Advances in Enzyme Inhibitors and Protein Degraders as Anticancer Agents
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 31 December 2025 | Viewed by 90
Special Issue Editors
2. School of Dentistry and Medical Sciences, Charles Sturt University, Wagga Wagga, NSW, Australia
Interests: drug discovery; enzyme inhibitors; anticancer agents; sterols
Interests: biominerals; precision delivery; sustainable release; nano-enzyme; combinational therapies
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Cancer is known to be one of the leading causes of death worldwide, with approximately 20% of the population being diagnosed with cancer in their lifetime. Cancer costs the world economy trillions of dollars each year; therefore, there is a desperate need for new anticancer drugs with known mechanisms of action to circumnavigate issues pertaining to treatment efficacy and drug resistance.
Many oncogenic enzyme targets (i.e. KRAS, KATs) have been labelled “undruggable” in the past; however, advances in chemical biology and molecular biology have yielded tools that can drug these “undruggable” targets. One such technology that is rapidly advancing through clinical trials is a class of compounds called PROTACs (PROteolysis-TArgeting Chimeras). The first PROTAC to enter phase III trials was vepdegestrant (ARV-471), which is currently being studied as a potential treatment for patients with ER+/HER2− advanced breast cancer. We anticipate that the approval of PROTACs as anticancer agents is just a matter of time.
The use of antibody–drug conjugates (ADCs) as anticancer agents is rising exponentially. More than ten ADCs have already gained Food and Drug Administration (FDA) approval, and we expect this number to rise significantly in the coming years given the fact that there are hundreds of ADCs currently being investigated in clinical trials. Despite the numerous challenges faced by those that develop anticancer therapeutics, we envisage that the next breakthrough anticancer agent is just around the corner.
In this Special Issue, both original research articles and reviews (including scoping reviews) are welcome. Research areas may include, but are not limited to, the following: in silico, artificial intelligence, high-throughput screens, combination therapy, biomarkers, inhibitors, formulation, drug conjugates, tool compounds, drug discovery, and clinical trials.
Dr. David J. Leaver
Dr. Li Li
Guest Editors
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Keywords
- anticancer agents
- mechanism of action
- epigenetics
- PROTAC
- antibody–drug conjugates
- enzymes
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