literature

HBV mutation literature information.

7-Deaza-7-fluoro modification confers on 4'-cyano-nucleosides potent activity against entecavir/adefovir-resistant HBV variants and favorable safety.

PMID: 32084506 2020 Antiviral research

Abstract: Southern blot analysis using wild-type HBV (HBVWT)-encoding-plasmid-transfected HepG2 cells revealed that CdFA efficiently suppresses the production of HBVWT (IC50 = 153.7 nM), entecavir (ETV)-resistant HBV carrying L180M/S202G/M204V substitutions (HBVETVR; IC50 = 373.2 nM), and adefovir dipivoxil (ADV)-resistant HBV carrying A181T/N236T substitutions (HBVADVR; IC50=192.6 nM), whereas ETV and ADV were less potent against HBVETVR and HBVADVR (IC50: >1,000 and 4,02

Result: We then analyzed the interactions of ETV-TP and CdFA-TP with HBV-RT, in which three amino acid substitutions associated with HBV's resistance to ETV (L180M/S202G/M204V) have been introduced (RTETV-R).

Viral quasispecies of hepatitis B virus in patients with YMDD mutation and lamivudine resistance may not predict the efficacy of lamivudine/adefovir rescue therapy.

PMID: 30906435 2019 Experimental and therapeutic medicine

Result: Common and frequent mutations identified in the cohort of the present study included rtL80V/I, rtV84M, rtL91I, rtN118H/D/T, rtT128A, rtL180M, rtT184L/S/A, rtV191I, rtS202G, rtV207I/M, rtS213T

Synthesis of an Anti-hepatitis B Agent, 2'-Fluoro-6'-methylene-carbocyclic Adenosine (FMCA) and Its Phosphoramidate (FMCAP).

PMID: 30589264 2019 The Journal of organic chemistry

Abstract: Furthermore, in vitro, these agents have demonstrated significant activity against lamivudine/entecavir triple mutants (L180M + S202G + M204V).

CMCdG, a Novel Nucleoside Analog with Favorable Safety Features, Exerts Potent Activity against Wild-Type and Entecavir-Resistant Hepatitis B Virus.

PMID: 30670420 2019 Antimicrobial agents and chemotherapy

Abstract: CMCdG also reduced the level of HBVETV-R L180M/S202G/M204V viremia by ~1 log in HBVETV-R L180M/S202G/M204V-infected human liver-chimeric mice, while ETV (1 mg/kg/day q.d.) completely failed to reduce the viremia.

Abstract: CMCdG potently inhibited HBV production in HepG2.2.15 cells (50% inhibitory concentration [IC50], ~30 nM) and HBVWT Ce plasmid-transfected Huh7 cells (IC50, 206 nM) and efficiently suppressed ETV-resistant HBVETV-R L180M/S202G/M204V (IC50, 2,657 nM), while it showed no or little cytotoxicity (50% cytotoxic concentration, >500 muM in most hepatocytic cells examined).

Abstract: CMCdG's in vitro activity was determined using quantitative PCR a

Hepatitis B virus mutation pattern rtL180M+A181C+M204V may contribute to entecavir resistance in clinical practice.

PMID: 30866789 2019 Emerging microbes & infections

Abstract: Patient-derived representative rtA181C-containing mutants, rtL180M+A181C+M204V, rtL180M+A181C+M204V+M250V, and rtL180M+A181C+S202G+M204V, exhibited 45.7%, 25.9%, and 25.0% replication capacity and 85.6-, 356.1-, and 307.1-fold decreased susceptibility to ETV respectively compared to the wild-type strain, while the three mutants remained sensitive to tenofovir (TDF).

Method: Recombinant vectors that harboured a patient-de

Potential resistant mutations within HBV reverse transcriptase sequences in nucleos(t)ide analogues-experienced patients with hepatitis B virus infection.

PMID: 31147594 2019 Scientific reports

Introduction: These two categories are known as classical mutations, which include: (i) M204I/V mutation, which associates with LAM or LDT resistance; (ii) N236T or A181T/V mutations, which associate with ADV resistance; (iii) M204V + L180M and either T184A/G/I/L/S or S202G or M250V to develop resistance to ETV.

Table: S202G

[Determination of reverse transcriptase inhibitor nucleoside analogue resistance profile in pretreatment phase of patients with viral hepatitis B].

PMID: 31130120 2019 Mikrobiyoloji bulteni

Abstract: Primary drug resistance mutations such as rtI169T, rtA181T/V, rtT184A/C/F/G/I/L/M/S, rtA194T, rtS202C/G/I, rtM204I/V/S, rtN236T, rt M250I/L/V and rtV173L were not detected in any of the patient samples.

Prevalence of Hepatitis B Virus Infection in Shenzhen, China, 2015-2018.

PMID: 31558731 2019 Scientific reports

Introduction: A total of 8 HBV classical mutation sites are conventionally tested for HBV patients in most clinical labs, including M204I/V, L180M, T184A/F/I/L/S, L181T/V, M250I/L/V, M236T, S202G, and V207I.

Characterization and Clinical Significance of Natural Variability in Hepatitis B Virus Reverse Transcriptase in Treatment-Naive Chinese Patients by Sanger Sequencing and Next-Generation Sequencing.

PMID: 31189581 2019 Journal of clinical microbiology

Result: Considering that the low sensitivity of Sanger sequencing limited the detection of NAr mutations with a low rate (<20%), 4 classical drug resistance mutations (S202C/G/I, M204I/V/S, N236T, and M250I/L/V) and 12 putative NAr mutations (V207I, S213T, V214A, Q215P/S, L217R, E218D, L229G/V/W/F, I233V, P237H, N/H238D/S/T, Y245H, and S/C256G)

Hepatitis B virus rtA181T/sW172non-stop mutation may increase resistance fold to adefovir- and entecavir-resistant mutants compared to rtA181T/sW172* mutation.

PMID: 29630974 2018 Antiviral research

Abstract: 3.69-fold in half maximal effective concentration of wild-type strain); rtA181T/sW172L + rtS202G + rtM204V strain exhibited higher HBV DNA production and entecavir resistance fold than that of rtA181T/sW172* + rtS202G + rtM204V strain (50.98% vs.

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