G-pro­tein-coupled recept­ors (GPCRs) are a large fam­ily with about 800 mem­bers, includ­ing recept­ors for light, taste, and smell, as well as approx­im­ately 400 recept­ors for neur­o­trans­mit­ters and hor­mones. The lat­ter are the most import­ant group of drug tar­gets, such as for beta-block­ers, anti­histam­ines, opioids, and the new dia­betes and weight-loss med­ic­a­tions. All GPCRs share com­mon struc­tural fea­tures and sim­ilar activ­a­tion mech­an­isms. They trans­mit their sig­nals to G pro­teins and β-arrestins, through which they reg­u­late numer­ous body func­tions. n.

At ISAR Bioscience, we use bio­chem­ical, phar­ma­co­lo­gical, and micro­scopic tech­niques to invest­ig­ate the mech­an­isms of their func­tion and their poten­tial for the devel­op­ment of innov­at­ive drug ther­apies. We are research­ing the role of GPCRs in dis­eases of the nervous, immune, and car­di­ovas­cu­lar sys­tems and search for novel drug can­did­ates. In this endeavor, we col­lab­or­ate closely with the former Receptor Sig­nal­ing Research Group at the Max Del­brück Cen­ter in Ber­lin, the Rudolf Boehm Insti­tute at the Uni­ver­sity of Leipzig, and the SFB 1423 “Struc­tural Dynam­ics of GPCR Activ­a­tion and Sig­nal­ing” based in Leipzig.

ISAR Bioscience is coordin­at­ing a European research con­sor­tium to develop a ground­break­ing tech­no­logy for char­ac­ter­iz­ing drug can­did­ates that act on GPCRs. The “Uni­S­ens” Pathfinder pro­ject, fun­ded by the European Innov­a­tion Coun­cil, is devel­op­ing a novel assay designed to dir­ectly meas­ure GPCR activ­a­tion and dis­tin­guish between dif­fer­ent types of activ­a­tion. Our part­ners from uni­ver­sit­ies and star­tups are based in France, the Neth­er­lands, Spain, the Czech Repub­lic, and Switzerland.