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Sökning: WFRF:(Turner Mark A) > Turner J > Biocatalysis in Dru...

Biocatalysis in Drug Design: Engineered Reductive Aminases (RedAms) Are Used to Access Chiral Building Blocks with Multiple Stereocenters

Casamajo, Arnau Rué (författare)
Department of Chemistry, UniDepartment of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, United Kingdom
Yu, Yuqi (författare)
Department of Chemistry, UnDepartment of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, United Kingdom
Schnepel, Christian (författare)
KTH,Industriell bioteknologi
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Morrill, Charlotte (författare)
Department of Chemistry, University of Manchester, Manchester Institute of BiotechnologDepartment of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, United Kingdom
Barker, Rhys (författare)
Department of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, United Kingdom
Levy, Colin W. (författare)
Department of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, United Kingdom
Finnigan, James (författare)
Department of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, United Kingdom
Spelling, Victor (författare)
Early Chemical Development, Pharmaceutical Sciences, Biopharmaceuticals R&D, AstraZeneca, Mölndal, Gothenburg, 431 50, Sweden
Westerlund, Kristina (författare)
Medicinal Chemistry, Research and Early Development; Cardiovascular, Renal and Metabolism, Biopharmaceuticals R&D, AstraZeneca, Pepparedsleden 1, Mölndal, 431 50 Gothenburg Sweden
Petchey, Mark (författare)
Compound Synthesis and Management, Discovery Sciences, Biopharmaceuticals R&D, AstraZeneca, Mölndal, Gothenburg, 431 50, Sweden
Sheppard, Robert J. (författare)
Medicinal Chemistry, Research and Early Development; Cardiovascular, Renal and Metabolism, Biopharmaceuticals R&D, AstraZeneca, Pepparedsleden 1, Mölndal, 431 50 Gothenburg Sweden
Lewis, Richard J. (författare)
Department of Medicinal Chemistry, Research and Early Development, Respiratory and Immunology (R&I), BioPharmaceuticals R&D, AstraZeneca, Sweden
Falcioni, Francesco (författare)
Early Chemical Development, Pharmaceutical Sciences, Biopharmaceuticals R&D, AstraZeneca, Cambridge, CB21 6GP, United Kingdom
Hayes, Martin A. (författare)
Compound Synthesis and Management, Discovery Sciences, Biopharmaceuticals R&D, AstraZeneca, Mölndal, Gothenburg, 431 50, Sweden
Turner, Nicholas J. (författare)
Department of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, United Kingdom
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 (creator_code:org_t)
NA, 2023
2023
Engelska.
Ingår i: Journal of the American Chemical Society. - : NA. - 0002-7863 .- 1520-5126. ; 145:40, s. 22041-22046
Relaterad länk:
https://doi.org/10.1...
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https://urn.kb.se/re...
https://doi.org/10.1...
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  • Tidskriftsartikel (refereegranskat)
Abstract Ämnesord
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  • Novel building blocks are in constant demand during the search for innovative bioactive small molecule therapeutics by enabling the construction of structure-activity-property-toxicology relationships. Complex chiral molecules containing multiple stereocenters are an important component in compound library expansion but can be difficult to access by traditional organic synthesis. Herein, we report a biocatalytic process to access a specific diastereomer of a chiral amine building block used in drug discovery. A reductive aminase (RedAm) was engineered following a structure-guided mutagenesis strategy to produce the desired isomer. The engineered RedAm (IR-09 W204R) was able to generate the (S,S,S)-isomer 3 in 45% conversion and 95% ee from the racemic ketone 2. Subsequent palladium-catalyzed deallylation of 3 yielded the target primary amine 4 in a 73% yield. This engineered biocatalyst was used at preparative scale and represents a potential starting point for further engineering and process development.

Ämnesord

NATURVETENSKAP  -- Kemi -- Organisk kemi (hsv//swe)
NATURAL SCIENCES  -- Chemical Sciences -- Organic Chemistry (hsv//eng)

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