literature

HIV mutation literature information.

Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs.

PMID: 20535242 2010 Letters in drug design & discovery

Introduction: (1)) retains activity against HIV-1 containing the single key NNRTI mutations K103N, V106A or L100I.

Introduction: Mutations associated with resistance to NNRTIs include L100I, K101E, K103N, V106A, V108I, V179D, Y181C, Y188C/L/H, G190A/E/S, M230L, P236L and Y318F.

HIV type-1 genotypic resistance profiles in vertically infected patients from Argentina reveal an association between K103N+L100I and L74V mutations.

PMID: 20587857 2010 Antiviral therapy

Abstract: The non-nucleoside K103N+L100I mutations were observed at high frequency (15.5%) and were significantly associated with the nucleoside mutation L74V in BF recombinants.

Abstract: The results provide clinical evidence of a molecular interaction between K103N+L100I and L74V mutations at the reverse transcriptase gene in vivo, limiting the future use of second-generation non-nucleoside reverse transcriptase inhibitors such as etravirine.

Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.

PMID: 20598556 2010 Bioorganic & medicinal chemistry

Abstract: It also proved more active against mutant L100I, K103N, Y188L, and K103N+Y181C RT HIV-1 strains than efavirenz.

Genetic characterization of HIV type 1 among patients with suspected immune reconstitution inflammatory syndrome after initiation of antiretroviral therapy in Kenya.

PMID: 20624074 2010 AIDS research and human retroviruses

Abstract: These included nucleoside reverse transcriptase inhibitor (RTI) mutations: M41L, K65R, D67N, K70R, M184V, and K219Q, and nonnucleoside RTI mutations: K101P, L100I, K103N, and Y181C.

Distinct mutation pathways of non-subtype B HIV-1 during in vitro resistance selection with nonnucleoside reverse transcriptase inhibitors.

PMID: 20805392 2010 Antimicrobial agents and chemotherapy

Abstract: In subtype B viruses, on the other hand, known NNRTI-associated mutations (e.g., Y181C, P236L, L100I, V179D, and K103N) were selected by the NNRTIs.

Update of the drug resistance mutations in HIV-1: December 2010.

PMID: 21245516 2010 Topics in HIV medicine

Abstract: For etravirine, L100I*, K101P*, and Y181C*/I*/V* are denoted with asterisks (instead of bolded) to reflect that these individual mutations each have the greatest impact (ie, highest weighting scores) on reduced phenotypic susceptibility and impaired clinical response when compared with other etravirine mutations (Haddad M et al, CROI, 2010; Abstract 574).

[In vitro selection and identification of HIV strain which is resistance to two new HIV-1 nonnucleoside reverse transcriptase inhibitors].

PMID: 21351434 2010 Yao xue xue bao

Abstract: For JB26, there was a L100I (TTA-->ATA) mutation at passage 10.

Abstract: JB25 had amino acid substitution L100I (TTA-->ATA) at passage 6, and then changed into 100 M (ATA-->ATG) at passage 12, which was rare mutation form and had not been reported.

QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.

PMID: 18457904 2009 European journal of medicinal chemistry

Abstract: Additionally, the results indicate that logP plays a vital role in the prediction of the activity of DAPYs, and the cyano group on the left wing is important for inhibiting the mutant forms L100I and Y188N.

Abstract: For the activity values against HIV-1 RT wild-type and mutant strains (L100I, Y181C and Y188N) of 34 diarylpyrimidines (DAPYs) taken from literature, multiple linear regression analysis and the crossvalidation of Leave-One-Out method are carried out against the activity values with the hydrophobicity index logP, the modified steric parameter L(Y), the Muliken charge of nitrogen atom on the right wing N(C) and the indicator index I for the substituents R(3)' and R(1) on the left wing, and four good QSAR models are established: R=0.8211(N=34), R=0.8599 (N=33), R=

Non-nucleoside HIV-1 reverse transcriptase inhibitors di-halo-indolyl aryl sulfones achieve tight binding to drug-resistant mutants by targeting the enzyme-substrate complex.

PMID: 18984007 2009 Antiviral research

Abstract: By comparing the activities of the different compounds against wild-type RT and the resistant enzymes carrying the single mutations Lys103Asn, Leu100Ile, and Tyr181Ile (K103N, L100I, and Y181I), we found that one compound (RS1914) dissociated from the mutated enzymes almost 10-fold slower than from the wild type RT.

Antiretroviral combinations implicated in emergence of the L74I and L74V resistance mutations in HIV-1-infected patients.

PMID: 19050391 2009 AIDS (London, England)

Abstract: The K103N substitution also plays an important role in the L74I emergence when not associated with the other non-NRTI mutations seen in this study: L100I, G190A and Y181C.

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