Enzyme Inhibitors: Design, Synthesis and Biological Evaluation

Dear Colleagues,

Enzymes are specialized proteins that increase the speed of chemical reactions, thus acting as biocatalysts. In the human body, enzymes catalyze all kinds of chemical reactions, playing vital roles in digestion and metabolism, blood coagulation, neuronal signaling, DNA repair, and replication, as well as many other functions. Under physiological conditions, an enzyme works by first binding to its substrate, forming an enzyme-substrate complex, which is next converted into the final product. The final product then dissociates from the enzyme, and a new catalytic cycle begins. Although they are crucial for life, dysfunctional, improperly regulated, over-active, or over-expressed enzymes contribute to the pathology of many diseases. Both naturally derived and synthetic molecules can bind to enzymes and alter their catalytic activity, and, in most cases, reduce enzyme activity. Many of these enzyme inhibitors are approved drugs, and enzyme inhibition continues to play a pivotal role in medicinal chemistry. A primary understanding of the action of enzyme inhibitors is fundamental for the development of new therapeutic agents. This Special Issue focuses on all aspects of enzyme inhibitors, ranging from the design and synthesis of these compounds, to their pharmacological evaluation, to computational modeling and structural biology studies that seek to understand the interactions between inhibitors and enzymes. Papers that focus on innovative aspects or novel mechanisms of enzyme inhibition are also welcome. We hope that this Special Issue stimulates authors and readers and makes an important contribution to the field of medicinal chemistry.

Dr. Letizia Crocetti
Dr. Maris Cinelli
Guest Editors

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