Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical...

Area of Science:

• Molecular Biology
• Pharmacology
• Biochemistry

Background:

• Transforming growth factor-beta (TGF-β) is a key regulator of cellular processes, and its aberrant signaling is implicated in diseases such as fibrosis, cardiovascular disease, and cancer.
• The TGF-β signaling pathway, involving SMAD-dependent and -independent cascades, is a validated drug target due to its role in various pathologies.

Purpose of the Study:

• To review the current research on organic molecules designed as TGF-β signaling pathway inhibitors.
• To focus on the biological functions and binding poses of these inhibitors in different stages of development.

Main Methods:

• Literature review of existing research on TGF-β inhibitors.
• Analysis of organic molecules targeting TGF-β signaling, including those in clinical and preclinical development.

Main Results:

• Overview of various organic molecules developed as TGF-β inhibitors.
• Discussion of their mechanisms of action, including down-regulating TGF-β expression or inhibiting receptor kinase activity.

Conclusions:

• Organic molecules targeting the TGF-β pathway represent a promising therapeutic strategy for diseases associated with its dysregulation.
• Further research into their biological functions and binding poses is essential for advancing their clinical application.