Small-Molecule Modulators Targeting Emerging Therapeutic Pathways: Design, Synthesis and Biological Evaluation
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Chemical Biology".
Deadline for manuscript submissions: 31 May 2025 | Viewed by 7140
Special Issue Editor
Interests: protein–protein interaction; small-molecule inhibitors; kinase inhibitors; molecular glues; immunomodulators; anticancer therapeutics
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
In the post-genomic era, the therapeutic modalities of human diseases have evolved dramatically. Small-molecule modulators used to be the standard option for defined therapeutic pathways; however, antibodies, nucleotide-based drugs, and cell-based therapies are attracting increasing amounts of attention. Many novel therapeutic targets are emerging driven by advancements in biologic and clinical research, providing new opportunities for small-molecule modulators. For example, the inhibition of cellular protein–protein interactions was once considered undruggable but has now been proven to be workable in light of Venetoclax. In addition, specific cellular protein(s) can now be selectively degraded in the presence of rationally designed PROTACs and/or molecular glues, while small-molecule modulators of human immunity also show great therapeutic promises in human clinical trials. Notwithstanding, small-molecule modulators of enzymes are still a fruitful area of research delivering numerous marketed drugs. One notable example is that more than 70 small-molecule inhibitors of kinases have been approved by the FDA and hundreds of clinical trials are ongoing, testing more novel ones. In view of the dynamic evolution of small-molecule modulators targeting emerging therapeutic pathways, this Special Issue welcomes original research concerning their design, synthesis and biological evaluation
Prof. Dr. Yujun Zhao
Guest Editor
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Keywords
- immunomodulator
- enzymatic modulator
- PROTAC
- molecular glue
- modulator of PPI
- receptor agonist
- receptor antagonist
- small molecules
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