HTRF Resource Library

Comparison of two Homogenous Time-Resolved Fluorescence (HTRF®) assays for high throughput screening of a natural product library

By: Michael F. Jobling, Gregory A. Fechner, Ronald J. Quinn, Vicky M. Avery

Natural Product Discovery, AstraZeneca, and Eskitis Institute for Cell and Molecular Therapies, Griffith University, Queensland, Australia

Abstract:
Natural products and their derivatives have historically been invaluable as a source of therapeutic agents. In fact, nearly 50% of all new chemical entities introduced over the last 25 years were natural products, semi-synthetic natural product analogues or synthetic compounds based on natural product core structures. This presentation describes the use of technologies based on homogenous time-resolved flourescence (HTRF^®), for the screening of a natural product library. Both assays are based on commercially available kits from Cisbio international, developed for the screening of large synthetic compound libraries, and are capable of miniturisation. Screening results obtained for a GPCR and an ezyme target will be examined, and compared to older, more established technologies. IC50's of control compounds, Z' values, and assay conditions will be presented.