New Strategies for Drug Development
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 31 December 2025 | Viewed by 1408
Special Issue Editor
Interests: biodegradation of aromatics including nonsteroidal anti-inflammatory drugs; enzymes involved in the breakdown of aromatics; immobilization of microorganisms and enzymatic proteins; microbial metabolism, kinetics, biocatalysis, protein purification and characterisation
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Special Issue Information
Dear Colleagues,
The search for new medicinal substances has accompanied man since ancient times. In the era of working on a new project concerning, among others, drug safety, protection of antibiotics, patent protection of drugs, and equal access to them, attention is paid to introducing safe, effective, and high-quality medicinal products to the market. Scientific projects are concerned with developing medicines that respond to previously unmet medical needs, including those related to neurodegenerative, autoimmune, or oncological diseases. Research on new antimicrobial agents is also supported to combat resistance to antimicrobial agents. The design and synthesis of new drugs, both using classical organic synthesis and the increasingly popular biotechnology or genetic engineering, aim to support the protection of public health, prolong life, and improve its quality. The most important research direction in pharmacy is to improve the interactions between the drug and its site of action. The aim is to develop medicines with increased biological activity and limited side effects that will reach specific sites in the body.
The search for new drugs involves three strategies. The first is the synthesis of new chemical compounds dedicated to the pharmacotherapy of a specific disease; the second strategy is based on the search for new indications for medicinal substances previously used in the pharmacotherapy of other diseases; the last strategy is modifying the structure, either of existing drugs or known biologically active natural substances. In this process, biotransformation processes are increasingly used with whole microorganisms and isolated, pure enzyme preparations.
Since the first successful attempts to isolate and purify biologically active substances from plants, which were used as drugs, the discovery of the existence of relationships between the structures of chemical compounds and their biological activity and the isolation of the so-called leading structures have had an epochal significance in the development of drugs. Plants have been a valuable source of many compounds with different leading structures since ancient times. Many of these substances have been used as drugs without changing their chemical structure; the rest have been modified into their synthetic analogues.
The most critical issue in drug design is determining the structure of the so-called leading compound. This structure should exhibit properties of therapeutic value. However, the leading compound serves only as a basis for obtaining other clinically valuable substances. Three methods are used to obtain the leading structure and its analogues: biosynthesis, total synthesis, and semi-synthetic procedures. The most popular methods of searching for new compounds that can exhibit biological and pharmacological activities entail making changes within the structures of known, active molecules, replacing a fragment of one molecule with another, or designing a new structure while maintaining groups. The exchange of substituents through simple chemical transformation gently adjusts the modified drug to its target site. This is a method where you can quickly gain access to new analogues. Currently, stereoselective enzymes obtained from microorganisms are increasingly used in such processes. Bacteria and fungi are efficient sources of biocatalysts, characterized by a wide range of pathways for synthesizing bioactive molecules. Drug design, using leading structures provided by the world of microorganisms, is supported by bioinformatics analyses.
Another promising direction of research is the development of drugs based on nucleic acids (RNA and DNA). In addition, biotechnology provides tools for sequence design, gene cloning, expression and purification, and analytics, both recombinant proteins and monoclonal antibodies, as well as drug candidates based on nucleic acids, including mRNA.
This Special Issue aims to present a broad picture of the latest achievements in new drug development strategies, both through bioinformatics tools and biotechnological methods, including biotransformation processes of natural products with biological activity. Original articles are welcome, as well as reviews on research on innovative methods of obtaining new biologically active substances.
Prof. Dr. Danuta Wojcieszyńska
Guest Editor
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Keywords
- drugs
- biosynthesis
- biotransformation
- natural products
- biological activity
- bioactive compounds
- structure–activity relationship
- drug development
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