A. Cdc42 and Rac1 variants used in the study
|
Small GTPase
|
Mutant
|
Phenotype
|
Cdc42
|
Q61L |
GTPase defective |
|
G12V |
GTPase defective |
|
T17N |
Dominant negative (nucleotide binding-defective) |
|
F28L |
Fast-cycling (increased GDP/GTP exchange) |
|
D118N |
Elevated GDP/GTP exchange |
|
R66A |
RhoGDI binding-defective |
|
T35A |
Effector loop mutant |
|
F37A |
Effector loop mutant |
|
Y40C |
Effector loop mutant |
|
Δins |
Insert domain mutant |
|
SAAX |
CAAX box mutant |
Rac1
|
Q61L |
GTPase defective |
|
T17N |
Dominant negative (nucleotide binding- defective) |
|
F28L |
Fast-cycling (increased GDP/GTP exchange) |
|
P29S |
Fast-cycling (increased GDP/GTP exchange). Cancer mutation |
|
Rac1B |
Fast-cycling (increased GDP/GTP exchange). Cancer mutation |
B. Inhibitors used in the study
|
Inhibitor
|
Concentration Used
|
Targeted Pathway
|
GGTI298
|
10 μM |
Inhibitor of geranylgeranylation |
FFT277
|
10 μM |
Inhibitor of farnesylation |
2-bromopalmitate (2-BP)
|
100 μM |
Inhibitor of palmitoylation |
SU6656
|
2 μM |
Inhibitor of Src family kinases |
LY294002
|
10 μM |
Inhibitor of PI3 kinases |
Y27632
|
10 μM |
Inhibitor of Rho kinase (ROCK) |
NSC23766
|
30 μM |
Inhibitor of Rac |
ML-141
|
10 μM |
Inhibitor of Cdc42 |
SMIFH2
|
30 μM |
Inhibitor of formins |
CK-666
|
100 μM |
Inhibitor of Arp2/3 |