A structural and thermodynamic escape mechanism from a drug resistant mutation of the HIV‐1 protease

  title={A structural and thermodynamic escape mechanism from a drug resistant mutation of the HIV‐1 protease},
  author={Sonia Vega and L. Kang and A. Vel{\'a}zquez-Campoy and Y. Kiso and L. M. Amzel and E. Freire},
  journal={Proteins: Structure},
  • Sonia Vega, L. Kang, +3 authors E. Freire
  • Published 2004
  • Chemistry, Medicine
  • Proteins: Structure
  • The efficacy of HIV‐1 protease inhibition therapies is often compromised by the appearance of mutations in the protease molecule that lower the binding affinity of inhibitors while maintaining viable catalytic activity and substrate affinity. The V82F/I84V double mutation is located within the binding site cavity and affects all protease inhibitors in clinical use. KNI‐764, a second‐generation inhibitor currently under development, maintains significant potency against this mutation by… CONTINUE READING
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