Promega will be giving a special product presentation at MIKIW this year to promote their newest release. This will take place during the lunch hour on Saturday, April 18th. Attendance is optional, but encouraged!
Early-stage drug discovery increasingly pursues protein targets that are poorly defined, lack known ligands, or have no reliable functional assays — a population representing a substantial and largely untapped portion of the human proteome. For these difficult targets, the fundamental question of whether a small molecule actually engages its intended protein inside a cell has historically been unanswerable without extensive, target-specific assay development. The TarSeer™ BRETSA™ Target Engagement System is a new cell-based platform designed to address precisely this challenge. BRETSA (Bioluminescence Resonance Energy Transfer Shift Assay) detects compound binding by monitoring changes in target protein thermal stability directly in cells, using a luciferase-tagged target protein and a cell-permeable fluorescent probe binding to exposed hydrophobic regions of denatured proteins. As the target denatures upon heating, probe binding brings it into proximity with the luciferase, generating a measurable BRET signal that shifts when a compound engages the target and alters the thermal stability of that protein — providing direct cellular evidence of binding without the need for target-specific antibodies, tracer compounds, or prior knowledge of a binding site. In this talk, we will introduce the scientific principles underlying the BRETSA platform and present data demonstrating its application across more than 20 target classes and multiple cellular compartments. The focus will be on the technology's potential to open new doors — enabling researchers to study intracellular target engagement for proteins that were previously difficult to assay in cellular environments. This presentation is intended as an early look at an emerging technology with significant potential implications for how we approach difficult targets in the drug discovery pipeline.
Presenter: Kyle Hooper, PH.D
