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[Preprint]. 2023 May 24:2023.05.24.542108. [Version 1] doi: 10.1101/2023.05.24.542108

Structural principles of peptide-centric Chimeric Antigen Receptor recognition guide therapeutic expansion

Yi Sun, Tyler J Florio, Sagar Gupta, Michael C Young, Quinlen F Marshall, Samuel E Garfinkle, Georgia F Papadaki, Hau V Truong, Emily Mycek, Peiyao Li, Alvin Farrel, Nicole L Church, Shereen Jabar, Matthew D Beasley, Ben R Kiefel, Mark Yarmarkovich, Leena Mallik, John M Maris, Nikolaos G Sgourakis
PMCID: PMC10245919  PMID: 37292750

Abstract

Peptide-Centric Chimeric Antigen Receptors (PC-CARs), which recognize oncoprotein epitopes displayed by human leukocyte antigens (HLAs) on the cell surface, offer a promising strategy for targeted cancer therapy 1 . We have previously developed a PC-CAR targeting a neuroblastoma- associated PHOX2B peptide, leading to robust tumor cell lysis restricted by two common HLA allotypes 2 . Here, we determine the 2.1 Å structure of the PC-CAR:PHOX2B/HLA-A*24:02/β2m complex, which reveals the basis for antigen-specific recognition through interactions with CAR complementarity-determining regions (CDRs). The PC-CAR adopts a diagonal docking mode, where interactions with both conserved and polymorphic HLA framework residues permit recognition of multiple HLA allotypes from the A9 serological cross-reactivity group, covering a combined American population frequency of up to 25.2%. Comprehensive characterization using biochemical binding assays, molecular dynamics simulations, and structural and functional analyses demonstrate that high-affinity PC-CAR recognition of cross-reactive pHLAs necessitates the presentation of a specific peptide backbone, where subtle structural adaptations of the peptide are critical for high-affinity complex formation and CAR-T cell killing. Our results provide a molecular blueprint for engineering CARs with optimal recognition of tumor-associated antigens in the context of different HLAs, while minimizing cross-reactivity with self-epitopes.

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