Fig. 2: Design of bipartite CRAC activators.
From: On-demand treatment of metabolic diseases by a synthetic drug-inducible exocytosis system
A Conceptual design. Synthetic CRAC activators can also be expressed as two separate proteins in which STIM1ct and the oligomeric domain are each fused to different proteins that conditionally interact with each other via constitutive or chemically-inducible protein-protein interactions (PPI). In the absence of PPI, STIM1ct cannot interact with the oligomeric complex and therefore remains in a resting state. Only pre-programmed PPI events can allow individual STIM1ct molecules to join an oligomeric “docking station”, resulting in STIM1ct oligomerization and Orai1 activation. B Experimental validation by Ca2+-dependent gene expression. Source data are provided as a Source Data file. Numbers indicate average fold-changes of SEAP expression within column groups.
