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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Itraconazole 是一种三唑类抗真菌药物。
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RS-127445(MT 500)是5-HT2B受体拮抗剂,pKi和pIC50分别为9.5和10.4。
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Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
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Abiraterone是一种有效的类固醇细胞色素P450 17alpha-羟化酶-17, 20-裂解酶(CYP17)抑制剂,IC50为2 nM;对前列腺癌有活性。
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Baicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。
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