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Cellular and Molecular Biology

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Receptor Tyrosine Kinases as Therapeutic Targets

CELLS-KW63AB

Receptor Tyrosine Kinases (RTKs) are necessary for numerous cell-signaling events which promote cell growth and replication. RTK-1 activation leads to signaling through Ras/Rap/MAPK pathway.

A rare mutation resulting in a constitutively active form of RTK-1 causes a rare form of leukemia. Using a drug which binds close to an ATP binding pocket prevents tumor growth.

How might this drug alter RTK-1 activity?

A

The drug increases RTK-1 activity by facilitating the transfer of phosphate to a serine residue on RTK-1.

B

The drug decreases RTK-1 activity by inhibiting the binding of ATP in its proper binding pocket.

C

The drug increases RTK-1 activity by facilitating autophosphorylation, a common method of tyrosine kinase receptor activation.

D

The drug transiently increases RTK-1 activity followed by a continued decrease of activity by facilitating receptor desensitization.