Structural insights and clinical advances in small-molecule inhibitors targeting TGF-β receptor I.

ABSTRACT: The dysregulation of the transforming growth factor β (TGF-β) signaling pathway plays a critical role in the onset and progression of several diseases, including cancer. Notably, TGF-β has emerged as a significant barrier to effective outcomes in cancer immunotherapies, particularly those using immune checkpoint inhibitors. In response to this challenge, small-molecule inhibitors targeting the TGF-β receptor I (TGF-βRI) have garnered attention as promising candidates for modulating the TGF-β signaling pathway. This comprehensive review focuses on the development of small-molecule inhibitors targeting TGF-βRI. We provide a detailed analysis of the structural biology of TGF-βRI, highlighting key binding interactions and structural insights derived from high-resolution X-ray crystal structure

SUBMITTER: Leonardo-Sousa C 

PROVIDER: S-EPMC11923830 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature