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Stabilized polypeptides as regulators of RAB GTPase function

机译:稳定的多肽作为RAB GTPase功能的调节剂

摘要

The present invention provides inventive polypeptides comprising a C terminal RAB binding domain (RabBD) of RAB family interacting proteins (FIPs) stabilized by peptide stapling, and pharmaceutical compositions thereof. Also provided are methods for modulating RAB function comprising contacting an inventive stapled polypeptide with a RAB protein, and methods of treatment associated with modulation of RAB activity. The present invention also provides methods of making the inventive stapled polypeptides by ring closing metathesis of unstapled polypeptide precursors.
机译:本发明提供了本发明的多肽,其包含通过肽钉合稳定的RAB家族相互作用蛋白(FIP)的C端RAB结合结构域(RabBD),及其药物组合物。还提供了调节RAB功能的方法,其包括使本发明的装订多肽与RAB蛋白接触,以及与调节RAB活性相关的治疗方法。本发明还提供了通过无钉多肽前体的闭环易位来制备本发明的钉多肽的方法。

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