Antimalarial Lead Discovery and Chemical Genomics
Author Information
Author(s): Garcia-Bustos Jose F., Gamo Francisco-Javier
Primary Institution: Tres Cantos Medicine Development Campus, GlaxoSmithKline, Spain
Hypothesis
What is the nature of the bias in chemical diversity identified in screens for Plasmodium falciparum?
Conclusion
The study suggests that a one-to-one correlation between chemical families and individual targets cannot be reliably established.
Supporting Evidence
- Thousands of hit structures for Plasmodium falciparum are now publicly available.
- The chemical diversity identified may not represent the necessary chemotypes to inhibit drugable targets.
- Compounds in the same chemical family can show different effects on parasites.
Takeaway
Scientists are trying to find new medicines for malaria by looking at many different chemicals, but it's hard to know which ones will work because they can affect the germs in different ways.
Methodology
The study discusses the analysis of chemical screens against Plasmodium falciparum and the challenges in correlating chemical families with drug targets.
Potential Biases
The starting compound libraries are biased towards certain physicochemical properties and human targets.
Limitations
The study acknowledges the difficulty in estimating the coverage of target space and the subjective nature of chemical classification.
Digital Object Identifier (DOI)
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