Design, Synthesis, and Targeted Delivery of an Immune Stimulant that Selectively Reactivates Exhausted CAR T Cells

Angew Chem Int Ed Engl. 2022 Apr 4;61(15):e202113341. doi: 10.1002/anie.202113341. Epub 2022 Feb 16.

Abstract

Although chimeric antigen receptor (CAR) T cells have demonstrated significant promise in suppressing hematopoietic cancers, their applications in treating solid tumors have been limited by onset of CAR T cell exhaustion that accompanies continuous CAR T cell exposure to tumor antigen. To address this limitation, we have exploited the abilities of recently designed universal CARs to bind fluorescein and internalize a fluorescein-TLR7 agonist conjugate by CAR-mediated endocytosis. We demonstrate here that anti-fluorescein CAR-mediated uptake of a fluorescein-TLR7-3 conjugate can reactivate exhausted CAR T cells, leading to dramatic reduction in T cell exhaustion markers (PD-1+ Tim-3+ ) and shrinkage of otherwise resistant tumors without inducing systemic activation of the immune system. We conclude that CAR T cell exhaustion can be reversed by administration of a CAR-targeted TLR7 agonist, thereby enabling the CAR T cells to successfully treat solid tumors without incurring the systemic toxicity that commonly accompanies administration of nontargeted TLR7 agonists.

Keywords: CAR T Cell Therapy; Cancer; Immunology; T Cell Exhaustion; Toll-Like Receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antigens, Neoplasm
  • Fluorescein / metabolism
  • Humans
  • Immunotherapy, Adoptive
  • Neoplasms* / metabolism
  • Receptors, Chimeric Antigen* / metabolism
  • T-Lymphocytes
  • Toll-Like Receptor 7 / metabolism

Substances

  • Antigens, Neoplasm
  • Receptors, Chimeric Antigen
  • Toll-Like Receptor 7
  • Fluorescein