Contact usContact us
   DTECT ALL <SUP>TM</SUP>

In this section

    DTect-All

    GENERAL PRINCIPLE

    DTect-AllTM is a binding technology designed for the identification of every compounds interacting with the 7-transmembrane (7-TM) domain of engineered GPCRs. The corresponding FRET-based assays, developed on stable cell lines, are screened in presence of fluorescent probes that act as surrogate markers of the GPCR change of conformation.

    DTect-AllTM IS A THREE STEP PROCESS

    The external truncation (STEP 1) focuses the test on potential allosteric modulator sites by removing all or part of the endogenous ligand binding site (orthosteric site). A fluorescent protein is fused to the GPCR to create the energy donor of the FRET detection system.

    The energy acceptor of the detection system is made of a fluorescent probe interacting non-selectively with extracellular loops or 7-TM domain. The probe is obtained by screening a proprietary collection of more than 5,000 GPCR-frequent-hitter fluorescent molecules enabling the selection of a probe suitable for FRET interaction (STEP 2). Domain’s probe collection allows assay development for every GPCR, including orphans. The double labeling system detects GPCR-interacting ligand only on-target.

    The resulting binding assay is screened to identify compounds disturbing FRET-signal by conformational change of the GPCR 7-TM (STEP 3). Most interesting GPCR-interacting ligands are not competitively displacing the probe and bind at any site on the receptor surface.

    DTect-All