E3 ubiquitin ligase
E3 ubiquitin ligase (A ubiquitin ligase ) is a protein that recruits an E2 ubiquitin-conjugating enzyme that has been loaded with ubiquitin, recognizes a protein substrate, and assists or directly catalyzes the transfer of ubiquitin from the E2 to the protein substrate. The ubiquitin is attached to a lysine on the target protein by an isopeptide bond. E3 ligases interact with both the target protein and the E2 enzyme, and so impart substrate specificity to the E2. Commonly, E3s polyubiquitinate their substrate with Lys48-linked chains of ubiquitin, targeting the substrate for destruction by the proteasome. However, many other types of linkages are possible and alter a protein's activity, interactions, or localization. Ubiquitination by E3 ligases regulates diverse areas such as cell trafficking, DNA repair, and signaling and is of profound importance in cell biology. E3 ligases are also key players in cell cycle control, mediating the degradation of cyclins, as well as cyclin dependent kinase inhibitor proteins.
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Dianicline是选择性 α4β2 nAChR 部分激动剂。
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Desformylflustrabromine hydrochloride是α4β2的阳性变构的调节剂（positive allosteric modulator）, 也是muscle-type nAChR的抑制剂。
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Chlorisondamine diiodide是Nicotinic 拮抗剂。
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CC4
EI0704
CC4是高亲和性，具有亚型选择性的α6β2和α4β2部分激动剂。
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bPiDDB是Orthosteric nAChR 拮抗剂。
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