TY - DATA T1 - Synthetic Route to Human Relaxin‑2 via Iodine-Free Sequential Disulfide Bond Formation PY - 2016/10/18 AU - Xu Yang AU - Vasily Gelfanov AU - Fa Liu AU - Richard DiMarchi UR - https://acs.figshare.com/articles/journal_contribution/Synthetic_Route_to_Human_Relaxin_2_via_Iodine-Free_Sequential_Disulfide_Bond_Formation/4039806 DO - 10.1021/acs.orglett.6b02751.s001 L4 - https://ndownloader.figshare.com/files/6503940 KW - Relaxin KW - insertion KW - relaxin B-chain assembly KW - iodine KW - Synthetic Route KW - absence KW - sequential disulfide bond formation process KW - thiol KW - B chain KW - penicillin G acylase-labile Phacm KW - combination KW - solubility KW - activator KW - Iodine-Free Sequential Disulfide Bond Formation KW - relaxin -2 KW - isoacyl dipeptide segments KW - resin KW - cysteine protection KW - Human KW - challenge N2 - 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. ER -