Incorporation of Aliphatic Proline Residues into Recombinantly Produced Insulin

ACS Chem Biol. 2023 Dec 15;18(12):2574-2581. doi: 10.1021/acschembio.3c00561. Epub 2023 Nov 14.

Abstract

Analogs of proline can be used to expand the chemical space about the residue while maintaining its uniquely restricted conformational space. Here, we demonstrate the incorporation of 4R-methylproline, 4S-methylproline, and 4-methyleneproline into recombinant insulin expressed in Escherichia coli. These modified proline residues, introduced at position B28, change the biophysical properties of insulin: Incorporation of 4-methyleneproline at B28 accelerates fibril formation, while 4-methylation speeds dissociation from the pharmaceutically formulated hexamer. This work expands the scope of proline analogs amenable to incorporation into recombinant proteins and demonstrates how noncanonical amino acid mutagenesis can be used to engineer the therapeutically relevant properties of protein drugs.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acids / metabolism
  • Escherichia coli / genetics
  • Escherichia coli / metabolism
  • Insulin* / metabolism
  • Models, Molecular
  • Molecular Conformation
  • Proline*

Substances

  • Insulin
  • Proline
  • Amino Acids