Abstract

The modern-age drug discoveryrevolves around the use of multiple high-resolution structural biology methods. Over the years, these methods led to the genesis of some of the most historic drugs that perhaps would have been difficult if the discipline of structure-based drug discoveryhad not evolved. Researchers across the globe, either from academia or the pharmaceutical industries, have been working diligently to establish the rules of drug-likeness that capacitate an inhibitor to emerge as a possible drug against the desired target beyond the phases of clinical trials. This chapter provides the basics of structure-aided drug discovery and discusses the developments that took place using structural biology methods as the fundamental unit of the drug discovery process.

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