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Halogenase engineering and its utility in medicinal chemistry
Abstract
Halogenation is commonly used in medicinal chemistry to improve the potency of pharmaceutical leads. While synthetic methods for halogenation present selectivity and reactivity challenges, halogenases have evolved over time to perform selective reactions under benign conditions. The optimization of halogenation biocatalysts has utilized enzyme evolution and structure-based engineering alongside biotransformation in a variety of systems to generate stable site-selective variants. The recent improvements in halogenase-catalyzed reactions has demonstrated the utility of these biocatalysts for industrial purposes, and their ability to achieve a broad substrate scope implies a synthetic tractability with increasing relevance in medicinal chemistry.
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“Nonetheless, fluorinase has been successfully leveraged in biosynthetic pathways to produce a variety of simple organofluorines used as PET tracers and medical imaging agents58–60.”
From The link between ancient microbial fluoride resistance mechanisms and bioengineering organofluorine degradation or synthesis (2024) · cites this paper as [58]
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Research works printed but not linked: 1
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Cited by
Stockbridge, R. B., & Wackett, L. P. (2024) · Nature Communications · doi:10.1038/s41467-024-49018-1 · Cited by 80
Metadata
- Authors
- Fraley, A. E., & Sherman, D. H.
- Venue
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier BV
- Published
- 2018-06
- Volume
- 28
- Issue
- 11
- Pages
- 1992-1999
- ISSN
- 0960-894X
- PMC
- PMC5964047
- Cited by
- 45
- References
- 71
- Language
- en
- Licence
- www.elsevier.com/tdm/userlicense/1.0/ (tdm)
- www.elsevier.com/legal/tdmrep-license (tdm)
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