Abstract
The remarkable precision of the pharmacological modulation, including high degree of specificity, probe dependence, and signaling bias, confers to GPCR allosteric modulators unique advantages over orthosteric classical ligands. At present, GPCR allosteric modulation appears as an innovative approach that may enable the therapeutic targeting of previously intractable GPCRs or provide safer therapeutics for currently targeted receptors. The discovery of GPCR allosteric modulators entails a number of intense challenges from the standpoint of standard drug discovery programs, including, in particular, rational design. Recently, several structures of receptors in complex with small-molecule allosteric modulators have been solved across all human GPCR classes: A, B, C, and F. These breakthroughs are expected to contribute to the structure-based design of GPCR allosteric drugs with an improved therapeutic action. Recent Food and Drug Administration (FDA) approvals and clinical trials evidence that GPCR allosteric modulation is a viable drug discovery strategy and it represents a reliable source for safe drugs in the near future.
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