Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry...

Area of Science:

• Cell Biology
• Cancer Research
• Pharmacology

Background:

• Monopolar spindle 1 (Mps1) is a dual-specificity protein kinase essential for kinetochore localization and the spindle assembly checkpoint (SAC).
• Cancer cells exhibit chromosomal instability due to cell cycle checkpoint dysfunction, with Mps1 overexpression being a common adaptation.
• Mps1's role in cancer makes it a significant therapeutic target for novel anti-cancer drug development.

Purpose of the Study:

• To review Mps1 inhibitors developed over the last decade.
• To highlight their potential in treating advanced cancers, particularly triple-negative breast cancer (TNBC).
• To provide a reference for future exploration of Mps1 inhibitors.

Main Methods:

• Literature review of Mps1 inhibitors.
• Analysis of Mps1 overexpression in various cancer types.
• Discussion of clinical trial progress for Mps1-targeting compounds.

Main Results:

• Mps1 is frequently overexpressed in cancers, contributing to chromosomal instability.
• Several Mps1 inhibitors have been developed and advanced to clinical trials.
• These inhibitors show promise for treating advanced non-haematologic malignancies, including TNBC.

Conclusions:

• Mps1 is a validated therapeutic target in oncology.
• Targeting Mps1 represents a viable strategy for cancer treatment.
• Continued research into Mps1 inhibitors may yield more effective cancer therapies.