Tetraspanins: useful multifunction proteins for the possible design and development of small-molecule therapeutic tools

Tetraspanins constitute a well-conserved superfamily of four-span small membrane proteins (TM4SF), with >30 members in humans, with important roles in numerous mechanisms of cell biology. Moreover, tetraspanins associate with either specific partner proteins or another tetraspanin, generating a network of interactions involved in cell and membrane compartmentalization and having a role in cellular development, proliferation, activation, motility, and membrane fusions. Therefore, tetraspanins are considered regulators of cellular signaling and are often depicted as ‘molecular facilitators’. In view of these many physiological functions, it is likely that these molecules are important actors in pathological processes. In this review, we present the main characteristics of this superfamily, providing a more detailed description of some significant representatives and discuss their relevance as potential targets for the design and development of small-molecule therapeutics in different pathologies.