HIP1R targets PD-L1 to lysosomal degradation to alter T cell-mediated cytotoxicity

Nat Chem Biol. 2019 Jan;15(1):42-50. doi: 10.1038/s41589-018-0161-x. Epub 2018 Nov 5.

Abstract

Expression of programmed cell death 1 (PD-1) ligand 1 (PD-L1) protects tumor cells from T cell-mediated immune surveillance, and immune checkpoint blockade (ICB) therapies targeting PD-1 and PD-L1 have exhibited significant clinical benefits. However, the relatively low response rate and observed ICB resistance highlight the need to understand the molecular regulation of PD-L1. Here we show that HIP1R targets PD-L1 to lysosomal degradation to alter T cell-mediated cytotoxicity. HIP1R physically interacts with PD-L1 and delivers PD-L1 to the lysosome through a lysosomal targeting signal. Depletion of HIP1R in tumor cells caused PD-L1 accumulation and suppressed T cell-mediated cytotoxicity. A rationally designed peptide (PD-LYSO) incorporating the lysosome-sorting signal and the PD-L1-binding sequence of HIP1R successfully depleted PD-L1 expression in tumor cells. Our results identify the molecular machineries governing the lysosomal degradation of PD-L1 and exemplify the development of a chimeric peptide for targeted degradation of PD-L1 as a crucial anticancer target.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing
  • B7-H1 Antigen / metabolism*
  • Binding Sites
  • Calcium-Binding Proteins / metabolism
  • Cell Cycle Proteins / metabolism
  • Cell Line, Tumor
  • Endosomal Sorting Complexes Required for Transport / metabolism
  • Humans
  • Lysosomes / drug effects
  • Lysosomes / metabolism*
  • Microfilament Proteins
  • Peptides / pharmacology
  • Programmed Cell Death 1 Receptor / metabolism
  • Protein Domains
  • Protein Sorting Signals
  • T-Lymphocytes, Cytotoxic / metabolism*
  • Vesicular Transport Proteins / genetics
  • Vesicular Transport Proteins / metabolism*

Substances

  • Adaptor Proteins, Signal Transducing
  • B7-H1 Antigen
  • CD274 protein, human
  • Calcium-Binding Proteins
  • Cell Cycle Proteins
  • Endosomal Sorting Complexes Required for Transport
  • HIP1R protein, human
  • Microfilament Proteins
  • PDCD1 protein, human
  • PDCD6IP protein, human
  • Peptides
  • Programmed Cell Death 1 Receptor
  • Protein Sorting Signals
  • Vesicular Transport Proteins