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Small GTPases. 2017 Jul 3;8(3):139-163. doi: 10.1080/21541248.2016.1211398. Epub 2016 Jul 21.

Rac1 in human diseases: The therapeutic potential of targeting Rac1 signaling regulatory mechanisms.

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a Cell Signaling Group, Cancer Research UK Manchester Institute , The University of Manchester , Manchester , UK.


Abnormal Rac1 signaling is linked to a number of debilitating human diseases, including cancer, cardiovascular diseases and neurodegenerative disorders. As such, Rac1 represents an attractive therapeutic target, yet the search for effective Rac1 inhibitors is still underway. Given the adverse effects associated with Rac1 signaling perturbation, cells have evolved several mechanisms to ensure the tight regulation of Rac1 signaling. Thus, characterizing these mechanisms can provide invaluable information regarding major cellular events that lead to aberrant Rac1 signaling. Importantly, this information can be utilized to further facilitate the development of effective pharmacological modulators that can restore normal Rac1 signaling. In this review, we focus on the pathological role of Rac1 signaling, highlighting the benefits and potential drawbacks of targeting Rac1 in a clinical setting. Additionally, we provide an overview of available compounds that target key Rac1 regulatory mechanisms and discuss future therapeutic avenues arising from our understanding of these mechanisms.


GTPase activating proteins (GAPs); Rac1; Rac1 targeting; cancer; cardiovascular diseases; guanine nucleotide dissociation inhibitors (GDIs); guanine nucleotide exchange factors (GEFs); inflammatory disorders; kidney diseases; neurodegenerative disorders; post-translational modifications

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