Helminths Of Veterinary Importance Research Articles

Target identification and validation for anthelmintic discovery

Anthelmintics presently used in humans were discovered using empirical biological screening processes targeting helminths of veterinary importance. The modern approach to drug discovery is based on genetic, bioinformatic and genomic identification of protein targets followed by specific validation assays and high-throughput screening using chemical libraries. Existing broad-spectrum anthelmintics bind just three classes of molecular targets; more classes of targets are urgently needed. In the absence of robust functional genomics technologies for helminth parasites, the technology of RNA interference in parasites and in the model Caenorhabditis elegans is the best available for discovery and validation of new targets. This article outlines and critically discusses an idealised drug discovery pipeline for anthelmintic discovery in nematodes.

Review: Approaches to New Parasiticides

Intensive use of parasiticides has sometimes led to severe resistance in arthropods and helminths of veterinary importance. In the context of the growing awareness of parasitic diseases, this has created a public demand for effective and safe control agents. During the last two decades considerable knowledge in parasite neurophysiology and endocrinology has accumulated which allows the development of new screening procedures and target-site-directed approaches for the discovery of new drugs. The suitability of this strategic approach is discussed on the basis of recent discoveries of new chemical and natural compounds. In particular, target sites such as GABA A receptors, muscarinic and nicotinic acetylcholine receptors, cuticle synthesis and degradation, ecdysteroid receptors, the calcium release channel and semiochemicals have been selected in order to demonstrate the current approaches to identify new chemical entities, biologically active against nematodes and arthropods.