DRUG DISCOVERY USING RECEPTORS THAT MODULATE GENE-EXPRESSION

Cytokines and non-peptidyl small molecules, such as steroid hormones, exert many of their effects on cells through rapid regulation of gene expression. This is achieved by the activation of different families o f latent transcription factors, which bind to specific sequences in th e promoters of regulated genes. High throughput assay systems have bee n developed based on a detailed molecular understanding of these trans criptional regulation processes, and are being used as screens for bot h agonists and antagonists of specific cytokines and hormones. The opp ortunities for the discovery of novel and selective compounds using th ese systems is discussed.