TY - JOUR
T1 - Overcoming HIV-1 resistance to protease inhibitors
AU - Freire, Ernesto
N1 - Funding Information:
I thank Dr Salman Muzammil for preparing Fig. 1 and Dr Hiroyasu Ohtaka for helpful discussions. This study was supported by grants from the National Institutes of Health GM 57144 and GM56550 and the National Science Foundation MCB0131241.
PY - 2006
Y1 - 2006
N2 - Protease inhibitors are key components in the chemotherapy of HIV-1 infection. However, despite their success, the appearance of viral mutations routinely compromises their clinical efficacy, creating a constant need for new and better inhibitors. An ideal inhibitor should be able to neutralize the wild type as well as mutants associated with drug resistance with high potency and high selectivity towards human targets, thus minimizing side effects. The evolution of protease inhibitors since 1995 has revealed the basis for extremely high affinity as well as different mechanisms by which inhibitors can escape the deleterious effects of mutations.
AB - Protease inhibitors are key components in the chemotherapy of HIV-1 infection. However, despite their success, the appearance of viral mutations routinely compromises their clinical efficacy, creating a constant need for new and better inhibitors. An ideal inhibitor should be able to neutralize the wild type as well as mutants associated with drug resistance with high potency and high selectivity towards human targets, thus minimizing side effects. The evolution of protease inhibitors since 1995 has revealed the basis for extremely high affinity as well as different mechanisms by which inhibitors can escape the deleterious effects of mutations.
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U2 - 10.1016/j.ddmec.2006.06.005
DO - 10.1016/j.ddmec.2006.06.005
M3 - Review article
AN - SCOPUS:33748514992
SN - 1740-6765
VL - 3
SP - 281
EP - 286
JO - Drug Discovery Today: Disease Mechanisms
JF - Drug Discovery Today: Disease Mechanisms
IS - 2
ER -