“…In the past two decades, with an in-depth understanding of allostery and the expeditious development of structural biology and computational biology tools, a series of emerging experimental and computational approaches for the development of allosteric drugs have commenced. The flurry of research into allosteric regulation has shown great potential for allosteric drug therapeutic development, such as oncoprotein Ras, − G protein-coupled receptors, − and protein kinases. − A number of site-oriented experimental approaches have been applied to detect allosteric sites, such as alanine-scanning mutagenesis, high-throughput screening, disulfide trapping, patch-clamp fluorometry, fragment-based screening, H/D exchange mass spectrometry, and photoaffinity labeling . Nevertheless, these experimental approaches are costly, time-consuming, arduous to cope with the challenges of the rapidly increasing number of allosteric drug targets, and incapable of identifying cryptic allosteric sites of proteins.…”