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Rational mutagenesi...
Rational mutagenesis of pig liver esterase (PLE-1) to resolve racemic clopidogrel
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- Gaber, Yasser (författare)
- Lund University,Lunds universitet,Bioteknik,Centrum för tillämpade biovetenskaper,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biotechnology,Center for Applied Life Sciences,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH,Beni-Suef University
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- Ismail, Mohamed (författare)
- Lund University,Lunds universitet,Bioteknik,Centrum för tillämpade biovetenskaper,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biotechnology,Center for Applied Life Sciences,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH,Helwan University
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- Bisagni, Serena (författare)
- Lund University,Lunds universitet,Bioteknik,Centrum för tillämpade biovetenskaper,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biotechnology,Center for Applied Life Sciences,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Takwa, Mohamad (författare)
- Lund University,Lunds universitet,Bioteknik,Centrum för tillämpade biovetenskaper,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biotechnology,Center for Applied Life Sciences,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Hatti-Kaul, Rajni (författare)
- Lund University,Lunds universitet,Bioteknik,Centrum för tillämpade biovetenskaper,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biotechnology,Center for Applied Life Sciences,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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(creator_code:org_t)
- Elsevier BV, 2015
- 2015
- Engelska 7 s.
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Ingår i: Journal of Molecular Catalysis B: Enzymatic. - : Elsevier BV. - 1873-3158 .- 1381-1177. ; 122, s. 156-162
- Relaterad länk:
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http://dx.doi.org/10...
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https://lup.lub.lu.s...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Clopidogrel is an important and widely used antiplatelet drug; only the (S)-isomer is the active biological enantiomer. The industrial production of the active enantiomer involves resolution of the racemic compound using stoichiometric amounts of L-camphor sulphonic acid and crystallization in a process using large amounts of solvent. In the present study, the possibility of enzyme catalysed kinetic resolution was investigated. Screening of a number of hydrolytic enzymes showed the crude pig liver esterase (PLE) to exhibit modest enantioselectivity in the hydrolysis of racemic clopidogrel. Molecular modeling simulations were applied on the homology model of PLE-1, the major isoenzyme in the crude PLE, and distinct sites of mutations were proposed and 'produced in the laboratory. The PLE-1 variants with one mutation i.e. PLE-1-F407L and PLE-1-F407I resolved the racemic substrate yielding the (R)-isomer with E value >100. Contrarily, the isoenzyme PLE-3 resolved the racemic substrate yielding (S)-clopidogrel with E value of 10. (C) 2015 Elsevier B.V. All rights reserved.
Ämnesord
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Nyckelord
- Clopidogrel
- Kinetic resolution
- Molecular modeling
- Enantioselectivity
- Esterase
Publikations- och innehållstyp
- art (ämneskategori)
- ref (ämneskategori)
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