Main > ENDOCRINOLOGY > Diabetes. Treatment > Insulin. Mimetics. > HeteroCyclic Quinone Deriv. > Co.: USA. M (Discovery/Patents) > Mechanism of Action

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Researchers designed an assay to identify agents that interact with & activate the insulin receptor. The new drug candidate works through a unique mechanism distinct from other known oral agents.
The insulin receptor is a large protein that traverses the cell membrane. The part that lies within the cell is actually an enzyme that catalyzes the transfer of phosphate from ATP to tyrosine residues on proteins. When insulin binds to the portion of the receptor that sits outside the cell, it switches the enzyme to its active conformation, triggering a series of protein phosphorylations that ultimately control the uptake of glucose.
Experiments suggests that new compd binds to the inside-
the-cell part of the insulin receptor near its ATP binding site, satabilizing the enzyme s active conformation. The new agent turns on the insulin receptor like insulin, but does so in a different way. The compd appears to act selectively, not activating other phosphate-transfer enzymes


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