Home
Resources
Publications
Inhibition of LIPG Phospholipase Activity Suppresses Tumor Formation of Human Basal-Like Triple-Negative Breast Cancer

Inhibition of LIPG Phospholipase Activity Suppresses Tumor Formation of Human Basal-Like Triple-Negative Breast Cancer

Pang-Kuo Lo, Yuan Yao, Qun Zhou

Sci Rep. 2020 Jun 2;10(1):8911.

PMID: 32488004

Abstract:

The endothelial lipase LIPG possesses serine phospholipase activity and is involved in lipoprotein metabolism. Our previous studies have revealed that LIPG overexpression is required for tumor formation and metastasis of human basal-like triple-negative breast cancer (TNBC). We also demonstrated that LIPG differentially regulates TNBC malignancy through its enzymatic and non-enzymatic functions. The present studies were aimed at determining how XEN445, a specific inhibitor targeting LIPG phospholipase activity, impacts on TNBC tumor formation and malignant features. We established a cell-based LIPG enzymatic assay system to measure the inhibitory effect of XEN445 on LIPG phospholipase activity and determine its IC50. We found that XEN445 preferentially inhibited the proliferation of LIPG-expressing TNBC cells but not LIPG-negative luminal breast cancer cells. XEN445 inhibited the self-renewal of cancer stem cells (CSCs) in vitro and TNBC tumor formation in vivo. However, XEN445 had no inhibitory effect on the invasiveness and CSC stemness of TNBC cells. Our studies suggest that targeting both LIPG enzymatic and non-enzymatic functions is an important strategy for the treatment of TNBC.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1515856924	XEN445		1515856-92-4	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: