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London 2014
 
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Training Day Lectures
Copies of PowerPoint slides

Lecture 1 | Theory Lecture 1 | Theory
Lecture 2 | Applications Lecture 2 | Applications
Lecture 3 | Case Study Lecture 3 | Case Study

Lecture 1 | TheoryTop of pageNext section
10:00 - 10:45

Petr Kuzmic (BioKin Ltd, Boston)

Selected aspects of chemical theory that are necessary for understanding the construction of biochemical binding mechanisms in the DynaFit software package.

Topics

  • Algebraic vs. numerical models
  • Statistical factors
  • Thermodynamic box
  • Intensive physical quantities
  • Rapid equilibrium enzyme kinetics

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Lecture 2 | ApplicationsTop of pageNext section
10:45 - 11:30

Jochen Reinstein (MPImF, Heidelberg)

The DynaFit software package has been deployed at the Max Planck Institute for Medical Research, Heidelberg, Germany, since before 2007. Dr. Jochen Reinstein will share some of his insights and experiences.

Lecture 3 | Case StudyTop of pageNext section
11:30 - 12:15

Petr Kuzmic (BioKin Ltd, Boston)

Technical details of how the DynaFit softwre package was used in a recently published report to determine the binding constants (and inactivation rate constants) for a series of covalent enzyme inhibitors acting as anti-cancer drugs.

Topics

  • Assumptions underpinning the "classic" method
  • Substrate depletion and inhibitor depletion
  • Failure of the "classic" method of kinetic analysis
  • Results for Neratinib
  • Correlation of cellular vs. biochemical potency

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Reference

  • Schwartz, Kuzmic et al. (2014) Proc. Natl. Acad. Sci. USA 111, 173-178. (pdf)

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