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2 genotype; 12-week suppression rates are 90% (INSTI-susceptible [INSTI-S] virus) and 35% (INSTI-R viru
4 hydro-1,8-naphthyridine-3-carboxamides as an INSTI scaffold, making a limited set of derivatives, and
7 ore potential interactions between NNRTI and INSTI resistance mutations, we investigated the combined
8 inhibition of the 3'-processing reaction by INSTIs and how INSTIs can be modified to overcome drug r
9 of bictegravir, a novel, potent, once-daily INSTI designed to improve on existing INSTI options with
10 rate envelope concept that broadly effective INSTIs can be designed by filling the envelope defined b
12 -daily INSTI designed to improve on existing INSTI options with the backbone of emtricitabine and ten
16 the 3'-processing reaction by INSTIs and how INSTIs can be modified to overcome drug resistance, nota
18 eration integrase strand transfer inhibitor (INSTI), was recently approved for use in the treatment o
19 smitted integrase strand transfer inhibitor (INSTI)-resistant (INSTI-R) virus is estimated at 0.1%.
20 ence of integrase strand transfer inhibitor (INSTI)-transmitted drug resistance (TDR) may increase wi
21 d integrase (IN) strand transfer inhibitors (INSTI) are key components of antiretroviral regimens.
22 1 integrase (IN) strand transfer inhibitors (INSTIs) approved by the FDA for the treatment of AIDS.
27 s were proven IN strand transfer inhibitors (INSTIs) that also displayed activity against ribonucleas
30 which act as IN strand transfer inhibitors (INSTIs), were the first anti-IN drugs to be approved by
31 tter efficacy against a broad panel of known INSTI resistant mutants than any analogues we have previ
33 ial HIV-1 treatment with bictegravir-a novel INSTI with a high in-vitro barrier to resistance and low
37 inically preferred unless DTG suppression of INSTI-R virus was <20% or 96-week DRV/r suppression was
38 examining the role of the MBG in a series of INSTIs, we have identified a scaffold (hydroxypyrones) t
41 tion that mutant viruses carrying NNRTI plus INSTI resistance mutations had reduced amounts of virion
44 ing, all patients are diagnosed with INSTI-S/INSTI-R virus prior to ART initiation and start DTG- or
48 Bictegravir, a novel, once-daily, unboosted INSTI, showed potent activity in a 10 day monotherapy st
49 weeks undergo IR testing; if diagnosed with INSTI-R virus, they change to ritonavir-boosted darunavi
50 IR testing, all patients are diagnosed with INSTI-S/INSTI-R virus prior to ART initiation and start
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