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Regulation of AMPK Activity by CRBN Is Independent of the Thalidomide-CRL4CRBN Protein Degradation Axis

التفاصيل البيبلوغرافية
العنوان: Regulation of AMPK Activity by CRBN Is Independent of the Thalidomide-CRL4CRBN Protein Degradation Axis
المؤلفون: Seung-Joo Yang, Seungje Jeon, Jeong Won Baek, Kwang Min Lee, Chul-Seung Park
المصدر: Pharmaceuticals, Vol 14, Iss 6, p 512 (2021)
بيانات النشر: MDPI AG, 2021.
سنة النشر: 2021
المجموعة: LCC:Medicine
LCC:Pharmacy and materia medica
مصطلحات موضوعية: thalidomide, AMP-activated protein kinase, cereblon, Medicine, Pharmacy and materia medica, RS1-441
الوصف: Cereblon (CRBN), a primary target of immune-modulatory imide drugs (IMiDs), functions as a substrate receptor in the CUL4-RBX1-DDB1-CRBN (known as CRL4CRBN) E3 ubiquitin ligase complex. Binding of IMiDs to CRBN redirects the CRL4CRBN E3 ubiquitin ligase to recruit or displace its substrates. Interaction between CRBN and the AMPK α subunit leads to CRL4CRBN-dependent degradation of the γ subunit and inhibits AMPK activity. However, the effect of thalidomide on the function of CRBN as a negative regulator of AMPK through interaction with the α subunit remains unclear. Here, we show that thalidomide does not affect AMPK activation or the binding affinity between CRBN and the AMPK α subunit. Thalidomide had no effect on AMPK activity independent of CRBN expression. The N-terminal region and C-terminal tail of CRBN, which is distinct from the IMiD binding site, were critical for interaction with the AMPK α subunit. The present results suggest that CRL4CRBN negatively regulates AMPK through a pathway independent from the CRBN-IMiD binding region.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1424-8247
Relation: https://www.mdpi.com/1424-8247/14/6/512; https://doaj.org/toc/1424-8247
DOI: 10.3390/ph14060512
URL الوصول: https://doaj.org/article/65432da45f4f47aebf32dc40c21a4792
رقم الأكسشن: edsdoj.65432da45f4f47aebf32dc40c21a4792
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14248247
DOI:10.3390/ph14060512