Selective P450BM3 Hydroxylation of Cyclobutylamine and Bicyclo[1.1.1]pentylamine Derivatives: Underpinning Synthetic Chemistry for Drug Discovery
Lucy A. Harwood, Ziyue Xiong, Kirsten E. Christensen, Ruiyao Wang, Luet L. Wong, Jeremy Robertson · 2023
Read Selective P450BM3 Hydroxylation of Cyclobutylamine and Bicyclo[1.1.1]pentylamine Derivatives: Underpinning Synthetic Chemistry for Drug Discovery by Lucy A. Harwood, Ziyue Xiong, Kirsten E. Christensen, Ruiyao Wang, Luet L. Wong, Jeremy Robertson (2023) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/pmc-10740007.txt.
Description
Lucy Harwood, Ziyue Xiong, Kirsten Christensen, Ruiyao Wang, Luet Wong, and Jeremy Robertson published a 2023 chemistry study on using engineered enzymes to build drug fragments with precision. Making a family of related compounds from one starting material, each edited at a different spot, saves enormous effort in drug discovery. That needs reagents that can pick one site among many similar ones.
Their panel of engineered P450 enzymes adds a hydroxyl group to ring shaped amine building blocks at unreactive carbon sites. The edits proceed with high selectivity for both position and handedness. The method also handles a bridged bicyclic scaffold prized in modern medicinal chemistry. It achieved the first direct selective edit of that scaffold's bridge, opening a short route to chiral drug building blocks.
Catalog record
| CREATOR | Lucy A. Harwood, Ziyue Xiong, Kirsten E. Christensen, Ruiyao Wang, Luet L. Wong, Jeremy Robertson |
|---|---|
| YEAR | 2023 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 21 KB |
| VERSION | 1.0 |
| LICENSE | CC BY 4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |