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Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Cereblon (CRBN) inhibits prostate cancer metastasis by negatively regulating 6-phosphogluconate dehydrogenase (6PGD)
Koushik Guchhait1, Hyeon-Seung Yoon1, Hyun-Su An1
1Department of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju, Korea.
Abstract:
Metastasis is the primary cause of mortality in advanced prostate cancer, and the emergence of resistance to androgen receptor (AR)-targeted therapies highlights the urgent need for alternative therapeutic strategies. Metabolic reprogramming has increasingly been recognized as a key driver of metastatic progression. In this study, we uncover a novel tumor-suppressive role for cereblon (CRBN), a substrate receptor of the CRL4CRBN E3 ubiquitin ligase complex, in modulating prostate cancer metastasis through regulation of 6-phosphogluconate dehydrogenase (6PGD), a critical enzyme in the oxidative pentose phosphate pathway (oxPPP). CRBN directly binds a conserved C-terminal α-helix in 6PGD, promoting its polyubiquitination and proteasomal degradation independently of immunomodulatory drugs (IMiDs). Genetic or pharmacological loss of CRBN via CRISPR/Cas9, RNA interference, or PROTAC-mediated degradation stabilized 6PGD and elevated the NADPH/NADP+ ratio. Conversely, re-expression of wild-type CRBN reduced 6PGD levels, restored NADPH/NADP+ ratio, and suppressed cell migration and invasion. Transcriptomic profiling revealed CRBN-induced upregulation of CDH1 and downregulation of the EMT marker MMP1, while CRBN degradation produced the opposite pattern-both effects were reversed by 6PGD inhibition. These regulatory effects were conserved across multiple cancer cell lines and observed in CRBN-deficient mouse tissues. Functional studies using intra-splenic xenograft models further demonstrated that CRBN suppresses metastatic dissemination. Collectively, our findings identify 6PGD as a novel endogenous substrate of CRBN and establish the CRBN-6PGD axis as a critical metabolic checkpoint in prostate cancer metastasis. Therapeutic targeting of this pathway may offer promising strategies for CRBN-deficient or 6PGD-driven cancers.
Insights
Cereblon (CRBN) suppresses prostate cancer metastasis by degrading 6-phosphogluconate dehydrogenase (6PGD). This CRBN-6PGD pathway is a key metabolic checkpoint, offering new therapeutic targets for advanced prostate cancer.
Area of Science:
- Oncology
- Molecular Biology
- Metabolism
Background:
- Metastasis drives prostate cancer mortality, necessitating new therapies beyond AR-targeted treatments.
- Metabolic reprogramming is a key factor in metastatic progression.
- Cereblon (CRBN) is a substrate receptor in the CRL4 E3 ubiquitin ligase complex.
Purpose of the Study:
- To investigate the role of CRBN in prostate cancer metastasis.
- To identify novel substrates and regulatory mechanisms of CRBN in cancer.
- To explore the CRBN-6PGD axis as a potential therapeutic target.
Main Methods:
- CRISPR/Cas9 and RNA interference for genetic manipulation of CRBN.
- PROTAC-mediated degradation to assess CRBN function.
- Biochemical assays to determine CRBN-6PGD binding and ubiquitination.
- Measurement of NADPH/NADP+ ratio.
- Transcriptomic profiling (RNA-seq).
- In vitro cell migration and invasion assays.
- In vivo intra-splenic xenograft models.
Main Results:
- CRBN directly binds and promotes the degradation of 6-phosphogluconate dehydrogenase (6PGD), independent of IMiDs.
- Loss of CRBN stabilizes 6PGD, increases the NADPH/NADP+ ratio, and promotes cell migration and invasion.
- CRBN re-expression reverses these effects, suppressing metastasis.
- CRBN regulates EMT markers (CDH1, MMP1) via 6PGD.
- These findings were conserved across cell lines and in mouse models.
Conclusions:
- CRBN acts as a tumor suppressor in prostate cancer metastasis by targeting 6PGD for degradation.
- The CRBN-6PGD interaction represents a novel metabolic checkpoint in cancer progression.
- Targeting the CRBN-6PGD pathway offers a promising therapeutic strategy for CRBN-deficient or 6PGD-driven cancers.
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