Background
Chimeric antigen receptor (CAR) T-cell is a rapidly emerging novel treatment modality for cancer, which has been especially successful against B-cell leukaemia and lymphoma. However, application to other haematological malignancies such as acute myeloid leukemia (AML) remains challenging due to the lack of suitable cancer-associated antigens. T cell immunoglobulin and mucin domain-containing protein 3 (TIM3) is an attractive target as it is overexpressed in AML bulk disease and leukemic stem cells, but they are also expressed on activated T-cells. Here, we report in vitro efficacy of a novel locally developed TIM3-specific CAR T-cell, following knock-out (KO) of TIM3 in modified T-cells to prevent fratricide.
Aim
To generate TIM3- targeting CAR (CARTIM3) T-cells and evaluate in vitro activity.
Methods
CAR short-chain variable fragment (scFv) was based upon an antibody patent. The scFv was cloned into an in-house CAR construct and electroporated into primary T-cells using the PiggyBat transposon/transposase system. TIM3 is a T-cell exhaustion marker upregulated upon T-cell activation, therefore two TIM3 guide RNAs (gRNAs) and Cas9 were co-electroporated with the CAR construct to prevent possible fratricide (n=3), then expanded in vitro using irradiated feeder cells and interleukin 15, for 2 weeks. At the end of culture period, CAR T-cells were assayed for CAR expression, exhaustion and memory phenotypes by flow cytometry. CAR T-cell function was determined by intracellular cytokine flow cytometry release and calcein-AM cytotoxicity assays upon co-culture with TIM3-overexpressing HEK293 and K562 cell lines. CAR without TIM3-targeting domain and CAR T-cells without TIM3 KO served as negative controls.
Results
The TIM3KO CARTIM3 T-cells expanded 3.8-fold with CAR expression of 75%±14%. There was no difference in phenotypes between cultures, besides lower TIM3 expression in the TIM3KO cultures as expected (7.5±7.9% vs 51.2±21%; p=0.0413).
Cytokines TNF-α and IFN-γ produced in response to TIM3 overexpressing cell lines were not significantly different to no-target controls. However, a strong cytotoxic response was observed exclusively for TIM3KO CARTIM3 T-cells, but none of the other control CARs at 20:1 effector:target ratio against TIM3 overexpressing HEK293 (60.1±12.9% vs 0.1±5.6%, p=0.0214) and K562 (90.5± 23.7% vs 13.2± 15.6%, p= 0.0128).
Discussion
We have demonstrated the successful generation of an anti-TIM3 CAR construct able to produce significant specific cytotoxicity against TIM3 overexpressing cell lines when expressed in T-cells with TIM3 KO. TIM3 is an extremely attractive AML target due to presence on leukaemic stem cells and this work could inform further translational studies.