Enzyme Inhibitors: Potential Therapeutic Approaches, 2nd Edition
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 15 August 2025 | Viewed by 159
Special Issue Editor
Interests: medicinal chemistry; enzymology; biochemistry; COX inhibitors; LOX inhibitors; HIV-1 RT inhibitors; HIV-1 integrase inhibitors; PTP1b inhibitors; HIV-1 protease inhibitors; anti-inflammatory; antidiabetic; antiviral; antibacterial; antifungal; food-derived antigens; anti-Neu5Gc
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Due to its involvement in all biochemical processes, enzymes constitute a major drug target occupying the second position after receptors. Several pathologic disorders have been related to enzyme dysregulation. Although there are cases in which enzyme administration is needed to counteract the lack or reduced activity of an enzyme, the main therapeutic approaches involve the administration of small molecules that moderate enzyme activity, with enzyme inhibition being the most common target. Inhibitors of human enzymes are used in the treatment of many common diseases, such as inflammation, hypertension, and hypercholesterolemia and are among the medications for the treatment of diabetes. Moreover, bacterial, fungal and viral enzymes are the targets of most antimicrobial and antiviral drugs. In addition to the continued increasing of the catalogue of enzymes that constitute drug targets, the research for novel inhibitors for known enzyme targets continues, aiming to develop agents with less side effects or novel drugs appropriate for resistant strains. Although competitive inhibitors are by far the most common type of inhibitors among the approved drugs or drugs under research, the development of inhibitors with non-competitive, uncompetitive, or mixed modes of inhibitory action attract scientific interest in special occasions. As inhibitors mimicking substrates and targeting the active site may more often exhibit low specificity, interacting with a variety of isoenzymes or enzymes acting on the same substrates, allosteric inhibitors may be preferred when allosteric sites exist. Moreover, uncompetitive or non-competitive inhibitors could be preferable because of their ability to better act at high substrate concentrations where competitive inhibitors are practically inactive, a situation which may locally occur at a cellular or tissue level.
This Special Issue aims to gather research and review articles on enzymes and enzyme inhibitors with pharmaceutical interest, covering a hot and developing area of medical research.
Prof. Dr. Phaedra Eleftheriou
Guest Editor
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Keywords
- enzymes
- inhibitors
- competitive
- uncompetitive
- non-competitive
- drug target
- pharmaceutical approach
- disease treatment
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