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Development of a novel peptide targeting GPR81 to suppress adipocyte-mediated tumor progression
Shaomeng Chen1, Xiuman Zhou1, Wanqiong Li1
1School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, No. 66, Gongchang Road, Shenzhen 518107, PR China.
Abstract:
GPR81, initially discovered in adipocytes, has been found to suppress lipolysis when activated. However, the current small molecules that target GPR81 carry the risk of off-target effects, and their impact on tumor progression remains uncertain. Here, we utilized phage display technology to screen a GPR81-targeting peptide named 7w-2 and proceeded to demonstrate its bioactivity. Although 7w-2 did not affect the proliferation of tumor cells, it effectively reduced adipocyte catabolism in vitro, consequently restraining the proliferation of co-cultured tumor cells. Furthermore, our findings revealed that 7w-2 could inhibit lipolysis in vivo, leading to a significant impediment in tumor growth and metastasis in the 4T1 murine tumor model. Additionally, 7w-2 exhibited the ability to significantly elevate the proportion and functionality of CD8+ T cells. Our study introduces 7w-2 as the first peptide targeting GPR81, shedding light on its potential role in adipocytes in suppressing tumor progression.
Insights
Researchers discovered a new peptide, 7w-2, that targets GPR81. This peptide inhibits fat breakdown in adipocytes, thereby restraining tumor growth and metastasis in mice.
Area of Science:
- Biochemistry
- Immunology
- Oncology
Background:
- G protein-coupled receptor 81 (GPR81) suppresses lipolysis in adipocytes.
- Existing small molecules targeting GPR81 have off-target effects and uncertain impacts on tumor progression.
- The role of adipocyte GPR81 in tumor progression requires further investigation.
Purpose of the Study:
- To identify and characterize a novel GPR81-targeting peptide.
- To evaluate the peptide's efficacy in modulating adipocyte function and tumor growth.
- To explore the peptide's impact on the tumor microenvironment and immune response.
Main Methods:
- Phage display technology was used to screen for GPR81-targeting peptides.
- The bioactivity of the identified peptide, 7w-2, was assessed in vitro and in vivo.
- Tumor cell proliferation, adipocyte catabolism, lipolysis, tumor growth, metastasis, and CD8+ T cell function were evaluated.
Main Results:
- Peptide 7w-2 effectively reduced adipocyte catabolism in vitro, restraining co-cultured tumor cell proliferation.
- In vivo, 7w-2 inhibited lipolysis, significantly impeding tumor growth and metastasis in the 4T1 murine model.
- 7w-2 enhanced the proportion and functionality of CD8+ T cells.
Conclusions:
- 7w-2 is the first identified peptide targeting GPR81.
- GPR81 in adipocytes plays a role in suppressing tumor progression.
- 7w-2 demonstrates potential as a therapeutic agent for cancer treatment by targeting adipocyte metabolism and enhancing anti-tumor immunity.
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