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Updated: Feb 15, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Cereblon (CRBN) deletion reverses streptozotocin induced diabetic osteoporosis in mice
Cong Yao1, Xiong Guo2, Wan-Xia Yao3
1Department of Plastic Surgery, The Second Affiliated Hospital of Xi'an Jiao Tong University, Xi'an, 710004, China.
Abstract:
Diabetes mellitus is a major cause to induce osteoporosis. Though the pathogenesis of osteoporosis progression has been well investigated, its still not fully understood. Recently, cereblon (CRBN) was considered as a negative modulator of adenosine monophosphate-activated protein kinase (AMPK) in vitro and in vivo. Here, we presented results indicating that CRBN could effectively regulate osteoporosis development. In STZ-induced wild type (WT) mice with diabetes, the osteoclasts were highly increased along with the deterioration of bone structure. However, CRBN knockout (KO) reduced blood glucose the levels and attenuated insulin resistance. What's more, CRBN ablation suppressed osteoclast differentiation and rescued diabetic bone loss in vivo, accompanied with decreased receptor activator of NF-kB ligand (RANKL), RANKL/osteoprotegerin (OPG), and tartrate-resistant acid phosphatase (TRAP) levels, as well as improved AMP-activated kinase (AMPK) α/acetyl-CoA carboxylase (ACC)αactivation. In vitro, suppressing CRBN expression could reduce RANKL-induced osteoclastogenesis, supported by the reduction of TRAP-positive cells. CRBN knockdown (KD) obviously reduced RANKL-induced activity of IκBα/nuclear factor-κB (NF-κB) pathway. In addition, osteoclast-specific genes expression levels stimulated by RANKL were also decreased by CRBN silence. More importantly, CRBN blockage increased phosphorylated AMPK-α and ACC-α expressions in RANKL-incubated cells. However, these processes could be abolished by suppressing AMPK-α with its inhibitor, Compound C. Collectively, our data suggested that CRBN is a potential treatment option against diabetes-induced osteolytic bone disease.
Insights
Cereblon (CRBN) regulates osteoporosis in diabetes. CRBN knockout improves glucose levels and bone loss by suppressing osteoclast formation and activating AMPK signaling pathways.
Area of Science:
- Endocrinology
- Bone Biology
- Molecular Biology
Background:
- Diabetes mellitus is a significant risk factor for osteoporosis.
- The precise mechanisms linking diabetes to bone loss are not fully elucidated.
- Cereblon (CRBN) has emerged as a potential regulator of metabolic and cellular processes.
Purpose of the Study:
- To investigate the role of Cereblon (CRBN) in the development of diabetes-induced osteoporosis.
- To explore the molecular mechanisms by which CRBN influences osteoclast differentiation and bone metabolism in diabetes.
Main Methods:
- Utilized STZ-induced diabetic wild-type and CRBN knockout mice models.
- Performed in vitro studies involving osteoclast differentiation assays with CRBN knockdown.
- Analyzed key signaling pathways including AMPK/ACC and NF-κB, along with relevant molecular markers (RANKL, OPG, TRAP).
Main Results:
- CRBN knockout in diabetic mice reduced blood glucose, attenuated insulin resistance, and preserved bone structure.
- CRBN ablation suppressed osteoclast differentiation and rescued diabetic bone loss by decreasing RANKL/OPG and increasing AMPK/ACC activation.
- In vitro, CRBN knockdown inhibited RANKL-induced osteoclastogenesis and NF-κB pathway activation, while enhancing AMPK signaling.
Conclusions:
- Cereblon (CRBN) plays a critical role in regulating osteoclast differentiation and bone metabolism in the context of diabetes.
- CRBN inhibition emerges as a promising therapeutic strategy for treating diabetes-induced osteolytic bone disease.
- Targeting CRBN may offer a novel approach to manage osteoporosis associated with diabetes mellitus.
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