1. Signaling Pathways
  2. PROTAC
  3. Ligands for E3 Ligase

Ligands for E3 Ligase ( E3泛素连接酶配体)

E3 ligase-recruiting Moiety

PROTAC(Proteolysis Targeting Chimeric Molecule,蛋白水解靶向嵌合分子)是由E3连接酶的配体(E3连接酶结合体)、连接子和靶蛋白的配体(靶蛋白结合体)组成的蛋白降解剂。PROTAC诱导E3连接酶与靶蛋白结合,导致泛素转移,靶蛋白降解。

E3连接酶催化泛素向靶蛋白的转移,决定蛋白的特异性。细胞中有数百种E3连接酶,但目前报道的PROTAC中成功应用的E3连接酶只有少数几种,如VHL(von Hippel-Lindau病肿瘤抑制蛋白)、CRBN(Cereblon)、MDM2(小鼠双微分2同源物)和IAP(凋亡抑制剂)。

A PROTAC (Proteolysis Targeting Chimeric Molecule) is a protein degrader comprised of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand for target protein (target binder). The association between an E3 ligase and a target protein induced by a PROTAC will lead to the transfer of ubiquitin and degradation of the targeted protein.

E3 ligases catalyze the transfer of ubiquitin to targeted proteins and determine the specificity of the proteins. There are hundreds of E3 ligases in cells, but only a limited number of them are successfully used in reported PROTACs, such as VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and IAP (inhibitor of apoptosis).

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