Well-defined homopolypeptides, copolypeptides, and hybrids of poly(l-proline)

Biomacromolecules. 2011 Jun 13;12(6):2396-406. doi: 10.1021/bm200495n. Epub 2011 May 25.

Abstract

l-Proline is the only, out of 20 essential, amino acid that contains a cyclized substituted α-amino group (is formally an imino acid), which restricts its conformational shape. The synthesis of well-defined homo- and copolymers of l-proline has been plagued either by the low purity of the monomer or the inability of most initiating species to polymerize the corresponding N-carboxy anhydride (NCA) because they require a hydrogen on the 3-N position of the five-member ring of the NCA, which is missing. Herein, highly pure l-proline NCA was synthesized by using the Boc-protected, rather than the free amino acid. The protection of the amine group as well as the efficient purification method utilized resulted in the synthesis of highly pure l-proline NCA. The high purity of the monomer and the use of an amino initiator, which does not require the presence of the 3-N hydrogen, led for the first time to well-defined poly(l-proline) (PLP) homopolymers, poly(ethylene oxide)-b-poly(l-proline), and poly(l-proline)-b-poly(ethylene oxide)-b-poly(l-proline) hybrids, along with poly(γ-benzyl-l-glutamate)-b-poly(l-proline) and poly(Boc-l-lysine)-b-poly(l-proline) copolypeptides. The combined characterization (NMR, FTIR, and MS) that results for the l-proline NCA revealed its high purity. In addition, all synthesized polymers exhibit high molecular and compositional homogeneity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anhydrides / chemistry*
  • Biocompatible Materials / chemical synthesis*
  • Circular Dichroism
  • Drug Carriers / chemical synthesis*
  • Lysine / analogs & derivatives
  • Lysine / chemistry
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Molecular Conformation
  • Peptides / chemical synthesis*
  • Polyethylene Glycols / chemistry
  • Proline / analogs & derivatives*
  • Proline / chemistry
  • Spectroscopy, Fourier Transform Infrared
  • Temperature

Substances

  • Anhydrides
  • Biocompatible Materials
  • Drug Carriers
  • Peptides
  • proline N-carboxyanhydride
  • epsilon-tert-butyloxycarbonyl-lysine
  • polyproline
  • Polyethylene Glycols
  • Proline
  • Lysine