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ABL1 Myristoyl Pocket
- Molecular classification
- Protein Domain, Allosteric regulatory site
01
Overview
The ABL1 myristoyl pocket is a deep hydrophobic cavity located in the C-lobe of the kinase domain of the ABL1 protein. It plays a crucial regulatory role by binding to either an N-terminal myristoyl group or small-molecule inhibitors, which induces conformational changes and stabilizes an autoinhibited state, reducing kinase activity. Targeting this site offers therapeutic potential for overcoming resistance seen with traditional ATP-site tyrosine kinase inhibitors.
- Other names
- Myristoyl-binding pocket of ABL1Myristate-binding pocket of ABL1
02
Mechanism of action
Allosteric inhibition; stabilizes inactive ABL1 conformation
03
Biological functions
Allosteric regulationAutoinhibition maintenanceProtein-protein interaction regulation
04
Disease associations
CancerChronic Myeloid LeukemiaDrug resistance
05
Safety considerations
Potential for off-target effects due to structural similarity with other proteins.Development of resistance to allosteric inhibitors.
06
Interacting drugs
Asciminib (ABL001)
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