The Transporter Map project addresses a critical gap in transporter drug discovery through an innovative
technology platform that enables comprehensive, family-wide screening of substrates and inhibitors.
Cellular transporters control the movement of nutrients and drugs across cell membranes, with approximately
1500 genes dedicated to their functions in the human genome. Despite their role in virtually every cellular
process and connection to numerous diseases, they have been largely untapped for treating human disease.
One major challenge for developing drugs for transporters has been the lack of robust assay technology for
family-wide transporter screening. While other successful target classes such as G protein-coupled receptors
(GPCRs) benefit from streamlined assay development, where one assay fits many targets, transporter assays
have required specialized, individual approaches for each transporter, making assay development expensive
and tedious. This has created a significant disparity in drug discovery outcomes. Despite similar disease
relevance, only 5% of transporters are targeted by approved drugs, compared to 24% of GPCRs.
Transporter Map aims to close this technology gap by combining a library of genetically-encoded biosensors
with an overexpression library of the entire transporter family. When a cell encounters a substrate compatible
with its overexpressed transporter, it takes it up, triggering a fluorescence change in one or multiple biosensors.
This fluorescence change enables the enrichment of cells expressing that transporter and allows identification
of specific transporters responsible for substrate uptake.
The Transporter Map platform transforms transporter research by providing a pooled screening method
previously unavailable to the field and has potential to significantly accelerate drug discovery efforts.