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An optimized chemical synthesis of human relaxin-2

Kostas K Barlos1, Dimitrios Gatos, Zoe Vasileiou

  • 1Department of Chemistry, University of Patras, Rion-Patras, Greece. barlos@cblpatras.gr

Journal of Peptide Science : an Official Publication of the European Peptide Society
|March 2, 2010
PubMed

Insights

Researchers developed a novel method for synthesizing human relaxin (RLX), a crucial hormone for pregnancy and cardiovascular health. This improved solid-phase synthesis overcomes previous challenges, enabling efficient production of RLX for therapeutic applications.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Endocrinology

Background:

  • Human relaxin (RLX) is a multifunctional hormone in the insulin superfamily.
  • RLX plays vital roles in pregnancy, aging, fibrosis, cardioprotection, vasodilation, inflammation, and angiogenesis.
  • RLX is under investigation for treating acute heart failure, fibrosis, and preeclampsia.

Purpose of the Study:

  • To overcome difficulties in chemical synthesis of RLX, particularly the insolubility of its B-chain.
  • To develop an efficient method for site-directed combination of RLX's A and B chains.
  • To improve the yield and purity of synthetic RLX for potential clinical use.

Main Methods:

  • Oxidation of the Met(25) residue in the RLX B-chain (RLXB) to improve solubility.
  • Solid-phase synthesis of the modified B-chain (RLXBO).
  • Random interchain combination of RLXBO with bicyclic A-chain (bcRLXA) isomers to achieve native interchain linkage.

Main Results:

  • Oxidation of Met(25) significantly enhanced the solubility of RLXB.
  • The modified B-chain (RLXBO) enabled effective solid-phase synthesis and interchain combination.
  • Met(O)(25)-RLX (RLXO) was synthesized in 62% yield and converted to native RLX in 78% yield via reduction.

Conclusions:

  • The novel oxidation strategy provides an efficient route for chemical synthesis of human relaxin.
  • This method overcomes previous limitations in RLX production, facilitating its therapeutic development.
  • Improved synthesis of RLX holds promise for treating various medical conditions.

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