10.1021/acs.orglett.6b02751.s001
Xu Yang
Xu
Yang
Vasily Gelfanov
Vasily
Gelfanov
Fa Liu
Fa
Liu
Richard DiMarchi
Richard
DiMarchi
Synthetic Route to Human Relaxin‑2 via Iodine-Free
Sequential Disulfide Bond Formation
American Chemical Society
2016
Relaxin
insertion
relaxin B-chain assembly
iodine
Synthetic Route
absence
sequential disulfide bond formation process
thiol
B chain
penicillin G acylase-labile Phacm
combination
solubility
activator
Iodine-Free Sequential Disulfide Bond Formation
relaxin -2
isoacyl dipeptide segments
resin
cysteine protection
Human
challenge
2016-10-18 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Synthetic_Route_to_Human_Relaxin_2_via_Iodine-Free_Sequential_Disulfide_Bond_Formation/4039806
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 bisÂ(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.