PDZ Protein Regulation of G Protein–Coupled Receptor Trafficking and Signaling Pathways

PDZ Protein Regulation of G Protein-Coupled Receptor Trafficking and Signaling Pathways.

G protein-coupled receptors (GPCRs) contribute to the regulation of every aspect of human physiology and are therapeutic targets for the treatment of numerous diseases. As a consequence, understanding the myriad of mechanisms controlling GPCR signaling and trafficking is essential for the development of new pharmacological strategies for the treatment of human pathologies. Of the many GPCR-inte...

Regulation of G protein-coupled receptor trafficking.

G protein-coupled receptors (GPCRs) mediate cellular responses to diverse extracellular stimuli to play a vital role in the control of physiology and behaviour. GPCR trafficking is of fundamental importance for the regulation of GPCRs signaling. In this mini review, we will discuss some of the recent findings on the mechanisms that regulate GPCR trafficking, which include (i) large dense-core v...

Protease-activated receptors: new concepts in regulation of G protein-coupled receptor signaling and trafficking.

Most G protein-coupled receptors (GPCRs) are reversibly activated upon ligand binding. However, activation of protease-activated G protein-coupled receptors (PARs) occurs through an irreversible proteolytic event that results in the generation of a tethered ligand that cannot diffuse away. This unusual mode of PAR activation raises important questions regarding the mechanisms responsible for te...

A direct and functional interaction between the trimeric G protein Go and Rab5 in G proteincoupled receptor signaling

Modeling of G-protein-coupled receptor signaling pathways.

G-protein-coupled receptors (GPCRs)2 are the largest family of cell membrane receptors. An estimated 50% of current pharmaceuticals target GPCRs (1), suggesting that further increases in our understanding ofGPCRs and the signaling pathways they initiate will lead to new drug targets. Mathematical and computationalmodeling (here, simply “modeling”) has a substantial history in modern biology and...