Beyond Thermodynamics: Drug Binding Kinetics Could Influence Epidermal Growth Factor Signaling

作者：Goyal Mayank; Rizzo Michael; Schumacher Frank; Wong Chung F^*

来源：Journal of Medicinal Chemistry, 2009, 52(18): 5582-5585.

DOI：10.1021/jm900974p

We modeled the kinetics of drug binding to protein kinases in the EGF signaling pathway relevant to non-small-cell lung cancer and found that binding kinetics could influence therapeutic potential, that fast binding kinetics was advantageous for most targets with a couple of exceptions, that targeting some protein kinases could enhance rather than attenuate the pathway, and that IC(50) could be sensitive to the kinetic parameters of drug binding.

• 出版日期2009-9-24