Question

In: Biology

You find some cells have mutations that permanently deactivate Raf. Pleasure list the protein(s) that would...

You find some cells have mutations that permanently deactivate Raf. Pleasure list the protein(s) that would be an effective drug target for reversing the effect of the Raf mutation and explain your reasoning.

Solutions

Expert Solution

RAF kinases are a family of three serine/threonine-specific protein kinases that are related to retroviral oncogenes The mouse sarcoma virus contains a RAF kinase-related oncogene that enhances fibrosarcoma induction. RAF is an acronym for Rapidly Accelerated Fibrosarcoma. RAF kinases participate in the RAS-RAF-MEK-ERK signal transduction cascade, also referred to as the mitogen-activated protein kinase (MAPK) cascade.

As you can see the proteins involved in Raf protein pathway are

RAS activates RAF.

MEK RAF activates MEK which further activates ERK.

ERK which is responsible for feedback inhibition.

So if there is mutation which deactivates the RAF it means cell is having mutation in the kinase activity of RAF because in the figure you can see they are kinase inhibitor which deactivates the RAF. So using this knowledge we can assume that if we use the kinase activator drug which compounds differ from ATP-centric drugs in that they do not compete with ATP for binding to the catalytic domain, generally acting by inducing conformational changes to modulate activity. example for such type of drug is small-molecule AMP kinase activator, parmitoyltransferase 1, increases activity of the enzyme inhibiting the autoinhibitory phosphorylation state of the enzyme. This type of activator molecules can be used.


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