63,比对其它受体的抑制性高100倍以上。
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PF-4981517是一种有效的,选择性的CYP3A4(P450)抑制剂,IC50为0.03 μM,比作用于CYP3A5和CYP3A7选择性高500倍以上。
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