Src Family Kinases as Therapeutic Targets in Advanced Solid Tumors: What We Have Learned So Far

Efficacy and safety of dasatinib with trastuzumab and paclitaxel in first line HER2-positive metastatic breast cancer: results from the phase II GEICAM/2010-04 study

(2019) Alberto Ocana et al.   BREAST CANCER RESEARCH AND TREATMENT

Src family kinases, HCK and FGR, associate with local inflammation and tumour progression in colorectal cancer

(2019) Antonia K. Roseweir et al.   CELLULAR SIGNALLING

c-Src is required for hypoxia-induced metastasis-associated functions in prostate cancer cells

(2019) Yao Dai et al.   OncoTargets and Therapy

Targeting Tyrosine Kinases in Cancer: Lessons for an Effective Targeted Therapy in the Clinic

(2019) Adriano Angelucci   Cancers

Predictive Biomarkers of Response to Src Inhibitors in Lung Cancer: Getting to YES1

(2019) Howard Y Li et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

YES1 Drives Lung Cancer Growth and Progression and Predicts Sensitivity to Dasatinib

(2019) Irati Garmendia et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

PTPN3 suppresses lung cancer cell invasiveness by counteracting Src-mediated DAAM1 activation and actin polymerization

(2019) Meng-Yen Li et al.   ONCOGENE

EGFR–c-Src-Mediated HDAC3 Phosphorylation Exacerbates Invasion of Breast Cancer Cells

(2019) Sung-Min Kwak et al.   Cells

Leptin Promotes Expression of EMT-Related Transcription Factors and Invasion in a Src and FAK-Dependent Pathway in MCF10A Mammary Epithelial Cells

(2019) Monserrat Olea-Flores et al.   Cells

Personalized Cancer Therapy: YES1 Is the New Kid on the Block

(2019) Kunal Rai   CANCER RESEARCH

A first-in-human phase I study to determine the maximum tolerated dose of the oral Src/ABL inhibitor AZD0424

(2018) Victoria K Woodcock et al.   BRITISH JOURNAL OF CANCER

c-Src inhibitor selectively inhibits triple-negative breast cancer overexpressed Vimentin in vitro and in vivo

(2018) Longquan Lou et al.   CANCER SCIENCE

Phase II Study of Paclitaxel and Dasatinib in Metastatic Breast Cancer

(2018) Patrick G. Morris et al.   Clinical Breast Cancer

Src- and confinement-dependent FAK activation causes E-cadherin relaxation and β-catenin activity

(2018) Charlène Gayrard et al.   JOURNAL OF CELL BIOLOGY

c-Src activity is differentially required by cancer cell motility modes

(2018) Jeremy S. Logue et al.   ONCOGENE

Src-mediated regulation of the PI3K pathway in advanced papillary and anaplastic thyroid cancer

(2018) Thomas C. Beadnell et al.   Oncogenesis

Association of Dasatinib With Progression-Free Survival Among Patients With Advanced Gastrointestinal Stromal Tumors Resistant to Imatinib

(2018) Scott M. Schuetze et al.   JAMA Oncology

SRC inhibition prevents P-cadherin mediated signaling and function in basal-like breast cancer cells

(2018) Ana Sofia Ribeiro et al.   Cell Communication and Signaling

Dual Mechanisms of LYN Kinase Dysregulation Drive Aggressive Behavior in Breast Cancer Cells

(2018) Giusy Tornillo et al.   Cell Reports

Downregulation of β-arrestin 1 suppresses glioblastoma cell malignant progression vis inhibition of Src signaling

(2017) Tian Lan et al.   EXPERIMENTAL CELL RESEARCH

Dual Src and EGFR inhibition in combination with gemcitabine in advanced pancreatic cancer: phase I results

(2017) Dana B. Cardin et al.   INVESTIGATIONAL NEW DRUGS

Phase I study of the combination of crizotinib (as a MET inhibitor) and dasatinib (as a c-SRC inhibitor) in patients with advanced cancer

(2017) Shumei Kato et al.   INVESTIGATIONAL NEW DRUGS

Structural and functional insights into the interaction between the Cas family scaffolding protein p130Cas and the focal adhesion-associated protein paxillin

(2017) Chi Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Src nuclear localization and its prognostic relevance in human osteosarcoma

(2017) Enrica Urciuoli et al.   JOURNAL OF CELLULAR PHYSIOLOGY

AC-93253 iodide, a novel Src inhibitor, suppresses NSCLC progression by modulating multiple Src-related signaling pathways

(2017) Yi-Hua Lai et al.   Journal of Hematology & Oncology

Augmentation of the anticancer activity of CYT997 in human prostate cancer by inhibiting Src activity

(2017) Yong Teng et al.   Journal of Hematology & Oncology

miR-140-5p suppresses the proliferation, migration and invasion of gastric cancer by regulating YES1

(2017) Zheng Fang et al.   Molecular Cancer

IL6 is associated with response to dasatinib and cetuximab: Phase II clinical trial with mechanistic correlatives in cetuximab-resistant head and neck cancer

(2017) L.P. Stabile et al.   ORAL ONCOLOGY

A pathology atlas of the human cancer transcriptome

(2017) Mathias Uhlen et al.   SCIENCE

LPP is a Src substrate required for invadopodia formation and efficient breast cancer lung metastasis

(2017) Elaine Ngan et al.   Nature Communications

TRIB1 promotes colorectal cancer cell migration and invasion through activation MMP-2 via FAK/Src and ERK pathways

(2017) Yuhui Wang et al.   Oncotarget

FRK inhibits breast cancer cell migration and invasion by suppressing epithelial-mesenchymal transition

(2017) Yetunde Ogunbolude et al.   Oncotarget

Promotion of Tumor Invasion by Tumor-Associated Macrophages: The Role of CSF-1-Activated Phosphatidylinositol 3 Kinase and Src Family Kinase Motility Signaling

(2017) Amy Dwyer et al.   Cancers

Phase 2 Placebo-Controlled, Double-Blind Trial of Dasatinib Added to Gemcitabine for Patients with Locally-Advanced Pancreatic Cancer

(2016) T. R. J. Evans et al.   ANNALS OF ONCOLOGY

A randomized, double-blind phase II study evaluating cediranib versus cediranib and saracatinib in patients with relapsed metastatic clear-cell renal cancer (COSAK)

(2016) T. Powles et al.   ANNALS OF ONCOLOGY

Phase II studies of two different schedules of dasatinib in bone metastasis predominant metastatic breast cancer: SWOG S0622

(2016) Anne F. Schott et al.   BREAST CANCER RESEARCH AND TREATMENT

Phase II Study of Dasatinib in Previously Treated Patients with Advanced Non-Small Cell Lung Cancer

(2016) Michael J. Kelley et al.   CANCER INVESTIGATION

TBCRC-010: Phase I/II Study of Dasatinib in Combination with Zoledronic Acid for the Treatment of Breast Cancer Bone Metastasis

(2016) Z. Mitri et al.   CLINICAL CANCER RESEARCH

Combined KIT and CTLA-4 Blockade in Patients with Refractory GIST and Other Advanced Sarcomas: A Phase Ib Study of Dasatinib plus Ipilimumab

(2016) Sandra P. D'Angelo et al.   CLINICAL CANCER RESEARCH

Suppression of SRC Signaling Is Effective in Reducing Synergy between Glioblastoma and Stromal Cells

(2016) Alessia Calgani et al.   MOLECULAR CANCER THERAPEUTICS

Src as a Therapeutic Target in Biliary Tract Cancer

(2016) Ah-Rong Nam et al.   MOLECULAR CANCER THERAPEUTICS

FYN promotes breast cancer progression through epithelial-mesenchymal transition

(2016) Ye-Gong Xie et al.   ONCOLOGY REPORTS

Bakuchiol suppresses proliferation of skin cancer cells by directly targeting Hck, Blk, and p38 MAP kinase

(2016) Jong-Eun Kim et al.   Oncotarget

Micro-Environmental Stress Induces Src-Dependent Activation of Invadopodia and Cell Migration in Ewing Sarcoma

(2016) Kelly M. Bailey et al.   NEOPLASIA

SARC009: Phase 2 study of dasatinib in patients with previously treated, high-grade, advanced sarcoma

(2015) Scott M. Schuetze et al.   CANCER

A phase II study of saracatinib (AZD0530), a Src inhibitor, administered orally daily to patients with advanced thymic malignancies

(2015) Matthew A. Gubens et al.   LUNG CANCER

Src family kinases differentially influence glioma growth and motility

(2015) Laura J. Lewis-Tuffin et al.   Molecular Oncology

Deregulated Expression of SRC, LYN and CKB Kinases by DNA Methylation and Its Potential Role in Gastric Cancer Invasiveness and Metastasis

(2015) Adriano Azevedo Mello et al.   PLoS One

Saracatinib as a metastasis inhibitor in metastatic castration-resistant prostate cancer: A University of Chicago Phase 2 Consortium and DOD/PCF Prostate Cancer Clinical Trials Consortium Study

(2015) Edwin M. Posadas et al.   PROSTATE

Tissue-based map of the human proteome

(2015) M. Uhlen et al.   SCIENCE

Yes-mediated phosphorylation of focal adhesion kinase at tyrosine 861 increases metastatic potential of prostate cancer cells

(2015) Tanushree Chatterji et al.   Oncotarget

Lyn modulates Claudin-2 expression and is a therapeutic target for breast cancer liver metastasis

(2015) Sébastien Tabariès et al.   Oncotarget

A novel nuclear Src and p300 signaling axis controls migratory and invasive behavior in pancreatic cancer

(2015) David Paladino et al.   Oncotarget

Focal adhesion kinase-dependent focal adhesion recruitment of SH2 domains directs SRC into focal adhesions to regulate cell adhesion and migration

(2015) Jui-Chung Wu et al.   Scientific Reports

Overcoming EMT-associated resistance to anti-cancer drugs via Src/FAK pathway inhibition

(2015) Catherine Wilson et al.   Oncotarget

Bosutinib plus capecitabine for selected advanced solid tumours: results of a phase 1 dose-escalation study

(2014) S J Isakoff et al.   BRITISH JOURNAL OF CANCER

Gene Signature-Guided Dasatinib Therapy in Metastatic Breast Cancer

(2014) L. Pusztai et al.   CLINICAL CANCER RESEARCH

Src inhibition potentiates antitumoral effect of paclitaxel by blocking tumor-induced angiogenesis

(2014) Simona Delle Monache et al.   EXPERIMENTAL CELL RESEARCH

The role of Src family kinases in growth and migration of glioma stem cells

(2014) XIAOSI HAN et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Phosphatase CD45 Both Positively and Negatively Regulates T Cell Receptor Phosphorylation in Reconstituted Membrane Protein Clusters

(2014) Gabriela Furlan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Bosutinib in Combination With the Aromatase Inhibitor Letrozole: A Phase II Trial in Postmenopausal Women Evaluating First-Line Endocrine Therapy in Locally Advanced or Metastatic Hormone Receptor-Positive/HER2-Negative Breast Cancer

(2014) B. Moy et al.   ONCOLOGIST

A Phase I/II Study Combining Erlotinib and Dasatinib for Non-Small Cell Lung Cancer

(2014) K. A. Gold et al.   ONCOLOGIST

Bosutinib in Combination With the Aromatase Inhibitor Exemestane: A Phase II Trial in Postmenopausal Women With Previously Treated Locally Advanced or Metastatic Hormone Receptor-Positive/HER2-Negative Breast Cancer

(2014) B. Moy et al.   ONCOLOGIST

Role of c-Src activity in the regulation of gastric cancer cell migration

(2014) YUN YANG et al.   ONCOLOGY REPORTS

The Inhibition of Src Family Kinase Suppresses Pancreatic Cancer Cell Proliferation, Migration, and Invasion

(2014) Dong Wook Je et al.   PANCREAS

Src as the link between inflammation and cancer

(2014) Sandy T. Liu et al.   Frontiers in Physiology

Phosphorylation of unique domains of Src family kinases

(2014) Irene Amata et al.   Frontiers in Genetics

A phase II trial of dasatinib in patients with metastatic castration-resistant prostate cancer treated previously with chemotherapy

(2013) Przemyslaw W. Twardowski et al.   ANTI-CANCER DRUGS

Dasatinib plus Capecitabine for Advanced Breast Cancer: Safety and Efficacy in Phase I Study CA180004

(2013) G. Somlo et al.   CLINICAL CANCER RESEARCH

A Phase II Trial of Saracatinib, an Inhibitor of src Kinases, in Previously-Treated Advanced Non–Small-Cell Lung Cancer: The Princess Margaret Hospital Phase II Consortium

(2013) Scott A. Laurie et al.   Clinical Lung Cancer

Crosstalk between Activated and Inactivated c-Src in Hepatocellular Carcinoma

(2013) Mei-Lin Chen et al.   DISEASE MARKERS

Phase I study of dasatinib in combination with capecitabine, oxaliplatin and bevacizumab followed by an expanded cohort in previously untreated metastatic colorectal cancer

(2013) John H. Strickler et al.   INVESTIGATIONAL NEW DRUGS

Treatment-Related Toxicities in a Phase II Trial of Dasatinib in Patients with Squamous Cell Carcinoma of the Lung

(2013) Andrew M. Brunner et al.   Journal of Thoracic Oncology

Docetaxel and dasatinib or placebo in men with metastatic castration-resistant prostate cancer (READY): a randomised, double-blind phase 3 trial

(2013) John C Araujo et al.   LANCET ONCOLOGY

Phase II Study of Dasatinib (BMS-354825) in Patients With Metastatic Adenocarcinoma of the Pancreas

(2013) C. E. Chee et al.   ONCOLOGIST

In silico identification of oncogenic potential of fyn-related kinase in hepatocellular carcinoma

(2012) Jia-Shing Chen et al.   BIOINFORMATICS

Effects of Src kinase inhibition by saracatinib (AZD0530) on bone turnover in advanced malignancy in a Phase I study

(2012) Rosemary A. Hannon et al.   BONE

Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours

(2012) S Kaye et al.   BRITISH JOURNAL OF CANCER

A Phase I Trial of Dasatinib, an Src-Family Kinase Inhibitor, in Combination with Paclitaxel and Carboplatin in Patients with Advanced or Recurrent Ovarian Cancer

(2012) A. A. Secord et al.   CLINICAL CANCER RESEARCH

Targeted Inhibition of Src Kinase with Dasatinib Blocks Thyroid Cancer Growth and Metastasis

(2012) C. M. Chan et al.   CLINICAL CANCER RESEARCH

Src-mediated regulation of E-cadherin and EMT in pancreatic cancer

(2012) Nagaraj et al.   Frontiers in Bioscience-Landmark

First report of the safety, tolerability, and pharmacokinetics of the Src kinase inhibitor saracatinib (AZD0530) in Japanese patients with advanced solid tumours

(2012) Yasuhito Fujisaka et al.   INVESTIGATIONAL NEW DRUGS

A phase 1 study of gemcitabine combined with dasatinib in patients with advanced solid tumors

(2012) David S. Hong et al.   INVESTIGATIONAL NEW DRUGS

Phase II study of the Src kinase inhibitor saracatinib (AZD0530) in metastatic melanoma

(2012) Tara C. Gangadhar et al.   INVESTIGATIONAL NEW DRUGS

Src-mediated phosphorylation of mammalian Abp1 (DBNL) regulates podosome rosette formation in transformed fibroblasts

(2012) L. R. Boateng et al.   JOURNAL OF CELL SCIENCE

A phase I study of dasatinib and weekly paclitaxel for metastatic breast cancer

(2011) M. N. Fornier et al.   ANNALS OF ONCOLOGY

Phase II study of single-agent bosutinib, a Src/Abl tyrosine kinase inhibitor, in patients with locally advanced or metastatic breast cancer pretreated with chemotherapy

(2011) M. Campone et al.   ANNALS OF ONCOLOGY

Phase I clinical trial of the Src inhibitor dasatinib with dacarbazine in metastatic melanoma

(2011) A P Algazi et al.   BRITISH JOURNAL OF CANCER

Phase I study of dasatinib (BMS-354825) in Japanese patients with solid tumors

(2011) Shunji Takahashi et al.   CANCER SCIENCE

Phase II Trial of Saracatinib (AZD0530), an Oral SRC-inhibitor for the Treatment of Patients with Hormone Receptor-negative Metastatic Breast Cancer

(2011) Ayca Gucalp et al.   Clinical Breast Cancer

Phase I Study of Bosutinib, a Src/Abl Tyrosine Kinase Inhibitor, Administered to Patients with Advanced Solid Tumors

(2011) A. I. Daud et al.   CLINICAL CANCER RESEARCH

A Phase 2 Trial of Dasatinib in Patients with Advanced HER2-Positive and/or Hormone Receptor-Positive Breast Cancer

(2011) E. L. Mayer et al.   CLINICAL CANCER RESEARCH

Phase II Trial of Dasatinib in Patients with Metastatic Breast Cancer Using Real-Time Pharmacodynamic Tissue Biomarkers of Src Inhibition to Escalate Dosing

(2011) Christina I. Herold et al.   CLINICAL CANCER RESEARCH

Phase I open-label study of cediranib, an oral inhibitor of VEGF signalling, in combination with the oral Src inhibitor saracatinib in patients with advanced solid tumours

(2011) Tanja Trarbach et al.   INVESTIGATIONAL NEW DRUGS

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

(2011) Helen J. Mackay et al.   INVESTIGATIONAL NEW DRUGS

Phase I and pharmacokinetic study of dasatinib and cetuximab in patients with advanced solid malignancies

(2011) Athanassios Argiris et al.   INVESTIGATIONAL NEW DRUGS

Phase II Trial of Dasatinib for Patients with Acquired Resistance to Treatment with the Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors Erlotinib or Gefitinib

(2011) Melissa L. Johnson et al.   Journal of Thoracic Oncology

Combating trastuzumab resistance by targeting SRC, a common node downstream of multiple resistance pathways

(2011) Siyuan Zhang et al.   NATURE MEDICINE

MicroRNA-mediated upregulation of integrin-linked kinase promotes Src-induced tumor progression

(2011) C Oneyama et al.   ONCOGENE

Specific Oncogenic Activity of the Src-Family Tyrosine Kinase c-Yes in Colon Carcinoma Cells

(2011) Florence Sancier et al.   PLoS One

Once-daily Dasatinib: Expansion of Phase II Study Evaluating Safety and Efficacy of Dasatinib in Patients With Metastatic Castration-resistant Prostate Cancer

(2011) Evan Y. Yu et al.   UROLOGY

Inhibition of epithelial to mesenchymal transition in metastatic breast carcinoma cells by c-Src suppression

(2010) Xiang Liu et al.   ACTA BIOCHIMICA ET BIOPHYSICA SINICA

Phase 2 study of dasatinib in the treatment of head and neck squamous cell carcinoma

(2010) Heather D. Brooks et al.   CANCER

A phase 2 trial of dasatinib in advanced melanoma

(2010) Harriet M. Kluger et al.   CANCER

A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer

(2010) Daniel J. Renouf et al.   INVESTIGATIONAL NEW DRUGS

Phosphorylation of Ser 21 in Fyn regulates its kinase activity, focal adhesion targeting, and is required for cell migration

(2010) Myeong Gu Yeo et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Phase I/II Study of the Src Inhibitor Dasatinib in Combination With Erlotinib in Advanced Non–Small-Cell Lung Cancer

(2010) Eric B. Haura et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II Study of Dasatinib in Patients With Advanced Non–Small-Cell Lung Cancer

(2010) Faye M. Johnson et al.   JOURNAL OF CLINICAL ONCOLOGY

Elevated c-Src and c-Yes expression in malignant skin cancers

(2010) Jang Lee et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Epithelial-Mesenchymal Transition in Cancer: Parallels Between Normal Development and Tumor Progression

(2010) Douglas S. Micalizzi et al.   JOURNAL OF MAMMARY GLAND BIOLOGY AND NEOPLASIA

c-Src–Mediated Phosphorylation of NoxA1 and Tks4 Induces the Reactive Oxygen Species (ROS)–Dependent Formation of Functional Invadopodia in Human Colon Cancer Cells

(2010) Davide Gianni et al.   MOLECULAR BIOLOGY OF THE CELL

Identification of c-Src as a Potential Therapeutic Target for Gastric Cancer and of MET Activation as a Cause of Resistance to c-Src Inhibition

(2010) W. Okamoto et al.   MOLECULAR CANCER THERAPEUTICS

A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study

(2009) Primo N. Lara et al.   ANTI-CANCER DRUGS

Rak Functions as a Tumor Suppressor by Regulating PTEN Protein Stability and Function

(2009) Eun-Kyoung Yim et al.   CANCER CELL

Phase II Study of Dasatinib in Patients with Metastatic Castration-Resistant Prostate Cancer

(2009) E. Y. Yu et al.   CLINICAL CANCER RESEARCH

Phase I Dose-Escalation and Pharmacokinetic Study of Dasatinib in Patients with Advanced Solid Tumors

(2009) G. D. Demetri et al.   CLINICAL CANCER RESEARCH

Cortactin regulates cofilin and N-WASp activities to control the stages of invadopodium assembly and maturation

(2009) Matthew Oser et al.   JOURNAL OF CELL BIOLOGY

An integrin αvβ3–c-Src oncogenic unit promotes anchorage-independence and tumor progression

(2009) Jay S Desgrosellier et al.   NATURE MEDICINE

Src kinases as therapeutic targets for cancer

(2009) Lori C. Kim et al.   Nature Reviews Clinical Oncology

The Role of Src in Solid Tumors

(2009) D. L. Wheeler et al.   ONCOLOGIST

N-WASP and cortactin are involved in invadopodium-dependent chemotaxis to EGF in breast tumor cells

(2009) Vera DesMarais et al.   CELL MOTILITY AND THE CYTOSKELETON

Targeting Src Family Kinases Inhibits Growth and Lymph Node Metastases of Prostate Cancer in an Orthotopic Nude Mouse Model

(2008) S. I. Park et al.   CANCER RESEARCH

Focal adhesion kinase is not required for Src-induced formation of invadopodia in KM12C colon cancer cells and can interfere with their assembly

(2008) S VITALE et al.   EUROPEAN JOURNAL OF CELL BIOLOGY

Preclinical evaluation of dasatinib, a potent Src kinase inhibitor, in melanoma cell lines

(2008) Alex J Eustace et al.   Journal of Translational Medicine

Inhibition of Src Family Kinases with Dasatinib Blocks Migration and Invasion of Human Melanoma Cells

(2008) R. Buettner et al.   MOLECULAR CANCER RESEARCH

The Tyrosine Kinase Activity of c-Src Regulates Actin Dynamics and Organization of Podosomes in Osteoclasts

(2007) Olivier Destaing et al.   MOLECULAR BIOLOGY OF THE CELL