Hamza Hameed
School of Life Sciences
Screening for antiparasitic leads from a library of natural products
from temperate zone plants.
There is an urgent need to identify and evaluate novel chemical scaffolds to seed the
drug discovery pipeline for parasitic diseases. Complementing international efforts to
explore the potential of huge commercial chemical libraries, the search for new leads
also encompasses the evaluation of natural products. PhytoQuest, a UK-based
Industrial Biotechnology small to medium-sized enterprise, has produced a library of
approximately 1000 molecules, isolated predominantly from temperate zone plants.
As such, this library represents a unique resource for lead discovery of high value
chemicals from temperate zone plants against parasitic diseases, with previous
studies focusing largely on plants from tropical and subtropical zones. The library
comprises a wide range of chemical classes, two thirds of which are novel, and the
remaining third not commercially available. Critically, the compounds are pure,
overcoming common issues with screening fractions of complex mixes, and have
been selected to reflect potential development, with a high degree of functionality
and physiochemical properties that match Lipinski’s Rule of Five. A subset of
approximately 650 compounds have been screened against the intraerythrocytic
stages of Plasmodium falciparum and axenic amastigotes of Leishmania mexicana,
with a further screen against Trypanosoma brucei now underway. Here we report a
characterization of our hits against P. falciparum and L. mexicana. This research is
supported by a BBSRC-funded High Value Chemicals from Plants (HVCfP) Proof of
Concept award to PhytoQuest and Keele University.
Postgraduate Conference 2016
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