The regulation of transcription by RNA polymerase II is the key controlling step in development, and its misregulation results in the pathogenesis of a number of human diseases including cancer. Several factors including the transcriptional initiation and elongation machineries, chromatin remodeling complexes, and chromatin modifiers have been shown to be central in the regulation of gene expression. Much has been learned about the molecular role of chromatin remodelers and modifiers in transcriptional control and human health. Most of such studies find their origination in the first discovery of histone deacetylase (HDAC) and its inhibitor trichostatin A (TSA). To date, other small molecular inhibitors of chromatin modifiers and interactors have been identified and some are being used successfully in clinic. The overall goal of this meeting is to gather experts in the area of genetics and biochemistry of chromatin and transcriptional regulators and further discuss how this process is involved in development and how small molecule inhibitors of transcription and chromatin modifiers can be used for the treatment of human diseases including cancer.