ReviewMolecular therapy. Oncology2025
Structural insights and clinical advances in small-molecule inhibitors targeting TGF-β receptor I.
Review in Molecular therapy. Oncology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
8 citing papers in PubMed.
- Antifibrotic hydrogel strategies for scarless tissue regeneration: mechanisms, design, and application.Bioactive materials · 2027Review
- Keratin 20 deficiency phenocopies human UAB and drives bladder fibrosis via a mechanotransduction-TGF-β axis.iScience · 2026Article
- Unraveling the causal role of TGF-βRII in osteoporosis and the potential of its associated differential genes as novel targets.European journal of medical research · 2025Article
- Unlocking the Role of OCT4 in Cancer Lineage Plasticity: A Cross-Cancer Perspective with an Emphasis on Prostate Cancer.Biomedicines · 2025Review
- Advances in mechanisms and challenges in clinical translation of synergistic nanomaterial-based therapies for melanoma.Frontiers in cell and developmental biology · 2025Review
- Nanomaterials targeting cancer stem cells to overcome drug resistance and tumor recurrence.Frontiers in oncology · 2025Review
- Identification of dual inhibitors of ROCK1 and TGFBR1 for overcoming metastasis: an integrated pharmacophore and docking driven CADD strategy.In silico pharmacology · 2025Article
- Developments in the study of the role of lactate metabolism in the genesis and progression of thyroid cancer.Frontiers in cell and developmental biology · 2025Review
Corrections and comments
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Authors and funding
5 authors.
Funding
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 structures. Additionally, we review the current landscape of TGF-βRI inhibitors in clinical trials, including eight promising inhibitors, and discuss their mechanisms of action, selectivity, and therapeutic potential. Our investigation extends to the patent literature, summarizing over 2 decades of innovation from leading pharmaceutical companies, spanning January 2000-May 2024. This consolidated structural and biochemical knowledge aims to facilitate the design of next-generation TGF-βRI inhibitors, addressing unmet clinical needs in oncology and fibrosis treatment. The synergistic potential of combining TGF-βRI and immune checkpoint inhibitors is also explored, offering promising avenues for enhancing cancer immunotherapy efficacy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.