BromoTag and dTAG dimerizers add a new tool for inducing protein proximity
- Describes bivalent chemical dimerizers built on BromoTag and dTAG to induce homo- and heterodimerization of proteins in cells.
- A split-luciferase (NanoBiT) assay profiled a compound library for the ability to create new protein–protein interactions.
- Selected compounds activated caspase-9 and c-Kit kinase with activity comparable to existing dimerizer systems, adding an option for chemically induced proximity.
💡 Points Based on the abstract
Linker-length and exit-vector SAR would show whether this is a general toolkit or a narrow geometry window; dimerizer activity can be geometry-sensitive, and a hook effect at high dose is a likely failure mode. Two checks matter most: a monomeric-ligand competition control, and a potency and kinetics comparison with FKBP-based dimerizers, including any liabilities of BromoTag's ligand.
A BromoTag-Based Toolkit for Rapid Modulation of Chemically Induced Proximity ↗