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Table 1 Inhibitors for RHO GTPases

From: RHO GTPase family in hepatocellular carcinoma

Target

Name of compound

Mechanism

Effect

Ref.

RHO GTPases

 RAC

EHT 1864

Lock in inactive state

Blocks migration and invasion of cancer cell

[141]

 RAC/CDC42

R-ketorolac

Targets RAC1 and CDC42

Blocks migration and invasion of cancer cell

[142]

 CDC42

ML141

Block nucleotide binding

Blocks migration and invasion of cancer cell

[143]

 RHO/RAC/CDC42

statins

Targeting HMG CoA reductase pathway to diminishing lipid modifications needed by Rho GTPases

Blocks proliferation and invasion of cancer cell

[146, 147]

Interaction of RHO and effectors

 ROCK

ATS907

Compete with ATP

In trial for glaucoma and ocular hypertension

[148]

 

AR-12286

Compete with ATP

In trial for glaucoma and ocular hypertension

[148]

 

Y-27632

Compete with ATP

Blocks proliferation, migration and invasion of cancer cell

[151]

 

fasudil

Compete with ATP

Blocks proliferation, migration and invasion of cancer cell

[152, 153]

 PAK

MBQ-167

Blocks PAK phosphorylation

Blocks growth, migration and EMT of cancer cell

[155]

 MRCK

BDP9066

Compete with ATP

Blocks proliferation and invasion of cancer cell

[156]

Interaction of RHO and RHOGEF

 RAC

NSC23766

Blocks interaction of RAC1 with TIAM1 and Trio

Blocks migration and invasion of cancer cell

[157,158,159]

 

1D-142

Block GEF binding

Blocks growth and invasion of cancer cell

[161]

 RAC/CDC42

EHop-016

Derivative of NSC23766

Blocks migration and invasion of cancer cell

[160]

 RHOA

Rhosin

Block GEF binding

Blocks migration and invasion of cancer cell

[162]

 

DC-Rhoin

Binds to the surface of RHOA by Cys107

Blocks migration and invasion of cancer cell

[140]