Degrading proteins in animals: “PROTAC”tion goes in vivo
2019年2月15日 · In a recent paper in Cell Discovery, Sun et al. have systematically investigated the potential usage of PROTACs in mice and large animals, such as pigs and rhesus monkeys.
Ligand-mediated protein degradation reveals functional conservation ...
2018年4月20日 · Upon binding to thalidomide and other immunomodulatory drugs, the E3 ligase substrate receptor cereblon (CRBN) promotes proteosomal destruction by engaging the …
Current advances and development strategies of orally …
2023年12月5日 · The CRBN-based PROTACs elicited several superiorities over VHL-based in the orally bioavailable PROTACs community. Many potential novel mechanisms were proposed …
Upon binding to thalidomide and other immunomodulatory drugs, the E3 ligase substrate receptor cereblon (CRBN) promotes proteosomal destruction by engaging the DDB1-CUL4A-Roc1 …
Cereblon: A Protein Crucial to the Multiple Functions of ...
CRBN helps the E3 ubiquitin ligase complex target ion channels for ubiquitination and therefore maintains the ion balance and reduces the incidence of ion channel disease. CRBN is a …
Developments of CRBN-based PROTACs as potential therapeutic agents
2021年12月5日 · A variety of small-molecule PROTACs (CRBN, VHL, IAPs, MDM2, DCAF15, DCAF16, and RNF114-based PROTACs) have been identified so far. In particular, CRBN …
CRBN配体的作用和最新进展 - 知乎 - 知乎专栏
它们被称为cereblon（CRBN）E3连接酶调节剂（CELMoD）或者免疫调节药物（IMiDs），与CRBN结合，CRBN与 DDB1 (damaged DNA binding protein 1)、Cul4A (Cullin 4A)、ROC1 …
The interacting domains in cereblon differentially modulate the ...
2018年12月9日 · Cereblon (CRBN), a substrate receptor of the cullin-4 RING E3 ligase (CRL4), has been utilized for the targeted protein degradation via small molecular weight CRBN …
Science | 靶向蛋白降解途径突破，几乎可用于任何疾病相关蛋白
2022年11月22日 · CELMoDs被设计成以一种新的方式攻击癌症，通过与一种称为cereblon的调节蛋白结合，从而触发关键癌症驱动蛋白的降解。 Scripps团队发现，这些药物为了发挥作用， …
Cereblon gene and protein conservation across different …
CRBN serves as a substrate receptor of the Cullin-Ring ligase 4 E3 ubiquitin ligase complex (CRL4 CRBN ), which recognizes substrates for ubiquitination and proteasomal degradation [79].