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N/C-degron pathways and inhibitor development for PROTAC applications

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成果类型:
期刊论文
作者:
Wu, Zhibin;Huang, Yunyuan;Liu, Ke*;Min, Jinrong
通讯作者:
Liu, Ke;Min, JR
作者机构:
[Liu, Ke; Wu, Zhibin; Min, Jinrong; Huang, Yunyuan] Cent China Normal Univ, Sch Life Sci, Hubei Key Lab Genet Regulat & Integrat Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Liu, K; Min, JR ] C
Cent China Normal Univ, Sch Life Sci, Hubei Key Lab Genet Regulat & Integrat Biol, Wuhan 430079, Peoples R China.
语种:
英文
关键词:
Degron;E3 ubiquitin ligase;Proteolysis-targeting chimera (PROTAC);Ubiquitination
期刊:
BIOCHIMICA ET BIOPHYSICA ACTA-GENE REGULATORY MECHANISMS
ISSN:
1874-9399
年:
2024
卷:
1867
期:
1
页码:
194952
基金类别:
In 2018, several C-terminal degradation signals were identified in human proteins, which can be recognized by the CRL E3 ligases as well as other E3s (Fig. 4) [62,63]. The Gly/C-degron was recognized by the Kelch-repeat domain-containing component of the CRL2 complexes, such as KLHDC2 [64], KLHDC3 [65], and KLHDC10 [66], and each recognin recognizes a distinct sequence motif. KLHDC2 prefers the C-end motif of -GG, KLHDC3 recognizes the −R/KG C-end motif and KLHDC10 targets the −A/W/PG C-end
机构署名:
本校为第一且通讯机构
院系归属:
生命科学学院
摘要:
Ubiquitination is a fascinating post-translational modification that has received continuous attention since its discovery. In this review, we first provide a concise overview of the E3 ubiquitin ligases, delving into classification, characteristics and mechanisms of ubiquitination. We then specifically examine the ubiquitination pathways mediated by the N/C-degrons, discussing their unique features and substrate recognition mechanisms. Finally, we offer insights into the current state of development pertaining to inhibitors that target the N/C-degron pathways, as well as the promising advance...

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