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. Author manuscript; available in PMC: 2016 Jun 18.
Published in final edited form as: Expert Opin Drug Discov. 2015 Jun 18;10(9):991–1010. doi: 10.1517/17460441.2015.1058775

Table 1.

Selected Rho GTPases and regulators relevant to human cancer:

Involvement in cancer Reference
Rho GTPase
RhoA Mutated in gastric carcinoma, Burkitt lymphoma, peripheral
and angioimmunoblastic T-cell lymphoma
[21,143-152]
Over-expressed in gastric carcinoma, testicular germ cell
tumor, head and neck squamous cell carcinoma, bladder, colon,
breast and lung cancer
[147-152]
Rac1 Mutated in melanoma, head and neck, and cutaneous squamous
cell carcinoma
[153-156]
Over-expressed in oral squamous cell carcinoma, gastric cell
carcinoma, breast, lung, testicular and prostate cancer
[147,148,151,152,157,158]
Cdc42 Over-expressed in breast cancer, melanoma, head and neck
squamous cell carcinoma, colorectal, non-small cell lung and
testicular cancer
[148,149,151,152,159-
161]
RhoGEFs
P-Rex1 Over-expressed in metastatic prostate tumor, breast cancer, and
melanoma
[162-164]
P-Rex2 Over-expressed in PTEN wild type breast cancer [165]
ECT2 Over-expressed in lung, esophageal squamous cell carcinoma,
glioblastoma, colorectal carcinoma, pancreatic, non-small cell
lung cancer
[166-170]
Trio Over-expressed in glioblastoma, breast cancer [171,172]
Activated in adult T-cell leukemia by alternative splicing [173]
Vav1 Over-expressed in neuroblastoma, pancreatic carcinoma,
metastatic melanoma and B-cell chronic lymphocytic leukemia
[174-177]
Vav2 Over-expressed in ovarian and breast cancer; Hyper-activated
in head and neck squamous cell carcinoma
[178-180]
Vav3 Over-expressed in prostate, breast cancer and glioblastoma [171,181]
Tiam1 Over-expressed in melanoma, breast, colon, prostate and renal
cell carcinoma
[182-186]
LARG Truncated and fusion to MLL in acute myelogenous leukemia [49]
BCR-Abl1 Fusion protein resulted from chromosome translocation
associated most CML. BCR contains a GEF and a GAP domain
[187]
DOCK1 Over-expressed in glioblastoma [188]
RhoGAPs
DLC-1 Two missense mutations in pancreatic cancer [189]
Loss-of-expression or down-regulation in lung, breast, liver,
colon, pancreatic, ovarian, uterine, gastric, prostate, renal
cancer, lymphoma, and ALL
[52,53,190-192]
p190-B Gene amplification and protein overexpression in
hepatocellular carcinoma cells
[58]
β2-
chimaerin
Down-regulated in breast cancer [96]
BCR-Abl1 Fusion protein resulted from chromosome translocation
associated with most CML. BCR contain a GEF and a GAP
domain
[187]
RhoGDIs
RhoGDI1 Over-expressed in colorectal and ovarian cancers [193,194]
Down-regulated in brain cancer and hepatocellular carcinoma [195-197]
Over-expressed or down-regulated in breast cancer in different
studies
[152,198]
RhoGDI2 Increased expression in pancreatic and ovarian cancer [199,200]
Down-regulated in bladder cancer [201,202]
Over-expressed or down-regulated in breast cancer in different
studies
[203]