1. Signaling Pathways
  2. PROTAC
  3. E3 Ligase Ligand-Linker Conjugates

E3 Ligase Ligand-Linker Conjugates 

E3 连接酶配体-连接子偶联物是蛋白水解靶向嵌合分子(PROTACs)的一部分,它包含一个 E3 泛素连接酶的配体和一个连接子,与靶蛋白的配体(如 JQ1 连接 BRD4 蛋白,Molibresib 连接 BET 蛋白)连接后,可用于构建靶蛋白泛素化降解的 PROTACs。目前,已发现多种PROTAC通过特异性靶向BET、雌激素受体(ER)、雄激素受体等表现出良好的生物活性。MedChemExpress(MCE)提供各种高质量的E3连接酶配体-接头结合物,包括von Hippel-Lindau(VHL)配体、MDM2配体、Cereblon(CRBN)配体和cIAP1配体与不同的接头(PEG、烷基链、烷基/醚等)结合。设计和合成各种新型PROTAC(ARV-825、dBET1、MT-802等)既方便又省时,可以扩大PROTAC在癌症、自身免疫、炎症和其他疾病治疗中的应用。

E3 Ligase Ligand-Linker Conjugate, which is one part of Proteolysis Targeting Chimeric Molecules (PROTACs), incorporates a ligand for the E3 ubiquitin ligase and a linker. After linked to the ligand for target protein (such as JQ1 for BRD4 protein, Molibresib for BET protein), those conjugates can be used for constituting PROTACs that targetprotein for ubiquitination and degradation. Currently, several PROTACs have been found to show good biological activity by specifically targeting BET, estrogen receptor (ER), androgen receptor, etc. MedChemExpress (MCE) offers a wide range of high quality E3 Ligase Ligand-Linker Conjugates including von Hippel-Lindau (VHL) ligands, MDM2 ligands, Cereblon (CRBN) ligands and cIAP1 ligands conjugating with different linkers (PEGs, Alkyl-Chain, Alkyl/ether, etc.). It’s convenient and time-saving for designing and synthesizinga wide variety of novel PROTACs (ARV-825, dBET1,MT-802, etc.), which can expand the application of PROTACs in the treatment of cancer, autoimmunity, inflammation and other diseases.

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