Mechanism of Adefovir, Tenofovir and Entecavir Resistance: Molecular Modeling Studies of How A Novel Anti-HBV Agent (FMCA) Can Overcome the Drug Resistance.
Abstract: In this regard, homology modeled structure of HBV polymerase was used for minimization, conformational search and Glide XP docking followed by binding energy calculation on wild-type as well as on mutant HBV-polymerases (N236T, L180M+M204V+S202G & A194T).
A novel pyridazinone derivative inhibits hepatitis B virus replication by inducing genome-free capsid formation.
PMID: 26349829
2015
Antimicrobial agents and chemotherapy
Abstract: Both the 3TC/ETV dually resistant L180M/M204I mutant and the adefovir (ADV)-resistant A181T/N236T mutant were as susceptible to 3711 as wild-type HBV.
Efficacy of tenofovir disoproxil fumarate therapy in nucleoside-analogue naive Iranian patients treated for chronic hepatitis B.
Result: No patient harbored previously described amino acid substitutions, including substitutions that could be associated with reduced TDF susceptibility (rtA181V/T, rtN236T or rtA194T).
Novel natural mutations in the hepatitis B virus reverse transcriptase domain associated with hepatocellular carcinoma.
Result: It is worth noting that we did not observe any of the common NA-related resistance mutations including rtM204V/I, rtS202C/G/I, rtL180M, rtA181T/V, rtT184A/I/L/G/C/M, rtA194T, rtI169T, rtV173L, rtL80I, rtN236T, and PMID: 24517926
2014
Antiviral therapy
Abstract: Patients with primary ADV-R mutations had either A181T/V or N236T mutations or both.
Screening and identification of a novel adefovir dipivoxil resistance associated mutation, rtN236V, of HBV from a large cohort of HBV-infected patients.
Abstract: rtN236V mutants from patient 1 and patient 2 exhibited 3.90-fold and 3.10-fold decreased susceptibility to ADV, respectively, compared to the wild-type virus; by contrast, rtN236T mutants from the patients had 4.50-fold and 4.75-fold decreased susceptibility, respectively.
Abstract: RESULTS: rtN236V was detected in six ADV-refractory patients; signature ADV-resistant mutations rtA181V and rtN236T were detected in 1,311 patients.
Mutation profiling of the hepatitis B virus strains circulating in North Indian population.
Discussion: rtN236T a primary mutation in the D domain, rtA181T/V at the B domain and rtQ215S at the C-D inter-domain have been associated with Adefovir and Lamivudine resistance were also observed in 8 cases.
Lamivudine and Adefovir Motif Variants Detected in chronic Hepatitis B patients.
Abstract: All rtA181V+rtN236T isolates conferred reduced susceptibility to ADV (FC values 2.3-4.2).
Abstract: CONCLUSIONS: Genotype B, C and D isolates with single ADV resistance mutations remained fully sensitive to TFV, while the double mutants rtA181T+rtN236T and rtA181V+rt
Abstract: Clinical isolates containing the rtA181T+rtN236T double mutant remained sensitive to TFV in genotype D but exhibited reduced susceptibility to TFV in genotypes B and C.
Long-term efficacy and emergence of multidrug resistance in patients with lamivudine-refractory chronic hepatitis B treated by combination therapy with adefovir plus lamivudine.
Abstract: HBV DNA levels of patients with rtA181S mutation at baseline and emergence of rtA181T + rtN236T double mutation or a wide variety of mutations during combination therapy could not be suppressed.
HBV mutation literature information.
PMID: 
2015
Current medicinal chemistry
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