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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Orteronel (TAK-700) is an inhibitor of the steroidogenic enzyme CYP17A1. It has higher specificity for the 17,20 lyase activity of CYP17A1 with IC50 of 38 nM. Phase III.
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GR 125487 sulfamate是活性选择性 5-HT4 拮抗剂，体内具有活性。
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GR 127935 hydrochloride是活性选择性 5-HT1B/1D 拮抗剂。
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GR 113808是活性选择性 5-HT4 拮抗剂。
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Fluvoxamine maleate是5-HT re-uptake inhibitor（重摄取抑制剂）。
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