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Drug Design via Equilibrium Analysis by sgyblee is a document available to read on EtoBox.

This document discusses using equilibrium principles to design improved drug ligands that bind more strongly to receptors. It presents an example of designing mutated versions of granulocyte colony stimulating factor (GCSF) that bind more tightly to receptors at pH 7.4 (outside cells) but more weakly at pH 5.5 (inside cells). Computational modeling was used to identify mutations predicted to increase the difference in binding affinity at the two pH levels. Experiments found that two histidine mutations, D11

Author

sgyblee

Language

EN