title: Synthetic Route to Human Relaxin-2 via Iodine-Free Sequential Disulfide Bond Formation.
abstract: A new synthetic route to human relaxin-2 has been established through a sequential disulfide bond formation process in the absence of iodine. It is enabled by a combination of cysteine protection with penicillin G acylase-labile Phacm and a newly identified thiol activator bis(5-(2-methoxyethoxy)-2-pyrimidinyl disulfide. The long-standing challenges in relaxin B-chain assembly and its poor solubility have been solved by the insertion of two isoacyl dipeptide segments. The overall yield was 25% from the B chain and 5.8% from the B-chain starting resin.
authors.affiliation: Department of Chemistry, Indiana University , Bloomington, Indiana 47405, United States.
authors.forename: Xu
authors.initials: X
authors.lastname: Yang
authors.affiliation: Novo Nordisk Research Center Indianapolis, Indianapolis, Indiana 46241, United States.
authors.forename: Vasily
authors.initials: V
authors.lastname: Gelfanov
authors.affiliation: Novo Nordisk Research Center Indianapolis, Indianapolis, Indiana 46241, United States.
authors.forename: Fa
authors.initials: F
authors.lastname: Liu
authors.affiliation: Department of Chemistry, Indiana University , Bloomington, Indiana 47405, United States.|Novo Nordisk Research Center Indianapolis, Indianapolis, Indiana 46241, United States.
authors.forename: Richard
authors.initials: R
authors.lastname: DiMarchi
mesh_terms: D002851:Chromatography, High Pressure Liquid; D004220:Disulfides / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D007455:Iodine / Q000737:chemistry; D015394:Molecular Structure; D012065:Relaxin / Q000138:chemical synthesis* / Q000737:chemistry; D012995:Solubility
chemical_list: D004220:Disulfides; C095068:RLN2 protein, human; D012065:Relaxin; D007455:Iodine