Editorial [Hot Topic: Enzyme Inhibitors as New Drugs for Microbial Diseases Control: Part I (Guest Editor: Alane Beatriz Vermelho)]

Enzymes from a variety of microorganisms have been characterized and explored as novel chemotherapeutic targets. In this context enzyme inhibitors have become a hot research area due to their immense potential for microbial disease control. This special issue of Current Enzyme Inhibition entitled “Enzyme inhibitors as new drugs for microbial disease control (Part I)”, brings together three reviews that focus on several important aspects of enzyme inhibition in Chagas disease and leishmaniasis, human immunodeficiency virus, type 1 (HIV-1) and pathogenic bacteria.

The first review by Maia and Fraga describe the use of the molecular hybridization approach as a powerful medicinal chemistry tool for designing ligands and prototypes able to act on at least two different molecular targets. Drug resistance is an increasing problem affecting the treatment of microorganisms of medical importance such as viruses, bacteria and other parasites. Consequently, the development of new chemotherapeutic agents that are more potent and less prone to resistance than the current drugs is an important matter. The review describes the use of a hybrid therapy strategy where a single chemical entity could modulate two or more biological targets to control the disease. An example of the hybrid approach is the Anti-HIV Prototype which involves the dual inhibition of HIV-1 through reverse transcriptase (RT) and integrase (IN).

In the second review Rodrigues et al. made a comprehensive description of the Cysteine peptidases inhibitors studied as a possible chemotherapeutic agents to control Chagas disease. Also other peptidase inhibitors against metallo-, aspartic and threonine (proteasome) peptidases that currently are in progress and could be promising targets in the future were described.

In the last review, Merlino et al. discusses the validity of several enzymes and pathways as chemotherapy targets against Chagas disease. Prenyl converting and transferring enzymes, cAMP- specific phosphodiesterases, polyamine and trypanothione synthetic pathways, triosephosphate isomerase, α-hydroxy acid dehydrogenases and trans-sialidase were evaluated in this review.

As the Guest Editor, I invited researchers from different universities that were working with inhibitors of microbial enzymes to describe the recent advances in their specific areas of this field. I am very grateful to all of these authors for providing their reviews that combined have provided such an excellent perspective of this important field. We would also like to thank the referees who have critically evaluated the papers.