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Description
  • CYP450 2D6 is a relatively flexible protein with plastic active site structure, allowing binding with high specificity of many different substrates of various sizes. Presence of a basic nitrogen atom at a distance of 5-7 ? from the site of metabolism is often found in the structure of typical substrates. After substrate binding, the active site structure is changed, embracing the substrate and fixing it in the optimal position for enzyme reaction. The alleles found in the human population that correspond to CYP450 2D6 variants with decreased enzymatic activity possess changed amino acids which, interestingly, do not directly participate in forming the active site. Instead, they probably take part in maintaining other properties of the enzyme, for example in the formation of solvent or substrate access channels.
  • CYP450 2D6 is a relatively flexible protein with plastic active site structure, allowing binding with high specificity of many different substrates of various sizes. Presence of a basic nitrogen atom at a distance of 5-7 ? from the site of metabolism is often found in the structure of typical substrates. After substrate binding, the active site structure is changed, embracing the substrate and fixing it in the optimal position for enzyme reaction. The alleles found in the human population that correspond to CYP450 2D6 variants with decreased enzymatic activity possess changed amino acids which, interestingly, do not directly participate in forming the active site. Instead, they probably take part in maintaining other properties of the enzyme, for example in the formation of solvent or substrate access channels. (en)
Title
  • Structural properties of CYP2D6: requirements for substrates and inhibitors
  • Structural properties of CYP2D6: requirements for substrates and inhibitors (en)
skos:prefLabel
  • Structural properties of CYP2D6: requirements for substrates and inhibitors
  • Structural properties of CYP2D6: requirements for substrates and inhibitors (en)
skos:notation
  • RIV/61989592:15110/14:33150428!RIV15-MSM-15110___
http://linked.open...avai/riv/aktivita
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  • I, P(GPP303/12/P019)
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  • 47880
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  • RIV/61989592:15110/14:33150428
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  • CYP2D6 inhibitors; CYP2D6 substrates; active site; cytochromes P450; CYP2D6 (en)
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  • [1203C57636FB]
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  • London
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  • neuveden
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  • CYP2D6: Genetics, Pharmacology and Clinical Relevance
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  • Otyepka, Michal
  • Anzenbacher, Pavel
  • Anzenbacherová, Eva
  • Berka, Karel
number of pages
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  • 10.2217/9781780844626
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  • Future Medicine Ltd.
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  • 978-1-78084-462-6
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  • 15110
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