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Addressing Unmet Medical Needs Drug Discovery Process Progress & Next Steps |
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Drug Discovery Process |
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Genelabs' drug discovery efforts have led to the identification of novel lead compounds with potent activity in preclinical models against the Hepatitis C Virus (HCV) and pathogenic fungi. Using structural and functional information on the molecular components of the relevant pathogen, Genelabs scientists design libraries of small molecules that are intended to bind to their molecular target with high affinity. These designed molecules are then synthesized by Genelabs medicinal chemists. Next, these compounds are assayed for activity in primary drug target screens by Genelabs biologists who evaluate the ability of the compounds to bind and affect the molecular target. Promising compounds are also screened in whole cell systems to evaluate the potency of activity, the breadth or selectivity of the effect, and the cellular availability of the compounds. The interplay between positive and negative biological effects is then analyzed and correlated to the structure of the compounds to provide a structure-activity relationship (SAR). This SAR is used to design subsequent generations of compounds, optimizing potency and the breadth and selectivity of activity. Optimized compounds are then tested for efficacy, toxicity, and drug metabolism/pharmacokinetics. Further optimization and investigation may yield novel drug candidates for preclinical development and ultimately clinical development. © Genelabs Technologies, Inc. All rights reserved. - Terms of Use |
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Genelabs' Drug Discovery Process  |