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. Author manuscript; available in PMC: 2020 May 29.
Published in final edited form as: Trends Biochem Sci. 2018 May 4;43(7):533–546. doi: 10.1016/j.tibs.2018.04.003

Figure 3. Pepducin-mediated biased GPCR signaling.

Figure 3.

An unbiased agonist will induce balanced signaling by promoting coupling to heterotrimeric G-proteins, GRKs and βarrs (A). This will lead to G protein-dependent and β-arrestin-dependent signaling as well as GPCR desensitization, endocytosis and degradation. The CXCR4 pepducin ATI-2341 stabilizes a receptor conformation that selectively promotes Gαi-biased signaling with minimal coupling to Gα13, GRKs and βarrs (B). ICL3-9 is a Gαs-biased pepducin from the β2AR that stabilizes a receptor conformation that enhances Gαs signaling with minimal coupling to GRKs and βarrs and reduced desensitization and internalization of the β2AR (C). ICL1-9 is an arrestin-biased pepducin from the β2ARthat promotes βarr-dependent signaling with minimal G-protein signaling (D).