Expanding the Cancer Drug Discovery Toolbox: A Focus on Protein Degradation, Allosteric Modulation, and Covalent Inhibition
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 25 February 2025 | Viewed by 49
Special Issue Editors
Interests: drug discovery; drug design and synthesis; organic synthesis; multicomponent reactions; multitarget directed ligands; protein degradation and modulation; cancer; neurodegenerative diseases
2. Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, “Sapienza” Università di Roma, Rome, Italy
Interests: medicinal chemistry; drug design and synthesis; organic synthesis; structure–activity relationship; antimicrobial and antiviral agents; anticancer agents
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Special Issue Information
Dear Colleagues,
Cancer drug discovery is continually evolving, driven by the need for more precise and effective therapies that can overcome drug resistance and target previously "undruggable" proteins. To this aim, in the last few years, an expanding range of chemical modalities have come of age, demonstrating clinical success and opening opportunities for biopharmaceutical innovation. Among them, three cutting-edge approaches reshape the medicinal chemistry landscape: protein degradation, allosteric modulation, and covalent inhibition.
One of the most significant advancements in this field is the rise of targeted protein degradation technologies, which have catalyzed a paradigm shift in therapeutic strategies and opened up new avenues for drug discovery. Notably, proteolysis targeting chimeras (PROTACs) have resulted in promising clinical candidates, offering a therapeutic option for challenging targets.
In recent years, there has been unprecedented innovation in allosteric drug discovery and development, with multiple drug candidates advancing into clinical studies. Allosterism, which involves designing small molecules to bind to non-orthosteric sites, allows for the fine-tuned regulation of protein activity, offering greater selectivity and reduced side effects.
Over the past 30 years, the rational design of covalent drugs has gained significant attention as a strategy to enhance selectivity by targeting non-conserved amino acids. Moreover, the prolonged target engagement of covalent drugs offers distinct pharmacodynamic advantages, including exceptional potency, particularly against high-turnover or drug-resistant proteins.
This Special Issue welcomes original and review articles that showcase recent advancements in these fields, emphasizing innovative chemical methodologies, structure-based drug design, and promising preclinical and clinical outcomes. The contributions will address key challenges such as optimizing drug-like properties, enhancing selectivity, and overcoming resistance mechanisms to revolutionize cancer therapy.
Dr. Rita Maria Concetta Di Martino
Dr. Antonella Messore
Guest Editors
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Keywords
- protein degradation
- proteolysis targeting chimeras
- hydrophobic tags
- molecular glues
- allosteric modulators
- covalent inhibitors
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