Leipzig University, Germany
Short Communication
Structural insights in the binding mode of neuropeptide Y at G protein coupled receptors and consequences for drug development
Author(s): Annette G Beck-Sickinger*
Peptides hormones play an important role in the regulation of manifold activities in the body. Many of them transmit their activity through G-Protein Coupled Receptors (GPCR), which are among the most promising drug targets nowadays. Accordingly, elucidating the binding mode of ligands is essential. Whereas several small molecule systems have been well characterized, ligand binding of large and flexible peptides is still more challenging. In addition to ligand binding and receptor activation, indirect mechanisms have been shown to play a role for drugs addressing GPCRs. This includes desensitization, internalization and accordingly their potential use as drug shuttles, e.g. in tumor targeting. Accordingly, in addition to ligand binding, internalization has to be addressed and to be studied, including arrestin recruitment. Accordingly, ligand binding, structural dynamics, and internali.. View More»
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