Abstract

We report an intermolecular native chemical ligation-assisted diaminodiacid strategy for the flexible construction of A11Cys-B11Cys disulfide surrogates of H2 relaxin. The practicality of this strategy was evidenced by the synthesis of four new H2 relaxin analogs, among which H2-2a-B28Ile is found to exhibit improved potency, selectivity, and stability compared with native H2 relaxin.

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