To: scaram(o)uche who wrote (21573 ) 6/5/1998 6:33:00 AM From: Henry Niman Respond to of 32384
Rick, The data on the small molecule mimic of G-CSF was presented at a couple of conferences in February. Rumor has it that a major Science article detailing the info will be coming out very soon. This of course would be an agonist, but would open up an avenue for finding antagonists also. Ligand of course has published extensively on identification of agonists and antagonists of transcription factors and they have many issued patents in that area. I suspect that the new data has generated an major flurry of new patent applications for small molecule agonists and antagonist of polypeptide hormone receptors. Here's the abstract of a somewhat recent review of an article on screening for agonists and antagonist of transcription factors: J Recept Signal Transduct Res 1997 Jan;17(1-3):531-543 Drug discovery using receptors that modulate gene expression. Lamb P, Rosen J Ligand Pharmaceuticals San Diego California 92121, USA. 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 of latent transcription factors, which bind to specific sequences in the promoters of regulated genes. High throughput assay systems have been developed based on a detailed molecular understanding of these transcriptional regulation processes, and are being used as screens for both agonists and antagonists of specific cytokines and hormones. The opportunities for the discovery of novel and selective compounds using these systems is discussed. Publication Types: Review Review, tutorial PMID: 9029513, UI: 97181352