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Published on: June 30, 2022
SPOP point mutations regulate substrate preference and affect its function
Yanran Deng1,2, Wenhao Ding3, Kaize Ma3
1Jiangsu Key laboratory of Drug Screening, China Pharmaceutical University, 210009, Nanjing, China.
Abstract:
The adaptor SPOP recruits substrates to CUL3 E3 ligase for ubiquitination and degradation. Structurally, SPOP harbors a MATH domain for substrate recognition, and a BTB domain responsible for binding CUL3. Reported point mutations always occur in SPOP's MATH domain and are through to disrupt affinities of SPOP to substrates, thereby leading to tumorigenesis. In this study, we identify the tumor suppressor IRF2BP2 as a novel substrate of SPOP. SPOP enables to attenuate IRF2BP2-inhibited cell proliferation and metastasis in HCC cells. However, overexpression of wild-type SPOP alone suppresses HCC cell proliferation and metastasis. In addition, a HCC-derived mutant, SPOP-M35L, shows an increased affinity to IRF2BP2 in comparison with wild-type SPOP. SPOP-M35L promotes HCC cell proliferation and metastasis, suggesting that M35L mutation possibly reprograms SPOP from a tumor suppressor to an oncoprotein. Taken together, this study uncovers mutations in SPOP's MATH lead to distinct functional consequences in context-dependent manners, rather than simply disrupting its interactions with substrates, raising a noteworthy concern that we should be prudent to select SPOP as therapeutic target for cancers.
Insights
The study identifies IRF2BP2 as a substrate of SPOP, a protein involved in cancer. Mutations in SPOP can paradoxically promote cancer by altering its interaction with IRF2BP2.
Area of Science:
- Molecular Biology
- Oncology
- Biochemistry
Background:
- The SPOP protein acts as an adaptor, recruiting substrates to the CUL3 E3 ligase for ubiquitination and degradation.
- SPOP possesses a MATH domain for substrate recognition and a BTB domain for CUL3 binding.
- Mutations in SPOP's MATH domain are linked to tumorigenesis, potentially by disrupting substrate interactions.
Purpose of the Study:
- To identify novel substrates of SPOP and investigate the functional consequences of SPOP mutations in hepatocellular carcinoma (HCC).
- To explore the role of SPOP and its mutant forms in regulating cell proliferation and metastasis in HCC.
Main Methods:
- Identification of IRF2BP2 as a novel substrate of SPOP.
- Analysis of SPOP's role in attenuating IRF2BP2-mediated effects in HCC cells.
- Characterization of a HCC-derived SPOP mutant (SPOP-M35L) and its affinity for IRF2BP2.
Main Results:
- SPOP suppresses HCC cell proliferation and metastasis by targeting IRF2BP2.
- Overexpression of wild-type SPOP inhibits HCC cell proliferation and metastasis.
- The SPOP-M35L mutant exhibits increased affinity for IRF2BP2 and promotes HCC cell proliferation and metastasis, suggesting a switch from tumor suppressor to oncoprotein.
Conclusions:
- Mutations in SPOP's MATH domain have context-dependent functional consequences beyond simple disruption of substrate interactions.
- The SPOP-M35L mutation may reprogram SPOP's function, promoting tumorigenesis in HCC.
- Caution is advised when considering SPOP as a therapeutic target for cancers due to the complex and context-dependent effects of its mutations.
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