Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.

Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci U S A (2010) 1.94

Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J Biol Chem (2012) 1.17

Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol (2012) 1.13

P-REX1 creates a positive feedback loop to activate growth factor receptor, PI3K/AKT and MEK/ERK signaling in breast cancer. Oncogene (2014) 1.09

The role of Rac1 in the regulation of NF-κB activity, cell proliferation, and cell migration in non-small cell lung carcinoma. Cancer Biol Ther (2012) 1.02

Identification of an autoinhibitory mechanism that restricts C1 domain-mediated activation of the Rac-GAP alpha2-chimaerin. J Biol Chem (2008) 0.98

Inhibition of the Rho GTPase, Rac1, decreases estrogen receptor levels and is a novel therapeutic strategy in breast cancer. Endocr Relat Cancer (2011) 0.95

Targeting Cdc42 with the small molecule drug AZA197 suppresses primary colon cancer growth and prolongs survival in a preclinical mouse xenograft model by downregulation of PAK1 activity. J Transl Med (2013) 0.94

Lysophosphatidic acid and sphingosine-1-phosphate promote morphogenesis and block invasion of prostate cancer cells in three-dimensional organotypic models. Oncogene (2011) 0.92

Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells. Am J Physiol Lung Cell Mol Physiol (2013) 0.88

Research resource: progesterone receptor targetome underlying mammary gland branching morphogenesis. Mol Endocrinol (2013) 0.87

Molecular pathways: targeting the kinase effectors of RHO-family GTPases. Clin Cancer Res (2014) 0.86

RAC3 is a pro-migratory co-activator of ERα. Oncogene (2011) 0.86

Targeting Rho-GTPases in immune cell migration and inflammation. Br J Pharmacol (2014) 0.85

Regulation of epithelial-mesenchymal transition in breast cancer cells by cell contact and adhesion. Cancer Inform (2015) 0.84

Loss of the E3 ubiquitin ligase HACE1 results in enhanced Rac1 signaling contributing to breast cancer progression. Oncogene (2015) 0.82

Regulation of Adherens Junctions in Trabecular Meshwork Cells by Rac GTPase and their influence on Intraocular Pressure. J Ocul Biol (2013) 0.79

The Rac activator Tiam1 is required for polarized protrusional outgrowth of primary astrocytes by affecting the organization of the microtubule network. Small GTPases (2012) 0.79

EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic β-cells. Cell Signal (2015) 0.78

Rac GTPase regulation of 3D invasion in neuroblastomas lacking MYCN amplification. Cell Adh Migr (2016) 0.78

A Novel Pharmacologic Activity of Ketorolac for Therapeutic Benefit in Ovarian Cancer Patients. Clin Cancer Res (2015) 0.78

Novel Activities of Select NSAID R-Enantiomers against Rac1 and Cdc42 GTPases. PLoS One (2015) 0.77

Tumor cell expression of MMP3 as a prognostic factor for poor survival in pancreatic, pulmonary, and mammary carcinoma. Genes Cancer (2015) 0.77

CD99 triggering induces methuosis of Ewing sarcoma cells through IGF-1R/RAS/Rac1 signaling. Oncotarget (2016) 0.77

Rho GTPases: Novel Players in the Regulation of the DNA Damage Response? Biomolecules (2015) 0.77

The Phospholipase Cγ2 Mutants R665W and L845F Identified in Ibrutinib-resistant Chronic Lymphocytic Leukemia Patients Are Hypersensitive to the Rho GTPase Rac2 Protein. J Biol Chem (2016) 0.77

PI3K signaling in cancer: beyond AKT. Curr Opin Cell Biol (2017) 0.76

Deregulation of Rho GTPases in cancer. Small GTPases (2016) 0.76

Heregulin/ErbB3 Signaling Enhances CXCR4-Driven Rac1 Activation and Breast Cancer Cell Motility via Hypoxia-Inducible Factor 1α. Mol Cell Biol (2016) 0.75

Therapeutic sensitivity to Rac GTPase inhibition requires consequential suppression of mTORC1, AKT, and MEK signaling in breast cancer. Oncotarget (2017) 0.75

Broadening the spectrum of actin-based protrusive activity mediated by Arp2/3 complex-facilitated polymerization: motility of cytoplasmic ridges and tubular projections. Cytoskeleton (Hoboken) (2014) 0.75

Par-1b is required for morphogenesis and differentiation of myoepithelial cells during salivary gland development. Organogenesis (2016) 0.75

Low Intensity Pulsed Ultrasound (LIPUS) promotes cell motility through vinculin-controlled Rac1 GTPase activity. J Cell Sci (2017) 0.75

Glucocorticoid therapy regulates podocyte motility by inhibition of Rac1. Sci Rep (2017) 0.75

GEF means go: turning on RHO GTPases with guanine nucleotide-exchange factors. Nat Rev Mol Cell Biol (2005) 10.44

The Ras superfamily at a glance. J Cell Sci (2005) 4.83

Distinct requirements for Ras oncogenesis in human versus mouse cells. Genes Dev (2002) 4.30

ROCK-generated contractility regulates breast epithelial cell differentiation in response to the physical properties of a three-dimensional collagen matrix. J Cell Biol (2003) 4.24

Inhibiting farnesylation of progerin prevents the characteristic nuclear blebbing of Hutchinson-Gilford progeria syndrome. Proc Natl Acad Sci U S A (2005) 3.64

Ras superfamily GEFs and GAPs: validated and tractable targets for cancer therapy? Nat Rev Cancer (2010) 3.59

Rho-family GTPases: it's not only Rac and Rho (and I like it). J Cell Sci (2004) 3.27

Activation of RalA is critical for Ras-induced tumorigenesis of human cells. Cancer Cell (2005) 3.17

Personalized medicine in non-small-cell lung cancer: is KRAS a useful marker in selecting patients for epidermal growth factor receptor-targeted therapy? J Clin Oncol (2010) 2.70

Divergent roles for RalA and RalB in malignant growth of human pancreatic carcinoma cells. Curr Biol (2006) 2.61

The dark side of Ras: regulation of apoptosis. Oncogene (2003) 2.60

Signaling interplay in Ras superfamily function. Curr Biol (2005) 2.59

Honokiol, a small molecular weight natural product, inhibits angiogenesis in vitro and tumor growth in vivo. J Biol Chem (2003) 2.44

Renewing the conspiracy theory debate: does Raf function alone to mediate Ras oncogenesis? Trends Cell Biol (2004) 2.32

K-Ras promotes growth transformation and invasion of immortalized human pancreatic cells by Raf and phosphatidylinositol 3-kinase signaling. Cancer Res (2007) 2.26

Rho Family GTPase modification and dependence on CAAX motif-signaled posttranslational modification. J Biol Chem (2008) 2.22

KRAS/BRAF mutation status and ERK1/2 activation as biomarkers for MEK1/2 inhibitor therapy in colorectal cancer. Mol Cancer Ther (2009) 2.22

Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. J Biol Chem (2007) 2.20

Ras history: The saga continues. Small GTPases (2010) 2.18

Ligand-dependent dynamics and intramolecular signaling in a PDZ domain. J Mol Biol (2004) 2.17

Structural basis for the selective activation of Rho GTPases by Dbl exchange factors. Nat Struct Biol (2002) 2.14

Inhibition of Ras for cancer treatment: the search continues. Future Med Chem (2011) 2.14

Tiam1 mediates Ras activation of Rac by a PI(3)K-independent mechanism. Nat Cell Biol (2002) 2.12

Rnd proteins function as RhoA antagonists by activating p190 RhoGAP. Curr Biol (2003) 1.84

XPLN, a guanine nucleotide exchange factor for RhoA and RhoB, but not RhoC. J Biol Chem (2002) 1.78

Involvement of Ras activation in human breast cancer cell signaling, invasion, and anoikis. Cancer Res (2004) 1.75

Ras family signaling: therapeutic targeting. Cancer Biol Ther (2003) 1.74

RhoG signals in parallel with Rac1 and Cdc42. J Biol Chem (2002) 1.70

DLC-1 suppresses non-small cell lung cancer growth and invasion by RhoGAP-dependent and independent mechanisms. Mol Carcinog (2008) 1.67

Opinion: Searching for the elusive targets of farnesyltransferase inhibitors. Nat Rev Cancer (2003) 1.67

Rac1b, a tumor associated, constitutively active Rac1 splice variant, promotes cellular transformation. Oncogene (2004) 1.66

Lack of extracellular signal-regulated kinase mitogen-activated protein kinase signaling shows a new type of melanoma. Cancer Res (2007) 1.62

Oncogenic Ras and its role in tumor cell invasion and metastasis. Semin Cancer Biol (2004) 1.62

The G12 family of heterotrimeric G proteins promotes breast cancer invasion and metastasis. Proc Natl Acad Sci U S A (2006) 1.54

Aurora-A phosphorylates, activates, and relocalizes the small GTPase RalA. Mol Cell Biol (2009) 1.51

Persistent signaling by dysregulated thrombin receptor trafficking promotes breast carcinoma cell invasion. Mol Cell Biol (2004) 1.50

A six-gene signature predicts survival of patients with localized pancreatic ductal adenocarcinoma. PLoS Med (2010) 1.46

Leukemia-associated Rho guanine nucleotide exchange factor promotes G alpha q-coupled activation of RhoA. Mol Cell Biol (2002) 1.43

Loss of transgelin in breast and colon tumors and in RIE-1 cells by Ras deregulation of gene expression through Raf-independent pathways. J Biol Chem (2001) 1.40

Overexpression of collagenase 1 (MMP-1) is mediated by the ERK pathway in invasive melanoma cells: role of BRAF mutation and fibroblast growth factor signaling. J Biol Chem (2004) 1.39

RhoE is a pro-survival p53 target gene that inhibits ROCK I-mediated apoptosis in response to genotoxic stress. Curr Biol (2006) 1.37

The RalGEF-Ral Effector Signaling Network: The Road Less Traveled for Anti-Ras Drug Discovery. Genes Cancer (2011) 1.32

Geranylgeranyltransferase I inhibitors target RalB to inhibit anchorage-dependent growth and induce apoptosis and RalA to inhibit anchorage-independent growth. Mol Cell Biol (2007) 1.32

Molecular basis for Rho GTPase signaling specificity. Breast Cancer Res Treat (2004) 1.28

Farnesyltransferase inhibitors: promises and realities. Curr Opin Pharmacol (2002) 1.24

Release of autoinhibition of ASEF by APC leads to CDC42 activation and tumor suppression. Nat Struct Mol Biol (2007) 1.22

Cellular N-Ras promotes cell survival by downregulation of Jun N-terminal protein kinase and p38. Mol Cell Biol (2002) 1.20

Identification and characterization of rain, a novel Ras-interacting protein with a unique subcellular localization. J Biol Chem (2004) 1.20

Regulation of Rnd3 localization and function by protein kinase C alpha-mediated phosphorylation. Biochem J (2009) 1.19

RasGRP4 is a novel Ras activator isolated from acute myeloid leukemia. J Biol Chem (2002) 1.19

Ras-mediated loss of the pro-apoptotic response protein Par-4 is mediated by DNA hypermethylation through Raf-independent and Raf-dependent signaling cascades in epithelial cells. J Biol Chem (2005) 1.18

Activation and involvement of Ral GTPases in colorectal cancer. Cancer Res (2011) 1.18

RAC1 inhibition targets amyloid precursor protein processing by gamma-secretase and decreases Abeta production in vitro and in vivo. J Biol Chem (2005) 1.17

Involvement of phosphatidylinositol 3-kinase, but not RalGDS, in TC21/R-Ras2-mediated transformation. J Biol Chem (2002) 1.16

Requirement for C-terminal sequences in regulation of Ect2 guanine nucleotide exchange specificity and transformation. J Biol Chem (2004) 1.16

Transforming activity of the Rho family GTPase, Wrch-1, a Wnt-regulated Cdc42 homolog, is dependent on a novel carboxyl-terminal palmitoylation motif. J Biol Chem (2005) 1.13

ROCK1 and ROCK2 are required for non-small cell lung cancer anchorage-independent growth and invasion. Cancer Res (2012) 1.12

Use of retrovirus expression of interfering RNA to determine the contribution of activated K-Ras and ras effector expression to human tumor cell growth. Methods Enzymol (2006) 1.11

Targeting signal transduction in pancreatic cancer treatment. Expert Opin Ther Targets (2007) 1.11

Context-dependent roles of mutant B-Raf signaling in melanoma and colorectal carcinoma cell growth. Mol Cancer Ther (2007) 1.10

Raf-independent deregulation of p38 and JNK mitogen-activated protein kinases are critical for Ras transformation. J Biol Chem (2002) 1.09

Oncogenic activity of Ect2 is regulated through protein kinase C iota-mediated phosphorylation. J Biol Chem (2010) 1.08

Critical and distinct roles of amino- and carboxyl-terminal sequences in regulation of the biological activity of the Chp atypical Rho GTPase. J Biol Chem (2005) 1.07

K-Ras promotes angiogenesis mediated by immortalized human pancreatic epithelial cells through mitogen-activated protein kinase signaling pathways. Mol Cancer Res (2009) 1.06

Auto-inhibition of the Dbl family protein Tim by an N-terminal helical motif. J Biol Chem (2007) 1.06

Atypical mechanism of regulation of the Wrch-1 Rho family small GTPase. Curr Biol (2004) 1.05

Interferon regulatory factor 7 is associated with Epstein-Barr virus-transformed central nervous system lymphoma and has oncogenic properties. J Virol (2004) 1.05

Effects of structure of Rho GTPase-activating protein DLC-1 on cell morphology and migration. J Biol Chem (2008) 1.05

Critical but distinct roles for the pleckstrin homology and cysteine-rich domains as positive modulators of Vav2 signaling and transformation. Mol Cell Biol (2002) 1.05

Aberrant receptor internalization and enhanced FRS2-dependent signaling contribute to the transforming activity of the fibroblast growth factor receptor 2 IIIb C3 isoform. J Biol Chem (2008) 1.04

Role of MAP kinases in the 1,25-dihydroxyvitamin D3-induced transactivation of the rat cytochrome P450C24 (CYP24) promoter. Specific functions for ERK1/ERK2 and ERK5. J Biol Chem (2002) 1.01

Cancer: Drug for an 'undruggable' protein. Nature (2013) 1.01

Involvement of fibroblast growth factor receptor 2 isoform switching in mammary oncogenesis. Mol Cancer Res (2008) 1.00

Ras effector switching promotes divergent cell fates in C. elegans vulval patterning. Dev Cell (2011) 0.96

Aberrant overexpression of the Rgl2 Ral small GTPase-specific guanine nucleotide exchange factor promotes pancreatic cancer growth through Ral-dependent and Ral-independent mechanisms. J Biol Chem (2010) 0.96

Ras signaling, deregulation of gene expression and oncogenesis. Cancer Treat Res (2003) 0.96

p68RacGAP is a novel GTPase-activating protein that interacts with vascular endothelial zinc finger-1 and modulates endothelial cell capillary formation. J Biol Chem (2004) 0.96

Mutant N-RAS protects colorectal cancer cells from stress-induced apoptosis and contributes to cancer development and progression. Cancer Discov (2012) 0.96

Real-time in vitro measurement of intrinsic and Ras GAP-mediated GTP hydrolysis. Methods Enzymol (2006) 0.96

Extracellular signal-regulated kinase (ERK) phosphorylates histone deacetylase 6 (HDAC6) at serine 1035 to stimulate cell migration. J Biol Chem (2013) 0.95

RhoA biological activity is dependent on prenylation but independent of specific isoprenoid modification. Cell Growth Differ (2002) 0.95

The RalB small GTPase mediates formation of invadopodia through a GTPase-activating protein-independent function of the RalBP1/RLIP76 effector. Mol Cell Biol (2012) 0.95

Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing. J Neurochem (2008) 0.94

Toward an Alzheimer's disease diagnosis via high-resolution blood gene expression. Alzheimers Dement (2010) 0.93

Regulator of G-protein signaling 14 (RGS14) is a selective H-Ras effector. PLoS One (2009) 0.93

A novel four transmembrane spanning protein, CLP24. A hypoxically regulated cell junction protein. Eur J Biochem (2004) 0.92

Differential involvement of RalA and RalB in colorectal cancer. Small GTPases (2012) 0.92

Citron kinase, a RhoA effector, enhances HIV-1 virion production by modulating exocytosis. Traffic (2006) 0.91

Response to MLN8237 in pancreatic cancer is not dependent on RalA phosphorylation. Mol Cancer Ther (2013) 0.91

Opposing roles of the extracellular signal-regulated kinase and p38 mitogen-activated protein kinase cascades in Ras-mediated downregulation of tropomyosin. Mol Cell Biol (2002) 0.90

Nitric oxide-releasing silica nanoparticle inhibition of ovarian cancer cell growth. Mol Pharm (2010) 0.89

Differential effects of PPARgamma ligands on oxidative stress-induced death of retinal pigmented epithelial cells. Invest Ophthalmol Vis Sci (2011) 0.89

RhoGDI2 antagonizes ovarian carcinoma growth, invasion and metastasis. Small GTPases (2011) 0.89

Phosphorylation by protein kinase Cα regulates RalB small GTPase protein activation, subcellular localization, and effector utilization. J Biol Chem (2012) 0.89

Established and emerging fluorescence-based assays for G-protein function: heterotrimeric G-protein alpha subunits and regulator of G-protein signaling (RGS) proteins. Comb Chem High Throughput Screen (2003) 0.88