[3D] Mechanism of Iressa Drug Resistance

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Protein kinases are a group of enzymes that transfer a phosphate from a molecule, such as the cofactor ATP, to one or more amino acid residues in a signaling protein. Over-functioning results in uncontrollable growth of cells, a tumor formation. ATP binds in the ATP-binding site of the tyrosine kinase domain and makes 2 important hydrogen bonds to the protein. A threonine side-chain at position 790 is present in the binding interaction. The binding of ATP to the tyrosine kinase domain of the protein leads to phosphorylation of the tyrosine residue, and as a result, proliferation of cells. The drug Iressa or Gefitinib is a Tyrosine Kinase inhibitor that blocks the binding of ATP, and thus no phosphorylation. Although it is similar in size, Iressa does not resemble the structure of the ATP molecule, but the drug binds in the ATP-binding pocket and prevents the protein from phosphorylation.

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Education

Tags:

• pharmacy
• Mechanism (biology)
• drug
• Pharmaceutical Drug
• iressa
• Drug Resistance
• Mutation
• yt3d:metadata=user

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