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Order the events that lead to desensitization of the GPCRs. __ Arrestins compete with G proteins...

Order the events that lead to desensitization of the GPCRs.

__

Arrestins compete with G proteins and bind to the phosphorylated sites of the GPCR
____

The GPCR bound to arrestin is taken in via endocytosis
___

The vesicle with the inactivated GPCR may fuse with lysosomes -> the GPCR will be degraded
___

GRK (G protein Coupled receptor kinase) phosphorylates the cytoplasmic side of GPCR
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ANSWER:

The sequence of events that lead to desensitization of the GPCRs are as follows:

1. GRK (G protein Coupled receptor kinase) phosphorylates the cytoplasmic side of GPCR.

2. Arrestins compete with G proteins and bind to the phosphorylated sites of the GPCR.

3. The GPCR bound to arrestin is taken in via endocytosis.

4. The vesicle with the inactivated GPCR may fuse with lysosomes -> the GPCR will be degraded.

Discussion: GRK is a family of kinases that phosphorylates the GPCR and turns off the activated state of it. It occurs in a two-step process first the GRK selectively phosphorylates the cytoplasmic receptor then arrestin binds to this phosphorylated site. After this step, the GRK and arrestin complex is internalized via endocytosis and finally, degradation of the GPCR is done by fusing the endosome with lysosome.

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