Real-time kinetics

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Real-time kinetics: Additional insights for improved RTK drug discovery

Real-time kinetics case study: EGF vs Epiregulin

Kinetics of SH2(Grb2) recruitment to the plasma membrane differ in response to EGF and epiregulin stimulation. Indeed, epiregulin-induced SH2(Grb2) recruitment was more efficacious (~25%) and displayed faster kinetics relative
to that observed with EGF (t1/2 = 31.3 sec vs. 253.8 sec, respectively). The plasma membrane recruitment of SH2(Grb2) in response to both agonists was sustained for at least 60 minutes and was rapidly reversed (within 7 mins) by the EGFR kinase inhibitor Gefitinib (Iressa®). Striking differences were observed in agonist-induced trafficking of the SH2(Grb2) biosensor to early endosomes. Notably, EGF, but not epiregulin, promoted a gradual time-dependent increase in SH2(Grb2) levels in the early endosome compartment. These results are consistent with previously published data demonstrating that EGF, but not epiregulin, promotes EGFR internalization.

RTK realtime kinetics data