Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.

In this study, we investigated the influence of single nucleotide polymorphisms on the conformation of mutated cytochrome P450 (CYP) 2B6 proteins using molecular dynamics (MD) simulation. Some of these mutations influence drug metabolism activities, leading to individual variations in drug efficacy...

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Main Authors: Kana Kobayashi, Ohgi Takahashi, Masahiro Hiratsuka, Noriyuki Yamaotsu, Shuichi Hirono, Yurie Watanabe, Akifumi Oda
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2014-01-01
Series:PLoS ONE
Online Access:https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0096789&type=printable
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author Kana Kobayashi
Ohgi Takahashi
Masahiro Hiratsuka
Noriyuki Yamaotsu
Shuichi Hirono
Yurie Watanabe
Akifumi Oda
author_facet Kana Kobayashi
Ohgi Takahashi
Masahiro Hiratsuka
Noriyuki Yamaotsu
Shuichi Hirono
Yurie Watanabe
Akifumi Oda
author_sort Kana Kobayashi
collection DOAJ
description In this study, we investigated the influence of single nucleotide polymorphisms on the conformation of mutated cytochrome P450 (CYP) 2B6 proteins using molecular dynamics (MD) simulation. Some of these mutations influence drug metabolism activities, leading to individual variations in drug efficacy and pharmacokinetics. Using computational docking, we predicted the structure of the complex between the antimalarial agent artemether and CYP2B6 whose conformations were obtained by MD simulation. The simulation demonstrated that the entire structure of the protein changes even when a single residue is mutated. Moreover, the structural flexibility is affected by the mutations and it may influence the enzyme activity. The results suggest that some of the inactive mutants cannot recognize artemether due to structural changes caused by the mutation.
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institution DOAJ
issn 1932-6203
language English
publishDate 2014-01-01
publisher Public Library of Science (PLoS)
record_format Article
series PLoS ONE
spelling doaj-art-2d4d283b6cb8404993e63bf7408456482025-08-20T03:00:27ZengPublic Library of Science (PLoS)PLoS ONE1932-62032014-01-0195e9678910.1371/journal.pone.0096789Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.Kana KobayashiOhgi TakahashiMasahiro HiratsukaNoriyuki YamaotsuShuichi HironoYurie WatanabeAkifumi OdaIn this study, we investigated the influence of single nucleotide polymorphisms on the conformation of mutated cytochrome P450 (CYP) 2B6 proteins using molecular dynamics (MD) simulation. Some of these mutations influence drug metabolism activities, leading to individual variations in drug efficacy and pharmacokinetics. Using computational docking, we predicted the structure of the complex between the antimalarial agent artemether and CYP2B6 whose conformations were obtained by MD simulation. The simulation demonstrated that the entire structure of the protein changes even when a single residue is mutated. Moreover, the structural flexibility is affected by the mutations and it may influence the enzyme activity. The results suggest that some of the inactive mutants cannot recognize artemether due to structural changes caused by the mutation.https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0096789&type=printable
spellingShingle Kana Kobayashi
Ohgi Takahashi
Masahiro Hiratsuka
Noriyuki Yamaotsu
Shuichi Hirono
Yurie Watanabe
Akifumi Oda
Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.
PLoS ONE
title Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.
title_full Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.
title_fullStr Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.
title_full_unstemmed Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.
title_short Evaluation of influence of single nucleotide polymorphisms in cytochrome P450 2B6 on substrate recognition using computational docking and molecular dynamics simulation.
title_sort evaluation of influence of single nucleotide polymorphisms in cytochrome p450 2b6 on substrate recognition using computational docking and molecular dynamics simulation
url https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0096789&type=printable
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