F18, a novel small-molecule nonnucleoside reverse transcriptase inhibitor, inhibits HIV-1 replication using distinct binding motifs as demonstrated by resistance selection and docking analysis.
PMID: 22037848
2012
Antimicrobial agents and chemotherapy
Abstract: Moreover, we induced F18-resistant viruses by in vitro serial passages and found that the mutation L100I appeared to be the dominant contributor to F18 resistance, further suggesting a binding motif different from that of nevirapine and efavirenz.
Multiple drugs and multiple targets: an analysis of the electrostatic determinants of binding between non-nucleoside HIV-1 reverse transcriptase inhibitors and variants of HIV-1 RT.
Prevalence of etravirine resistance associated mutations in HIV-1 strains isolated from infected individuals failing efavirenz: comparison between subtype B and non-B genetic variants.
Abstract: The most prevalent ETR RAMs observed were L100I, V90I, and K101E, with a prevalence of 16.4% (n = 9), 9.1% (n = 5), and 5.5% (n = 3), respectively.
HIV-1 subtype D infections among Caucasians from Northwestern Poland--phylogenetic and clinical analysis.
Result: We also checked population sequences for additional AZT/3TC/NVP-selected resistance mutations like M41L, D67N, K70R, L210W, T215Y/F and K219QE for AZT, K65R for 3TC and L100I, K101P, V106A/M, V108I, Y188C/L/H and G190A for NVP.
Transmitted drug resistance and phylogenetic relationships among acute and early HIV-1-infected individuals in New York City.
PMID: 22592583
2012
Journal of acquired immune deficiency syndromes (1999)
4Method: ARV resistance was defined by mutations at the following positions: M41L, A62V, K65R, D67N, T69ins, K70R, L74VI, Y115F, F116Y, Q151M, M184VI, T210W, T215YF and K219QE for Nucleoside Reverse Transcriptase Inhibitors (NRTI), L100I, K101EP, K103NS, V106AM
Minority variants associated with resistance to HIV-1 nonnucleoside reverse transcriptase inhibitors during primary infection.
Abstract: The 11 RAMs not detected by bulk sequencing were A98G (n=2), L100I (n=3), K101E (n=2), V106I (n=3) and E138G (n=1).
Arylazolyl(azinyl)thioacetanilide. Part 9: Synthesis and biological investigation of thiazolylthioacetamides derivatives as a novel class of potential antiviral agents.
PMID: 22870806
2012
Archives of pharmacal research
Abstract: The results showed that some 2-chloro substituted thiazolylthioacetamide derivatives possessed potent activity against wild type HIV-1 and several key mutant strains (E138K, K103N, L100I) of HIV-1 in MT-4 cells with EC(50) values in micromolar range.
Virological failure rates and HIV-1 drug resistance patterns in patients on first-line antiretroviral treatment in semirural and rural Gabon.
PMID: 23199801
2012
Journal of the International AIDS Society
Result: Major NNRTIs DRMs were also obtained at positions P225H (n=12), K101E (n=11), Y181C (n=10), G190A (n=7), Y188L (n=6), V90I (n=5), E138A/G (n=5), M230L (n=4), A98G (n=3), H221Y (n=3), L100I (n=3), V179D (n=2), and V106I (n=1).