Creating and Testing New Drugs to Fight Breast Cancer by Blocking LPA1 Receptors

What is it about?

Breast cancer has been a leading cause of mortality among women worldwide in recent years. Targeting LPA-LPA1 pathway using small molecules could improve breast cancer therapy. Thiazolidin-4-ones were developed and tested on MCF-7 cancer cells, and active compounds were analyzed for their effects on apoptosis, migration, angiogenesis, and LPA1 protein and gene expression. Compounds TZ-4 and TZ-6 effectively reduced the migration of MCF-7 cells and induced apoptosis. TZ-4, TZ-6, TZ-8 and TZ-14 significantly reduced the LPA1 protein, LPA1 and angiogenesis gene expression in treated MCF-7 cells. Molecular docking and MD simulation studies reveal the ligand interactions and stability of the LPA1-ligand complex. Developed thiazolidin-4-ones showed great potential as an LPA1-targeted approach to combating breast cancer.

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Why is it important?

Breast cancer is a major cause of death among women globally. Blocking the LPA-LPA1 pathway with small molecules could enhance breast cancer treatment. Researchers created and tested thiazolidin-4-ones on MCF-7 breast cancer cells, examining their impact on cell death, movement, blood vessel formation, and LPA1 protein and gene expression. Compounds TZ-4 and TZ-6 successfully reduced cancer cell movement and caused cell death. TZ-4, TZ-6, TZ-8, and TZ-14 significantly decreased LPA1 protein levels and gene expression related to LPA1 and blood vessel formation in cancer cells. Molecular studies showed how these compounds interact with and stabilize the LPA1 receptor. The newly developed thiazolidin-4-ones show strong promise as a targeted treatment for breast cancer by inhibiting the LPA1 receptor.

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