Chen Yang, Xiaofei Sun, Zhong Yu, Dan Liu, Rong Hu
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Small-molecule mTOR inhibitors in the clinic: From bench to bedside.
As a central modulator of cellular proliferation, metabolic processes, and immunological functions, the mechanistic target of rapamycin (mTOR) signaling pathway has emerged as an attractive therapeutic focus for managing diverse pathological conditions, including cancer, autoimmune disorders, and organ transplant rejection. mTOR inhibitors, initially identified in the context of cancer therapy, have shown efficacy in regulating immune responses and preventing abnormal cell proliferation. Pharmacological investigations spanning preclinical models to human subjects reveal mTOR-targeting agents possess immunomodulatory properties concurrent with antitumor effects, evidenced by multicenter clinical studies documenting improved progression-free survival rates and delayed oncological recurrence in epithelial-derived and hematopoietic malignancies. This review explores the development of mTOR inhibitors, tracing their journey from early laboratory discoveries to clinical application, and emphasizes their role in transforming the therapeutic landscape for a range of diseases.
期刊介绍:
Bioorganic Chemistry publishes research that addresses biological questions at the molecular level, using organic chemistry and principles of physical organic chemistry. The scope of the journal covers a range of topics at the organic chemistry-biology interface, including: enzyme catalysis, biotransformation and enzyme inhibition; nucleic acids chemistry; medicinal chemistry; natural product chemistry, natural product synthesis and natural product biosynthesis; antimicrobial agents; lipid and peptide chemistry; biophysical chemistry; biological probes; bio-orthogonal chemistry and biomimetic chemistry.
For manuscripts dealing with synthetic bioactive compounds, the Journal requires that the molecular target of the compounds described must be known, and must be demonstrated experimentally in the manuscript. For studies involving natural products, if the molecular target is unknown, some data beyond simple cell-based toxicity studies to provide insight into the mechanism of action is required. Studies supported by molecular docking are welcome, but must be supported by experimental data. The Journal does not consider manuscripts that are purely theoretical or computational in nature.
The Journal publishes regular articles, short communications and reviews. Reviews are normally invited by Editors or Editorial Board members. Authors of unsolicited reviews should first contact an Editor or Editorial Board member to determine whether the proposed article is within the scope of the Journal.