Current status of SRC inhibitors in solid tumor malignancies.

PubWeight™: 1.18‹?› | Rank: Top 10%

🔗 View Article (PMC 3228195)

Published in Oncologist on April 26, 2011

Authors

Lauren N Puls1, Matthew Eadens, Wells Messersmith

Author Affiliations

1: Division of Medical Oncology, University of Colorado Cancer Center, Aurora, Colorado, USA.

Associated clinical trials:

Safety and Efficacy of Saracatinib In Subjects With Lymphangioleiomyomatosis (SLAM-2) | NCT02737202

Articles citing this

Role of ABL family kinases in cancer: from leukaemia to solid tumours. Nat Rev Cancer (2013) 1.92

Multi-target drugs: the trend of drug research and development. PLoS One (2012) 1.28

Invading one step at a time: the role of invadopodia in tumor metastasis. Oncogene (2013) 1.13

Biomarker-driven trial in metastatic pancreas cancer: feasibility in a multicenter study of saracatinib, an oral Src inhibitor, in previously treated pancreatic cancer. Cancer Med (2012) 1.00

Epithelial-mesenchymal transition: a new target in anticancer drug discovery. Nat Rev Drug Discov (2016) 0.98

The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase. J Virol (2013) 0.92

Src inhibition blocks renal interstitial fibroblast activation and ameliorates renal fibrosis. Kidney Int (2016) 0.90

A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies. Invest New Drugs (2013) 0.89

SRC points the way to biomarkers and chemotherapeutic targets. Genes Cancer (2012) 0.88

Phase II evaluation of dasatinib in the treatment of recurrent or persistent epithelial ovarian or primary peritoneal carcinoma: a Gynecologic Oncology Group study. Gynecol Oncol (2012) 0.88

Src signaling pathways in prostate cancer. Cancer Metastasis Rev (2014) 0.86

New treatments for autosomal dominant polycystic kidney disease. Br J Clin Pharmacol (2013) 0.85

Phase I study of dasatinib in combination with capecitabine, oxaliplatin and bevacizumab followed by an expanded cohort in previously untreated metastatic colorectal cancer. Invest New Drugs (2013) 0.84

Targeting SRC and tubulin in mucinous ovarian carcinoma. Clin Cancer Res (2013) 0.83

Proteolysis of EphA2 Converts It from a Tumor Suppressor to an Oncoprotein. Cancer Res (2015) 0.83

Dasatinib promotes the expansion of a therapeutically superior T-cell repertoire in response to dendritic cell vaccination against melanoma. Oncoimmunology (2014) 0.82

Cross-talk between EphA2 and BRaf/CRaf is a key determinant of response to Dasatinib. Clin Cancer Res (2014) 0.82

Bioinformatic approaches to augment study of epithelial-to-mesenchymal transition in lung cancer. Physiol Genomics (2014) 0.82

Phosphorylation-mediated activation of LDHA promotes cancer cell invasion and tumour metastasis. Oncogene (2017) 0.82

Involvement of Src in the Adaptation of Cancer Cells under Microenvironmental Stresses. J Signal Transduct (2012) 0.81

The Emerging Role of ABL Kinases in Solid Tumors. Trends Cancer (2015) 0.81

Diacylglycerol kinase α promotes 3D cancer cell growth and limits drug sensitivity through functional interaction with Src. Oncotarget (2014) 0.80

Bosutinib plus capecitabine for selected advanced solid tumours: results of a phase 1 dose-escalation study. Br J Cancer (2014) 0.79

A novel 3D fibril force assay implicates src in tumor cell force generation in collagen networks. PLoS One (2013) 0.79

Drugs for solid cancer: the productivity crisis prompts a rethink. Onco Targets Ther (2013) 0.78

Dasatinib (BMS-35482) interacts synergistically with docetaxel, gemcitabine, topotecan, and doxorubicin in ovarian cancer cells with high SRC pathway activation and protein expression. Int J Gynecol Cancer (2014) 0.78

Strategies to avoid treatment-induced lineage crisis in advanced prostate cancer. Nat Rev Clin Oncol (2016) 0.78

The Human Kinome Targeted by FDA Approved Multi-Target Drugs and Combination Products: A Comparative Study from the Drug-Target Interaction Network Perspective. PLoS One (2016) 0.77

Src Inhibition Blocks c-Myc Translation and Glucose Metabolism to Prevent the Development of Breast Cancer. Cancer Res (2015) 0.77

Dasatinib, a Src inhibitor, sensitizes liver metastatic colorectal carcinoma to oxaliplatin in tumors with high levels of phospho-Src. Oncotarget (2016) 0.77

Phase II study of saracatinib (AZD0530) in patients with previously treated metastatic colorectal cancer. Invest New Drugs (2015) 0.76

Improvement of pyrazolo[3,4-d]pyrimidines pharmacokinetic properties: nanosystem approaches for drug delivery. Sci Rep (2016) 0.76

A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region. Chem Biol Drug Des (2014) 0.76

Novel autophosphorylation sites of Src family kinases regulate kinase activity and SH2 domain-binding capacity. FEBS Lett (2016) 0.75

SRC kinase inhibition with saracatinib limits the development of osteolytic bone disease in multiple myeloma. Oncotarget (2016) 0.75

How do kinases contribute to tonicity-dependent regulation of the transcription factor NFAT5? World J Nephrol (2016) 0.75

Novel Bioluminescent Activatable Reporter for Src Tyrosine Kinase Activity in Living Mice. Theranostics (2016) 0.75

The EMT spectrum and therapeutic opportunities. Mol Oncol (2017) 0.75

Articles cited by this

The protein kinase complement of the human genome. Science (2002) 35.36

Cellular functions regulated by Src family kinases. Annu Rev Cell Dev Biol (1997) 11.36

DNA related to the transforming gene(s) of avian sarcoma viruses is present in normal avian DNA. Nature (1976) 9.81

Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med (2010) 9.77

A renaissance for SRC. Nat Rev Cancer (2004) 6.27

Constitutive Stat3 activity up-regulates VEGF expression and tumor angiogenesis. Oncogene (2002) 6.17

Molecular complexity and dynamics of cell-matrix adhesions. J Cell Sci (2001) 5.77

Rous sarcoma virus: a function required for the maintenance of the transformed state. Nature (1970) 5.66

Regulation, substrates and functions of src. Biochim Biophys Acta (1996) 5.45

Purification of DNA complementary to nucleotide sequences required for neoplastic transformation of fibroblasts by avian sarcoma viruses. J Mol Biol (1976) 5.07

Hakai, a c-Cbl-like protein, ubiquitinates and induces endocytosis of the E-cadherin complex. Nat Cell Biol (2002) 5.02

Src family kinases in tumor progression and metastasis. Cancer Metastasis Rev (2003) 4.62

Mechanism of biological synergy between cellular Src and epidermal growth factor receptor. Proc Natl Acad Sci U S A (1999) 3.43

Role of Src expression and activation in human cancer. Oncogene (2000) 3.41

Differential regulation of cell motility and invasion by FAK. J Cell Biol (2003) 3.15

Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res (2005) 3.08

Identification of candidate molecular markers predicting sensitivity in solid tumors to dasatinib: rationale for patient selection. Cancer Res (2007) 2.84

Dasatinib (BMS-354825) tyrosine kinase inhibitor suppresses invasion and induces cell cycle arrest and apoptosis of head and neck squamous cell carcinoma and non-small cell lung cancer cells. Clin Cancer Res (2005) 2.76

Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res (2006) 2.41

Increase in activity and level of pp60c-src in progressive stages of human colorectal cancer. J Clin Invest (1993) 2.29

Potentiation of epidermal growth factor receptor-mediated oncogenesis by c-Src: implications for the etiology of multiple human cancers. Proc Natl Acad Sci U S A (1995) 2.29

Src protein-tyrosine kinase structure and regulation. Biochem Biophys Res Commun (2004) 2.23

Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol (2006) 2.07

Phase II study of dasatinib in patients with metastatic castration-resistant prostate cancer. Clin Cancer Res (2009) 1.99

Src family protein tyrosine kinases: cooperating with growth factor and adhesion signaling pathways. Curr Opin Cell Biol (1997) 1.97

Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival. Cancer Res (2007) 1.96

Elevated Src activity promotes cellular invasion and motility in tamoxifen resistant breast cancer cells. Breast Cancer Res Treat (2005) 1.94

Involvement of pp60c-src with two major signaling pathways in human breast cancer. Proc Natl Acad Sci U S A (1994) 1.94

Expression of pp60c-src protein kinase in adult and fetal human tissue: high activities in some sarcomas and mammary carcinomas. Cancer Res (1983) 1.88

Phase I/II study of the Src inhibitor dasatinib in combination with erlotinib in advanced non-small-cell lung cancer. J Clin Oncol (2010) 1.88

Phase II study of dasatinib in patients with advanced non-small-cell lung cancer. J Clin Oncol (2010) 1.79

Genomic strategy for targeting therapy in castration-resistant prostate cancer. J Clin Oncol (2009) 1.75

Quantitative relations between causative virus and cell in the Rous no. 1 chicken sarcoma. Virology (1955) 1.74

Analysis of pp60c-src protein kinase activity in human tumor cell lines and tissues. J Biol Chem (1986) 1.67

Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib. Mol Cancer Ther (2006) 1.66

Combined inhibition of c-Src and epidermal growth factor receptor abrogates growth and invasion of head and neck squamous cell carcinoma. Clin Cancer Res (2008) 1.63

Phase I dose-escalation and pharmacokinetic study of dasatinib in patients with advanced solid tumors. Clin Cancer Res (2009) 1.63

Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol (2009) 1.61

Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene (2008) 1.57

Antitumor effects and biomarkers of activity of AZD0530, a Src inhibitor, in pancreatic cancer. Clin Cancer Res (2009) 1.53

Overexpression and activation of the tyrosine kinase Src in human pancreatic carcinoma. Biochem Biophys Res Commun (1998) 1.52

The road to Src. Oncogene (2004) 1.51

Activation of c-Src by receptor tyrosine kinases in human colon cancer cells with high metastatic potential. Oncogene (1997) 1.48

A Src/Abl kinase inhibitor, SKI-606, blocks breast cancer invasion, growth, and metastasis in vitro and in vivo. Cancer Res (2007) 1.45

SKI-606 decreases growth and motility of colorectal cancer cells by preventing pp60(c-Src)-dependent tyrosine phosphorylation of beta-catenin and its nuclear signaling. Cancer Res (2006) 1.42

The role of Src in solid and hematologic malignancies: development of new-generation Src inhibitors. Cancer (2006) 1.41

c-Src kinase activity is required for hepatocyte growth factor-induced motility and anchorage-independent growth of mammary carcinoma cells. J Biol Chem (1998) 1.38

c-Yes tyrosine kinase activity in human colon carcinoma. Oncogene (1993) 1.35

ErbB2 promotes Src synthesis and stability: novel mechanisms of Src activation that confer breast cancer metastasis. Cancer Res (2005) 1.35

Oncogenes and onco-suppressor gene in adenocarcinoma of the oesophagus. Gut (1992) 1.31

Inhibition of c-Src expression and activation in malignant pleural mesothelioma tissues leads to apoptosis, cell cycle arrest, and decreased migration and invasion. Mol Cancer Ther (2007) 1.29

Analysis of pp60c-src in human colon carcinoma and normal human colon mucosal cells. Oncogene Res (1987) 1.29

SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res (2005) 1.29

A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study. Anticancer Drugs (2009) 1.26

Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors. Clin Cancer Res (2010) 1.23

Phase 1 pharmacokinetic and drug-interaction study of dasatinib in patients with advanced solid tumors. Cancer (2010) 1.22

Leukocyte protein tyrosine kinases: potential targets for drug discovery. Annu Rev Immunol (1997) 1.19

Src phosphorylates the insulin-like growth factor type I receptor on the autophosphorylation sites. Requirement for transformation by src. J Biol Chem (1996) 1.18

Expression of pp60c-src in human small cell and non-small cell lung carcinomas. Eur J Cancer (1992) 1.15

Preclinical evaluation of dasatinib, a potent Src kinase inhibitor, in melanoma cell lines. J Transl Med (2008) 1.13

Investigation of the Mek-MAP kinase-Rsk pathway in human breast cancer. Anticancer Res (1999) 1.11

Inhibition of Src with AZD0530 reveals the Src-Focal Adhesion kinase complex as a novel therapeutic target in papillary and anaplastic thyroid cancer. J Clin Endocrinol Metab (2009) 1.11

The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells. J Thorac Oncol (2009) 1.06

Activation of the MAP kinase pathway by FGF-1 correlates with cell proliferation induction while activation of the Src pathway correlates with migration. J Cell Biol (1998) 1.02

Phase II study of saracatinib (AZD0530) for patients with recurrent or metastatic head and neck squamous cell carcinoma (HNSCC). Anticancer Res (2011) 1.01

Efficacy and pharmacodynamic effects of bosutinib (SKI-606), a Src/Abl inhibitor, in freshly generated human pancreas cancer xenografts. Mol Cancer Ther (2009) 1.01

The Src family of protein tyrosine kinases: regulation and functions. Dev Suppl (1993) 1.00

A phase II trial of the Src kinase inhibitor saracatinib (AZD0530) in patients with metastatic or locally advanced gastric or gastro esophageal junction (GEJ) adenocarcinoma: a trial of the PMH phase II consortium. Invest New Drugs (2011) 0.98

Src activation in malignant and premalignant epithelia of Barrett's esophagus. Gastroenterology (1997) 0.97

Gene array and fluorescence in situ hybridization biomarkers of activity of saracatinib (AZD0530), a Src inhibitor, in a preclinical model of colorectal cancer. Clin Cancer Res (2010) 0.96

c-Src tyrosine phosphorylation of epidermal growth factor receptor, P190 RhoGAP, and focal adhesion kinase regulates diverse cellular processes. Chem Rev (2001) 0.95

A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer. Invest New Drugs (2010) 0.92

Altered MAP kinase (ERK1,2) regulation in primary cultures of mammary tumor cells: elevated basal activity and sustained response to EGF. Carcinogenesis (1999) 0.91

A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies. Invest New Drugs (2013) 0.89

Src stimulates insulin-like growth factor I (IGF-I)-dependent cell proliferation by increasing IGF-I receptor number in human pancreatic carcinoma cells. Cancer Res (1998) 0.89

Development of candidate genomic markers to select breast cancer patients for dasatinib therapy. Mol Cancer Ther (2010) 0.85

SRC as a target for anti-cancer drugs. Anticancer Drug Des (1996) 0.84

Src kinase inhibitors induce apoptosis and mediate cell cycle arrest in lymphoma cells. Anticancer Drugs (2007) 0.83

Overexpression of tissue inhibitor of matrix metalloproteinases-1 (TIMP-1) in metastatic MDCK cells transformed by v-src. Clin Exp Metastasis (1999) 0.81

Establishment of two new human bladder carcinoma cell lines, CAL 29 and CAL 185. Comparative study of cell scattering and epithelial to mesenchyme transition induced by growth factors. Br J Cancer (2001) 0.78

Articles by these authors

An in vivo platform for translational drug development in pancreatic cancer. Clin Cancer Res (2006) 5.52

Phase I pharmacologic and biologic study of ramucirumab (IMC-1121B), a fully human immunoglobulin G1 monoclonal antibody targeting the vascular endothelial growth factor receptor-2. J Clin Oncol (2010) 2.41

Colon cancer, version 3.2014. J Natl Compr Canc Netw (2014) 1.59

The role of functional MR imaging in the assessment of tumor response after chemoembolization in patients with hepatocellular carcinoma. J Vasc Interv Radiol (2006) 1.47

Binding of gefitinib, an inhibitor of epidermal growth factor receptor-tyrosine kinase, to plasma proteins and blood cells: in vitro and in cancer patients. Invest New Drugs (2006) 1.08

Oxaliplatin-induced neuropathy in colorectal cancer. J Oncol (2011) 1.07

Phase I safety, pharmacokinetic, and pharmacodynamic study of ENMD-2076, a novel angiogenic and Aurora kinase inhibitor, in patients with advanced solid tumors. Clin Cancer Res (2010) 0.98

A phase I study of EKB-569 in combination with capecitabine in patients with advanced colorectal cancer. Clin Cancer Res (2008) 0.89

A phase II study of the gamma secretase inhibitor RO4929097 in patients with previously treated metastatic pancreatic adenocarcinoma. Invest New Drugs (2014) 0.88

Metaanalysis of survival, complications, and imaging response following chemotherapy-based transarterial therapy in patients with unresectable intrahepatic cholangiocarcinoma. J Vasc Interv Radiol (2013) 0.85

Promising targets and drugs in development for colorectal cancer. Semin Oncol (2011) 0.77

TNF-blockade in patients with advanced hormone refractory prostate cancer. Invest New Drugs (2009) 0.76

ACR Appropriateness Criteria: rectal cancer-metastatic disease at presentation. Curr Probl Cancer (2010) 0.76

Chemotherapy agents: a primer for the interventional radiologist. Semin Intervent Radiol (2010) 0.76

Development of novel targeted agents in the treatment of metastatic colorectal cancer. Clin Colorectal Cancer (2011) 0.75