Enediynes: Exploration of microbial genomics to discover new anticancer drug leads
نویسندگان
چکیده
The enediyne natural products have been explored for their phenomenal cytotoxicity. The development of enediynes into anticancer drugs has been successfully achieved through the utilization of polymer- and antibody-drug conjugates (ADCs) as drug delivery systems. An increasing inventory of enediynes would benefit current application of ADCs in many oncology programs. Innovations in expanding the enediyne inventory should take advantage of the current knowledge of enediyne biosynthesis and post-genomics technologies. Bioinformatics analysis of microbial genomes reveals that enediynes are underexplored, in particular from Actinomycetales. This digest highlights the emerging opportunities to explore microbial genomics for the discovery of novel enediyne natural products.
منابع مشابه
Strain Prioritization and Genome Mining for Enediyne Natural Products
The enediyne family of natural products has had a profound impact on modern chemistry, biology, and medicine, and yet only 11 enediynes have been structurally characterized to date. Here we report a genome survey of 3,400 actinomycetes, identifying 81 strains that harbor genes encoding the enediyne polyketide synthase cassettes that could be grouped into 28 distinct clades based on phylogenetic...
متن کاملRecent Advances in Drug Repositioning for the Discovery of New Anticancer Drugs
Drug repositioning (also referred to as drug repurposing), the process of finding new uses of existing drugs, has been gaining popularity in recent years. The availability of several established clinical drug libraries and rapid advances in disease biology, genomics and bioinformatics has accelerated the pace of both activity-based and in silico drug repositioning. Drug repositioning has attrac...
متن کاملEnediyne compounds - new promises in anticancer therapy.
Scientists of all kinds have long been intrigued by the nature, action and potential of natural toxins that possess exceptional antibacterial and anticancer activities. These compounds, named enediynes, are among the most effective chemotherapeutic agents known. Often compared with intelligent weapons, due to the unique structure and sophisticated mechanism by which they destroy double-helical ...
متن کاملAn Overview of Asparaginase Enzyme Features: An Anticancer Enzyme with High Potency
Introduction: One of the important findings in the pharmaceutical and medical industry is the use of the asparaginazase enzyme as an anticancer drug. The asparaginase enzyme, hydrolyzing the amino acid of asparagine, reduces this amino acid in the blood and causes the death of cancer cells. Today, the enzyme is used to treat various types of leukemia, particularly acute lymphoblastic leukemia, ...
متن کاملImproving Drug Discovery From Microorganisms
Microorganisms remain unrivalled in their ability to produce bioactive small molecules for drug development. However, the core technologies used to discover microbial natural products have not evolved significantly over the past several decades, resulting in a shortage of new drug leads. Advances in DNA-sequencing and bioinformatics technologies now make it possible to rapidly identify the clus...
متن کامل