Figure 5
Figure 5. Hyperactive downstream signaling in relapse CLL acquired PLCγ2 variants can be blocked by targeting SYK or LYN. (A) Calcium flux from 3 individual relapse CLL (R) bearing mutated PLCγ2 or 12 nonresistant CLL samples (NR) were measured, and 5E6 cells per well in 96-half well microplates were stimulated with 10 μg/ml α-IgM at 37°C for 15 minutes, and then measured by BD Calcium Assay Kit. The data represent AUC from 7 and 12 replicates in resistant and nonresistant samples, respectively; 1.0 μM ibrutinib was pretreated for 1 hour followed by washout. (B) The data represents calcium release by 3 individual relapse CLL (R) or the mean of 12 nonresistant samples (NR) stimulated with 10 μg/ml α-IgM in the presence of 0.5 μM GS-9973, 2.5 μM R406, or 0.1 μM dasatinib; 1.0 μM ibrutinib was pretreated for 1 hour followed by washout. ***P < .001. (C) The downstream phospho-protein activation was accessed in CLL cells from a single patient (patient #2 in Table 1) in the baseline or relapse setting. The detailed information of the 3 relapsed CLL patient samples analyzed here are listed in Table 1.

Hyperactive downstream signaling in relapse CLL acquired PLCγ2 variants can be blocked by targeting SYK or LYN. (A) Calcium flux from 3 individual relapse CLL (R) bearing mutated PLCγ2 or 12 nonresistant CLL samples (NR) were measured, and 5E6 cells per well in 96-half well microplates were stimulated with 10 μg/ml α-IgM at 37°C for 15 minutes, and then measured by BD Calcium Assay Kit. The data represent AUC from 7 and 12 replicates in resistant and nonresistant samples, respectively; 1.0 μM ibrutinib was pretreated for 1 hour followed by washout. (B) The data represents calcium release by 3 individual relapse CLL (R) or the mean of 12 nonresistant samples (NR) stimulated with 10 μg/ml α-IgM in the presence of 0.5 μM GS-9973, 2.5 μM R406, or 0.1 μM dasatinib; 1.0 μM ibrutinib was pretreated for 1 hour followed by washout. ***P < .001. (C) The downstream phospho-protein activation was accessed in CLL cells from a single patient (patient #2 in Table 1) in the baseline or relapse setting. The detailed information of the 3 relapsed CLL patient samples analyzed here are listed in Table 1.

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