Drug Resistance to HIV-1 Integrase Inhibitors Among Treatment-Naive Patients in Beijing, China.
PMID: 35300056
2022
Pharmacogenomics and personalized medicine
Abstract: Furthermore, one patient having S230R mutation resulted in low-level resistance to RAL, EVG, DTG and BIC.
Result: Among 12 IN-related polymorphic accessory mutations, only E138A, S230R and G16
Result: Furthermore, one patient having S230R mutation resulted in low-level resistance to RAL, EVG, DTG and BIC (as shown in Table 2).
Table: S230R
Discussion: 3 IN-related drug resistance mutations were E138A, S230R and G163R.
Discussion: S230R mutation can lead to potential resistance to CAB and low-level resistance to BIC, DTG, RAL and EVG.
Integrase Inhibitor Resistance Mechanisms and Structural Characteristics in Antiretroviral Therapy-Experienced, Integrase Inhibitor-Naive Adults with HIV-1 Infection Treated with Dolutegravir plus Two Nucleoside Reverse Transcriptase Inhibitors in the DAWNING Study.
PMID: 34694877
2022
Antimicrobial agents and chemotherapy
Table: S230R
Discussion: In the SAILING study, R263K emerged alone in 2 participants and in combination with the integrase substitutions A49G plus S230R in one participant.
HIV Pretreatment Drug Resistance Trends in Mexico City, 2017-2020.
Result: The largest clusters with INSTI PDR transmission were cluster INSTI-1, with 5 nodes sharing the S230R mutation, formed by 4 cisgender men and 1 transgender woman, with median age 23 (20-32); and
Result: The most frequent surveillance drug resistance mutations (SDRMs) were K103NS (6.7%) to NNRTI; M41L (1.2%) and T215CDEF (2.1%) to NRTI; M46IL (1.7%) to PI; and E138AKT (0.2%), Q148HKR (0.1%), and S230R (0.1%) to INSTI (Figure 2a).
Characterizing HIV-1 Genetic Subtypes and Drug Resistance Mutations among Children, Adolescents and Pregnant Women in Sierra Leone.
Result: Polymorphic accessory INSTI-selected mutations, which have minimal effect on INSTI susceptibility were observed in 8 children/adolescents, as follows: T97A (n = 2), E157Q (n = 5), and S230SR (n = 1).
Virologic failure after 48 weeks of raltegravir-based regimen in low HIV-1 incidence setting.
Integrase strand transfer inhibitor (INSTI)-resistance mutations for the surveillance of transmitted HIV-1 drug resistance.
PMID: 31617907
2020
The Journal of antimicrobial chemotherapy
Abstract: Among the 29 relatively common INSTI-selected mutations, 24 emerged as candidates for inclusion on a list of INSTI surveillance drug-resistance mutations: T66A/I/K, E92G/Q, G118R, F121Y, E138A/K/T, G140A/C/S, Y143C/H/R/S, S147G, Q148H/R/K, N155H, S230R and R263K.
HIV-1 acquired drug resistance to integrase inhibitors in a cohort of antiretroviral therapy multi-experienced Mexican patients failing to raltegravir: a cross-sectional study.
Variability in HIV-1 Integrase Gene and 3'-Polypurine Tract Sequences in Cameroon Clinical Isolates, and Implications for Integrase Inhibitors Efficacy.
PMID: 32106437
2020
International journal of molecular sciences
Discussion: The aa substitutions E92Q, S119R, E138A, Y143R, G148H/R, and S230R/N are more prevalent in subtype-B than in non-B subtypes, whereas mutations such as L74I/M, T97A, L101I, E157Q, T214A, and V201I are more prevalent in non-B subtypes compared to HIV-1 subtype B.
Occurrence of the S230R integrase strand inhibitor mutation in a treatment-naive individual case report.
Discussion: Pham et al, using an infectious molecular clone with the insertion of S230R by site-directed mutagenesis, showed that this mutation conferred a 63% reduction of integrase enzyme efficiency and a fold change in mean IC50 of 3.85, 3.72, 1.52, and 1.21 for DTG, cabotegravir, raltegravir.
Discussion: The S230R mutation has been previously described in 2 individuals failing DTG monotherapy in the DOMONO study.
Discussion: These results demonstrated that the S230R substitution caused similar effects on viral repl
Discussion: This lack of detectable phenotypic resistance may have been reflective of the low copy number of virus carrying the S230R mutation (167 copies/mL).
Discussion: and elvitegravir (EVG), respectively, compared to virus lacking S230R.
Raltegravir-Induced Adaptations of the HIV-1 Integrase: Analysis of Structure, Variability, and Mutation Co-occurrence.
Result: Cluster D also has S230N, which is not associated with resistance to RAL; however, another mutation in this position (S230R) is associated with resistance to DTG.
Result: Furthermore, position 230, which may bear the mutation S230R in patients treated with RAL, EVG, or DTG also displays low entropies in both treated and non-treated patients.