ol6b02751_si_001.pdf (738.94 kB)
Synthetic Route to Human Relaxin‑2 via Iodine-Free Sequential Disulfide Bond Formation
journal contribution
posted on 2016-10-18, 00:00 authored by Xu Yang, Vasily Gelfanov, Fa Liu, Richard DiMarchiA 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.
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Relaxininsertionrelaxin B-chain assemblyiodineSynthetic Routeabsencesequential disulfide bond formation processthiolB chainpenicillin G acylase-labile PhacmcombinationsolubilityactivatorIodine-Free Sequential Disulfide Bond Formationrelaxin -2isoacyl dipeptide segmentsresincysteine protectionHumanchallenge
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