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Issue 41, 2020
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Is it time for biocatalysis in fragment-based drug discovery?

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Abstract

The use of biocatalysts for fragment-based drug discovery has yet to be fully investigated, despite the promise enzymes hold for the synthesis of poly-functional, non-protected small molecules. Here we analyze products of the biocatalysis literature to demonstrate the potential for not only fragment generation, but also the enzyme-mediated elaboration of these fragments. Our analysis demonstrates that biocatalytic products can readily populate 3D chemical space, offering diverse catalytic approaches to help generate new, bioactive molecules.

Graphical abstract: Is it time for biocatalysis in fragment-based drug discovery?

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Article information


Submitted
27 Jul 2020
Accepted
07 Oct 2020
First published
07 Oct 2020

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2020,11, 11104-11112
Article type
Perspective

Is it time for biocatalysis in fragment-based drug discovery?

J. I. Ramsden, S. C. Cosgrove and N. J. Turner, Chem. Sci., 2020, 11, 11104 DOI: 10.1039/D0SC04103C

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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