Dear Colleagues,

Modulating enzyme activity is a proven strategy in drug discovery, as shown by the small-molecule armament of marketed drugs – about half of the total – that is directed against enzymes. Rationales for targeting enzymes are typically based on their pivotal roles in disease states, and the possibility of designing chemical entities capable of docking sensitive ligand-binding sites. In today’s post-genomic era, this area of research can take advantage of, and be expedited by, major advances in target identification and validation, production of natural product and chemical libraries, nutraceutical research, cell-free and cell-based assay methods, high-throughput screening technologies, hyphenated techniques, as well as cheminformatics and bioinformatics resources.

The natural world provided huge number of secondary metabolites with intriguing medical properties known by humankind. Because in recent decade, hundreds of new natural enzyme inhibitors derived from the natural world and these molecules are able to target important biological human proteins or enzymes are identified. Notably, some of these molecules which illustrated activities towards enzymes relevant to cancer, have been included in clinical trials to evaluate their effectiveness.

This Special Issue welcomes original articles, communications and reviews dealing with the isolation and/or the investigation of mechanisms of action of natural products, natural product derivatives and synthetic compounds with potential effects towards cancer-associated enzymes. Finding target-identification (with biological assays together with computational studies), in vivo studies, bioavailability, toxicity, and the design of novel molecules with improved biological effects against cancer-associated enzymes are also welcome. Pharmacological studies should include appropriate positive controls.

Prof. Dr. Hidayat Hussain
Guest Editor

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• cancer
• natural products
• natural product derivatives
• synthetic compounds
• cancer-associated enzymes
• (activity-guided) isolation of natural products
• computational methods
• in vitro studies
• in vivo studies
• mechanism of action
• bioavailability
• toxicity