GPCRs constitute a major class of drug targets and modulating their signaling ca
ID: 179796 • Letter: G
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) GPCR is a seven transmembrane protein structure domain receptors to which heptahelical and serpentine receptors and to which G-protein are coupled to them..!! They are transmembrane protein and seven because they span the membrane 7 times.. The main function of GPCR is the signalling pathway which helps in cell signaling. It helps in transfer of lipids, nutrients and other molecules and also signals the cell about the presence outside the cell. The portion of these are present outside which is glycosilated and contains two Cystein molecules which bind to the ligand by forming the disulphide bond.. The presence of theroinine and serine can also helps in binding. It can bind to the N-terminal in metabotrophic glutamate receptors
(b) the ligand which binds here are proteins, amino acids, lipids, peptides, some signalling molecules like epinephrine, prostagladin, eye pigment rhdopsin etc.
(c) the one way to study the drug interactions is the measuring the given drug concentration outside the cells which will decrease dur to the binding of these drug molecules to the receptor..
The second method is the bio-info tools method in which u can check for auto - docking method by software.
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