Hit To Lead In-Depth Focus 2017
In this In-Depth Focus we look at a pragmatic approach to hit validation following biochemical high-throughput screening as well as Identification of hits and leads for human African trypanosomiasis.
- A pragmatic approach to hit validation following biochemical high-throughput screening
Progressing actives from a high-throughput screen (HTS) of a target protein into suitable starting points for lead identification is fraught with pitfalls. The volume and quality of the HTS output is a function of the quality of the screening library, as well as specific properties of both the target and the screening assay. Agnes Martin, Laurent Rigoreau and Sheila McLoughlin review the pragmatic approaches they have elaborated to validate the output of over 40 biochemical HTS campaigns against cancer targets.
- Identification of hits and leads for human African trypanosomiasis
Neglected tropical diseases affect more than one billion people and new targets and drugs are needed to tackle these infections. The multi-disciplinary NMTrypI consortium has identified a number of different compound classes which could be effective against these diseases. Sheraz Gul, Giulia Pasini and Maria Paola Costi review some of these compounds.