Method: NNRTI-selected mutations included A98G, L100I, K101E/P/N/H, K103N/S, V106A/M, V108I, V179D/E, Y181C/I/V, Y188L/C/H, G190A/S/E/Q, P225H, F227L, M230L, P236L, and K238T.
Result: L74V was associated with the NNRTI-resistance mutations L100I
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
PMID: 17803291
2007
Journal of medicinal chemistry
Abstract: Compound 16 was exceptionally potent against RT WT and RTs carrying the K103N, Y181I, and L100I mutations.
Design, synthesis and biological evaluation of a series of thioamides as non-nucleoside reverse transcriptase inhibitors.
PMID: 18045200
2007
Medicinal chemistry (Shariqah (United Arab Emirates))
Abstract: While compound (2) exhibited activity against the mutant strain L100I with IC(50) of 70.1 microM, compound (4) showed activity against the mutant strain K103N with IC(50) of 92.7 microM, and compound (8) with activity against the wild type enzyme with IC(50) of 8.9 microM.
In vitro selection of mutations in human immunodeficiency virus type 1 reverse transcriptase that confer resistance to capravirine, a novel nonnucleoside reverse transcriptase inhibitor.
Abstract: However, exposure to abacavir and/or efavirenz, presence of Q151M and/or L100I, and prior AIDS may favor the selection of this mutation.
Abstract: Moreover, the L100I mutation was independently associated with a higher probability of presenting K65R.
Interaction kinetic characterization of HIV-1 reverse transcriptase non-nucleoside inhibitor resistance.
PMID: 16610781
2006
Journal of medicinal chemistry
Abstract: The K103N and the L100I substitutions were found to facilitate both the entry of the inhibitor into the binding pocket as well as its exit, in contrast to what has been reported elsewhere.
Abstract: The Y181C, V108I, and P225H substitutions affected primarily the association and dissociation rate constants, while the K103N and the L100I substitutions also influenced the equilibrium between the two forms of the free enzyme.
L74V increases the reverse transcriptase content of HIV-1 virions with non-nucleoside reverse transcriptase drug-resistant mutations L100I+K103N and K101E+G190S, which results in increased fitness.
Abstract: K103N + L100I had a greater reduction in fitness and was less fit than K103N + V108I and K103N + P225H.
Abstract: K103N + L100I is the most drug-resistant of the double mutants but is the least common clinically.
Abstract: K103N, L100I, and P225H w
Abstract: In the presence of efavirenz, L100I was less fit than K103N, and K103N + L100I was more fit than K103N + V108I.
Emergence of antiretroviral therapy resistance-associated primary mutations among drug-naive HIV-1-infected individuals in rural western Cameroon.
PMID: 16885781
2006
Journal of acquired immune deficiency syndromes (1999)
Abstract: Reverse transcriptase inhibitor-associated primary resistance mutations were found in 5 (9.8%) samples: Y188C in 2 cases, and L100I, M184V, and V75I in 1 case each, although all of these mutations were found as minor populations.
Arylthiopyrrole (AThP) derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis, structure-activity relationships, and docking studies (part 2).
Abstract: This compound and its precursor 18b retained interesting activities against clinically relevant drug-resistant RT forms carrying K103N, Y181I, and L100I mutations.
Early virological failure in treatment-naive HIV-infected adults receiving didanosine and tenofovir plus efavirenz or nevirapine.