EHop-016, Rac GTPase inhibitor

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

Rac1 also known as Ras-related C3 botulinum toxin substrate 1 is a small signaling GTPase belonging to the Rac subfamily of the Rho family of GTPases. It has a molecular mass of approximately 21 kDa. Rac1 functions as a molecular switch and is involved in transmitting signals within the cell. It is widely expressed across various cell types and tissues playing a role in actin cytoskeleton organization and cell migration. Rac1 activity is regulated by GEFs (guanine nucleotide exchange factors) and GAPs (GTPase-activating proteins) which facilitate its transition between an active GTP-bound state and an inactive GDP-bound state.

Biological function summary

Rac1 is involved in the regulation of various cellular processes such as cell growth motility and division. It also contributes to the formation of lamellipodia which are membrane protrusions involved in cell movement and adhesion. Rac1 is often found within complexes interacting with other proteins like EH domain-containing protein 1 (Ehop) and is an important player in signal transduction pathways involving the cytoskeleton. Inhibition of Rac1 activity is an important point of control in various cellular contexts impacting multiple downstream effects.

Pathways

Rac1 is an integral component of the Rho GTPase signaling pathway and the closely associated Wnt signaling pathway. It interacts with proteins such as GAP and GEF to regulate the dynamics of these pathways influencing cellular morphology and movement. These pathways further connect Rac1 to several downstream effectors demonstrating its role in intracellular communication and control. EHOP-016 is a known inhibitor that specifically targets Rac1 demonstrating potential for experimental modulation of pathways involving Rac1.

Associated diseases and disorders

Rac1 has been implicated in cancer particularly in its role in cell proliferation and migration that contributes to tumor growth and metastasis. Rac1’s aberrant regulation is associated with other disorders like neurodegenerative diseases where disruptions in cytoskeletal dynamics contribute to pathogenesis. It shares pathways with other proteins such as GEFs and GAPs which are also relevant in these conditions. Rac1's interaction with its regulatory partners makes it a significant focus in therapeutic strategies aiming to mitigate its pathogenic effects.