CASE 26 The Role of specific Amino Acids in n in Receptor Bi

CASE 26 The Role of specific Amino Acids in n in Receptor Binding and Signal Transduction of the glucagon analogs presented here, which is the best glucagon antagonist? Could you design a better glucagon antagonist than the analogs presented here?Explain the rationale for your design.

Solution

Antagonist is a molecule which opposes the base molecule to perform an action. Here, the base molecule is glucagon; antagonist will be a mutation which reduces the binding affinity of glucagon to the receptor, thereby reducing the ability to produce cyclic AMP.

From the above results, it is evident that \"Des-His1-Des-Asp9\" is the best antagonist. It reduces the binding affinity to 7, and finally reduces the production of cAMP to zero.

A better analog compared to this one will be the one whose binding affinity is also zero. So, if the analog will not bind, it will not be able to produce cAMP.