Lessons in Rational Drug Design for Protein Kinases

摘要

How do you design a drug that selectively recognizes one enzyme from among hundreds, all of which share the same substrate? This is the challenge confronting biochemists when developing small-molecule inhibitors of protein kinases, enzymes that regulate cellular growth, homeostasis, and signal transduc-tion. Fifteen years ago, intracellular kinases were considered too ubiquitous to be useful drug targets. But with mounting evidence for highly specific function in many kinases, many pharmaceutical endeavors today have screening programs for inhibitors of this class of enzymes.