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.

四跨膜蛋白构成了一个保守的四跨小膜蛋白 (TM4SF) 超家族，在人类中有超过 30 名成员，在多种细胞生物学机制中具有重要作用。此外，四跨膜蛋白与特定的伙伴蛋白或另一种四跨膜蛋白结合，产生一个参与细胞和膜区室化的相互作用网络，并在细胞发育、增殖、激活、运动和膜融合中发挥作用。因此，四跨膜蛋白被认为是细胞信号的调节剂，通常被描述为“分子促进剂”。鉴于这些许多生理功能，这些分子很可能是病理过程中的重要参与者。在这篇综述中，我们介绍了这个超家族的主要特征，