The therapeutic effect of a novel GAPDH inhibitor in mouse model of breast cancer and efficacy monitoring by molecular imaging
文献类型：期刊论文
| 作者 | Zhang, Yun-Qi3,4; Zhang, Wei1,2; Kong, Xiang-Tai1,2; Hai, Wang-Xi3,4; Guo, Rui3,4; Zhang, Min3,4; Zhang, Su-Lin1,2; Li, Biao3,4 |
| 刊名 | CANCER CELL INTERNATIONAL
 |
| 出版日期 | 2024-05-29 |
| 卷号 | 24期号:1页码:13 |
| 关键词 | Glyceraldehyde-3-phosphate dehydrogenase Inhibitor Breast cancer Warburg effect Positron emission tomography/computed tomography |
| DOI | 10.1186/s12935-024-03361-x |
| 通讯作者 | Zhang, Su-Lin(slzhang@simm.ac.cn) ; Li, Biao(lb10363@rjh.com.cn) |
| 英文摘要 | Background Breast cancer is a serious threat to women's health with high morbidity and mortality. The development of more effective therapies for the treatment of breast cancer is strongly warranted. Growing evidence suggests that targeting glucose metabolism may be a promising cancer treatment strategy. We previously identified a new glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor, DC-5163, which shows great potential in inhibiting tumor growth. Here, we evaluated the anticancer potential of DC-5163 in breast cancer cells.Methods The effects of DC-5163 on breast cancer cells were investigated in vitro and in vivo. Seahorse, glucose uptake, lactate production, and cellular ATP content assays were performed to examine the impact of DC-5163 on cellular glycolysis. Cell viability, colony-forming ability, cell cycle, and apoptosis were assessed by CCK8 assay, colony formation assay, flow cytometry, and immunoblotting respectively. The anticancer activity of DC-5163 in vivo was evaluated in a mouse breast cancer xenograft model.Results DC-5163 suppressed aerobic glycolysis and reduced energy supply of breast cancer cells, thereby inhibiting breast cancer cell growth, inducing cell cycle arrest in the G0/G1 phase, and increasing apoptosis. The therapeutic efficacy was assessed using a breast cancer xenograft mouse model. DC-5163 treatment markedly suppressed tumor growth in vivo without inducing evident systemic toxicity. Micro-PET/CT scans revealed a notable reduction in tumor 18F-FDG and 18F-FLT uptake in the DC-5163 treatment group compared to the DMSO control group.Conclusions Our results suggest that DC-5163 is a promising GAPDH inhibitor for suppressing breast cancer growth without obvious side effects. 18F-FDG and 18F-FLT PET/CT can noninvasively assess the levels of glycolysis and proliferation in tumors following treatment with DC-5163. |
| WOS关键词 | FDG-PET ; GLYCOLYSIS ; APOPTOSIS ; PATIENT ; CELLS |
| 资助项目 | Natural Science Foundation of Shanghai Municipality |
| WOS研究方向 | Oncology |
| 语种 | 英语 |
| WOS记录号 | WOS:001235332200002 |
| 出版者 | BMC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/311758]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhang, Su-Lin; Li, Biao |
| 作者单位 | 1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Canter, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 3.Shanxi Med Univ, Collaborat Innovat Ctr Mol Imaging Precis Med, Taiyuan 030000, Peoples R China 4.Shanghai Jiao Tong Univ, Sch Med, Ruijin Hosp, Dept Nucl Med, 197 Ruijin Second Rd, Shanghai 200025, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Yun-Qi,Zhang, Wei,Kong, Xiang-Tai,et al. The therapeutic effect of a novel GAPDH inhibitor in mouse model of breast cancer and efficacy monitoring by molecular imaging[J]. CANCER CELL INTERNATIONAL,2024,24(1):13. |
| APA | Zhang, Yun-Qi.,Zhang, Wei.,Kong, Xiang-Tai.,Hai, Wang-Xi.,Guo, Rui.,...&Li, Biao.(2024).The therapeutic effect of a novel GAPDH inhibitor in mouse model of breast cancer and efficacy monitoring by molecular imaging.CANCER CELL INTERNATIONAL,24(1),13. |
| MLA | Zhang, Yun-Qi,et al."The therapeutic effect of a novel GAPDH inhibitor in mouse model of breast cancer and efficacy monitoring by molecular imaging".CANCER CELL INTERNATIONAL 24.1(2024):13. |
入库方式： OAI收割
来源：上海药物研究所
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