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2017 ; 8
(3
): 139-163
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Rac1 in human diseases: The therapeutic potential of targeting Rac1 signaling
regulatory mechanisms
#MMPMID27442895
Marei H
; Malliri A
Small GTPases
2017[Jul]; 8
(3
): 139-163
PMID27442895
show ga
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.