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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A natural analog of resveratrol and an inhibitor of CYP1A1.
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Aripiprazole是一种人5-HT1A受体激动剂,Ki为4.2 nM。
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Palonosetron是5-HT3拮抗剂,能抑制化疗引起的恶心呕吐(CINV)。
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Desvenlafaxine是5-羟色胺(5-HT)和去甲肾上腺素(NE)重吸收抑制剂,Ki为40.2 nM和558.4 nM。
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Iloperidone是D2/5-HT2受体拮抗剂,可作用于精神分裂症。
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