GPCRs constitute a major class of drug targets and modulating their signaling ca

Question

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) GPCRs is a seven transmembrane structure and mediate cellular responses to numerous extracellular ligand signals. This receptor can be grouped into five major protein families based on their amino acid sequences. Based on the crystal structure, the common "druggable" site is the extracellular extension of the dopamine D3 orthosteric subpocket.

B) Subatomic particles, ions, small organic molecules, peptides, and proteins are the types of ligands.

C)techniques used to study drug interaction with GPCRs are: usage of engineered metal ion binding sites to probe intramolecular interactions, cryo-electron microscopy imaging, and neutron scattering.

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