Question( 50 point) GPCRs constitute a major class of drug targets and modulatin

Question

Question( 50 point)

GPCRs constitute a major class of drug targets and modulating their signaling can produce a wide range of pharmacological outcomes. With the growing number of high-resolution GPCR crystal structures, we have the unprecedented opportunity to leverage structure-based drug design techniques.

A. Describe the structure and functionality of GPCRs and identify the commonly druggable sites on the protein.

B. Describe the types of ligands that commonly bind GPCRs.

C. Describe techniques that are used to study drug interactions with GPCRs.

Explanation / Answer

A. GPCR has a integral membrane protein. It has seven transmembrane helices and two cysteine residues whih re present in the extracellular side. it's function is to sense extracellular ligands and activate signal transduction pathways inside the cell. There are some pockets present in the GPCR where the ligand can bind and thus these pockets acts as the common druggable sites.

B. Types of lignd that bind to GPCR are hormones, pheromones, neurotransmitter etc. These bind to GPCR and activate signaling pathways.

C. FRET is a technique that can be used to study interaction of drug with GPCR. Also fluorescence spectroscopy can be used to study this interaction as conformational changes can be studied when a ligand binds to the receptor.

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