Abstract
Histone deacetylase inhibitors (HDACi) are an emerging class of novel anti-cancer drugs that cause growth arrest, differentiation, and apoptosis of tumor cells. In addition, they have shown promise as anti-parasitic, antineurodegenerative, anti-rheumatologic and immunosuppressant agents. To date, several structurally distinct small molecule HDACi have been reported including aryl hydroxamates, benzamides, short-chain fatty acids, electrophilic ketones, and macrocyclic peptides. Macrocyclic HDACi possess the most complex cap-groups which interact with HDAC enzyme's outer rim and have demonstrated excellent HDAC inhibition potency and isoform selectivity. This review focuses on the recent progress and current state of macrocyclic HDACi.
Keywords: Cyclic tetrapeptide, depsipeptide, peptide mimetic, macrolide, ketolide, macrocycles, histone deacetylase inhibitors, HDAC
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Challenges, Consequences and Possible Treatments of Anticancer Drug Discovery ll
The use of several compounds has been the subject of increasing interest in phytochemistry, biochemistry, and other fields of research at the chemistry-biology-ecosystems interface. In spite of the continued search for new anticancer drugs, cancer remains a leading cause of death. Cancer mortalities are expected to increase to 12.9 million, ...read more
Related Journals
Anti-Cancer Agents in Medicinal Chemistry
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Current Bioactive Compounds
Current Cancer Drug Targets
Combinatorial Chemistry & High Throughput Screening
Current Cancer Therapy Reviews
Current Diabetes Reviews
Current Drug Safety
Current Drug Targets
Current Drug Therapy
Related Books
Herbs for Disease Prevention and Treatment
Anthocyanins: Pharmacology and Nutraceutical Importance
Herbal Medicine for Autoimmune Diseases
Therapeutic Insights into Herbal Medicine through the Use of Phytomolecules
The Roles and Responsibilities of Clinical Pharmacists in Hospital Settings
Bioactive Compounds from Medicinal Plants for Cancer Therapy and Chemoprevention
Science of Spices and Culinary Herbs - Latest Laboratory, Pre-clinical, and Clinical Studies
The Chemistry inside Spices & Herbs: Research and Development
The Chemistry inside Spices & Herbs: Research and Development
Drug Addiction Mechanisms in the Brain
34