The new fate of internalized membrane receptors: Internalized activation

Pharmacol Ther. 2022 May:233:108018. doi: 10.1016/j.pharmthera.2021.108018. Epub 2021 Oct 6.

Abstract

Classically, the fate of internalized membrane receptors includes receptor degradation and receptor recycling. However, recent findings have begun to challenge these views. Much research demonstrated that many internalized membrane receptors can trigger distinct signal activation rather than being desensitized inside the cell. Here, we introduce the concept of "internalized activation" which not only represents a new mode of receptor activation, but also endows the new fate for receptor internalization (from death to life). The new activation mode and fate of membrane receptor are ubiquitous and have unique theoretical significance. We systematically put forward the features, process, and regulation of "internalized activation" and its significance in signal transduction and diseases. "Internalized activation" will provide a completely new understanding for the theory of receptor activation, internalization and novel drug targets for precision medicine.

Keywords: Internalized activation; Receptor activation; Receptor fate; Receptor internalization; Signaling.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Endocytosis*
  • Humans
  • Signal Transduction*