The Koehler Lab aims to innovate in the earliest stages of drug discovery by building chemical tools and technologies to expand the repertoire of protein targets that are considered “undruggable."
We focus primarily on building chemical tools and methods for studying temporal aspects of transcriptional regulation in development and disease, with a focus on target validation in cancer.
Targeting oncogenic transcription factors
Our team is developing a general approach to small-molecule probe discovery for transcription factors by coupling high-throughput binding assays, like small-molecule microarrays (SMMs), with functional assays involving transcriptional and cellular readouts
Novel probes of deacetylases
Histone deacetylases (HDACs) have emerged as valuable targets for small-molecule probes and drugs due to their fundamental role in transcriptional regulation and implication in several diseases.
Small molecule microarray screening
Over the last decade, small-molecule microarrays (SMMs) have proven to be a general, robust and scalable screening platform for discovering protein-small molecule interactions that lead to modulators of protein function