Kinase_Lecture_MedChem2

Lies opposite the ribose binding pocket the

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Unformatted text preview: ve Form αC helix N- lobe C- lobe Ac5va5on loop Phosphoryla5on of PKB (Akt)'s Ac5va5on Loop Stabilizes Ac5ve Form αC helix N- lobe C- lobe Ac5va5on loop Kinase Inhibitors Protein Kinases ATP binding site Gln-767 H2 OC N H C Leu-768 3 H3 C Met-769 H3 C S Hydrophobic pocket H N O H N HBD H O N N HBA H H CleJ N N N O O H H H OH H OH Ribose pocket OP OP O O O OP N O O O O Gln-767 H2 OC N Protein Kinases ATP binding site H C Leu-768 3 H3C O Met-769 C H 3 S Hydrophobic pocket H N O H N HBD H N N HBA H H CleJ N N N O O H H OP O O H OH OP O O O OP N O H OH Ribose pocket • Purine base is buried deep into the binding site • Purine forms two hydrogen bonding interac4ons to the binding site • Ribose sugar binds to a ‘ribose binding pocket’ • Triphosphate chain lies along a cleJ towards the enzyme surface • Triphosphate interacts with two metal ions and amino acids • Specificity surface is an area of unoccupied binding site • An empty hydrophobic pocket lies opposite the ribose binding pocket • The gatekeeper residue is an amino acid situated at the entrance to the hydr...
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