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Beyond thermodynamics: drug binding kinetics could influence epidermal growth factor signaling.


ABSTRACT: 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.

SUBMITTER: Goyal M 

PROVIDER: S-EPMC2746254 | biostudies-literature | 2009 Sep

REPOSITORIES: biostudies-literature

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Beyond thermodynamics: drug binding kinetics could influence epidermal growth factor signaling.

Goyal Mayank M   Rizzo Michael M   Schumacher Frank F   Wong Chung F CF  

Journal of medicinal chemistry 20090901 18


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. ...[more]

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