Small-Molecule Inhibitors of the Receptor Tyrosine Kinases: Promising Tools for Targeted Cancer Therapies

SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo

(2014) Lu Wang et al.   CANCER LETTERS

Effects of Icotinib on Advanced Non-Small Cell Lung Cancer with Different EGFR Phenotypes

(2014) Huiyun Pan et al.   CELL BIOCHEMISTRY AND BIOPHYSICS

Abstract B30: Selective small molecule AXL inhibitor BGB324 overcomes acquired drug resistance in non-small cell lung carcinoma models.

(2014) Katarzyna Wnuk-Lipinska et al.   CLINICAL CANCER RESEARCH

Hepatocellular Carcinoma: Reasons for Phase III Failure and Novel Perspectives on Trial Design

(2014) J. M. Llovet et al.   CLINICAL CANCER RESEARCH

Targeting of the MET receptor tyrosine kinase by small molecule inhibitors leads to MET accumulation by impairing the receptor downregulation

(2014) Dominic Leiser et al.   FEBS LETTERS

The ROR1 pseudokinase diversifies signaling outputs in MET-addicted cancer cells

(2014) Alessandra Gentile et al.   INTERNATIONAL JOURNAL OF CANCER

The novel kinase inhibitor EMD1214063 is effective against neuroblastoma

(2014) Kathy Scorsone et al.   INVESTIGATIONAL NEW DRUGS

Pan-erbB inhibition potentiates BRAF inhibitors for melanoma treatment

(2014) Yuen-Keng Ng et al.   MELANOMA RESEARCH

The receptor tyrosine kinase ROR1 – An oncofetal antigen for targeted cancer therapy

(2014) Mohammad Hojjat-Farsangi et al.   SEMINARS IN CANCER BIOLOGY

Yhhu3813 is a novel selective inhibitor of c-Met Kinase that inhibits c-Met-dependent neoplastic phenotypes of human cancer cells

(2013) Chang-xi He et al.   ACTA PHARMACOLOGICA SINICA

Protective autophagy is involved in resistance towards MET inhibitors in human gastric adenocarcinoma cells

(2013) Magali Humbert et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia

(2013) E. I. Zimmerman et al.   BLOOD

Analytic performance studies and clinical reproducibility of a real-time PCRassay for the detection of epidermal growth factor receptor gene mutations informalin-fixed paraffin-embedded tissue specimens of non-small cell lungcancer

(2013) Patrick O’Donnell et al.   BMC CANCER

A Phase I dose-escalation study of the VEGFR inhibitor tivozanib hydrochloride with weekly paclitaxel in metastatic breast cancer

(2013) Erica L. Mayer et al.   BREAST CANCER RESEARCH AND TREATMENT

Dramatic Antitumor Effects of the Dual MET/RON Small-Molecule Inhibitor LY2801653 in Non-Small Cell Lung Cancer

(2013) I. Kawada et al.   CANCER RESEARCH

Distinct Effects of Ligand-Induced PDGFR  and PDGFR  Signaling in the Human Rhabdomyosarcoma Tumor Cell and Stroma Cell Compartments

(2013) M. Ehnman et al.   CANCER RESEARCH

Current challenges and clinical investigations of epidermal growth factor receptor (EGFR)- and ErbB family-targeted agents in the treatment of head and neck squamous cell carcinoma (HNSCC)

(2013) Roger B. Cohen   CANCER TREATMENT REVIEWS

Inhibition of Tumor Growth and Metastasis in Non-Small Cell Lung Cancer by LY2801653, an Inhibitor of Several Oncokinases, Including MET

(2013) W. Wu et al.   CLINICAL CANCER RESEARCH

EMD 1214063 and EMD 1204831 Constitute a New Class of Potent and Highly Selective c-Met Inhibitors

(2013) F. Bladt et al.   CLINICAL CANCER RESEARCH

Targeting MET: why, where and how?

(2013) Elena Ghiso et al.   CURRENT OPINION IN PHARMACOLOGY

Tyrosine Kinase Inhibitors: Their On-Target Toxicities as Potential Indicators of Efficacy

(2013) Devron R. Shah et al.   DRUG SAFETY

Promising New Molecular Targeted Therapies in Head and Neck Cancer

(2013) Kelly Dorsey et al.   DRUGS

First-Line Management of EGFR-Mutated Advanced Lung Adenocarcinoma: Recent Developments

(2013) Bin-Chi Liao et al.   DRUGS

FLT3 inhibitors for acute myeloid leukemia: a review of their efficacy and mechanisms of resistance

(2013) Michael R. Grunwald et al.   INTERNATIONAL JOURNAL OF HEMATOLOGY

Cancer Development, Progression, and Therapy: An Epigenetic Overview

(2013) Sibaji Sarkar et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Tivozanib Versus Sorafenib As Initial Targeted Therapy for Patients With Metastatic Renal Cell Carcinoma: Results From a Phase III Trial

(2013) Robert J. Motzer et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase III Randomized Trial Comparing the Efficacy of Cediranib As Monotherapy, and in Combination With Lomustine, Versus Lomustine Alone in Patients With Recurrent Glioblastoma

(2013) Tracy T. Batchelor et al.   JOURNAL OF CLINICAL ONCOLOGY

FLT3tyrosine kinase inhibitors in acute myeloid leukemia: clinical implications and limitations

(2013) Sabine Kayser et al.   LEUKEMIA & LYMPHOMA

The Novel ATP-Competitive Inhibitor of the MET Hepatocyte Growth Factor Receptor EMD1214063 Displays Inhibitory Activity against Selected MET-Mutated Variants

(2013) Michaela Medová et al.   MOLECULAR CANCER THERAPEUTICS

Inhibition of the Receptor Tyrosine Kinase ROR1 by Anti-ROR1 Monoclonal Antibodies and siRNA Induced Apoptosis of Melanoma Cells

(2013) Mohammad Hojjat-Farsangi et al.   PLoS One

Small Molecule ErbB Inhibitors Decrease Proliferative Signaling and Promote Apoptosis in Philadelphia Chromosome–Positive Acute Lymphoblastic Leukemia

(2013) Mary E. Irwin et al.   PLoS One

The Tyrosine Kinase Receptor ROR1 Is Constitutively Phosphorylated in Chronic Lymphocytic Leukemia (CLL) Cells

(2013) Mohammad Hojjat-Farsangi et al.   PLoS One

The molecular basis of targeting protein kinases in cancer therapeutics

(2013) Chung-Jung Tsai et al.   SEMINARS IN CANCER BIOLOGY

MET: A Critical Player in Tumorigenesis and Therapeutic Target

(2013) C. R. Graveel et al.   Cold Spring Harbor Perspectives in Biology

EGFR Tyrosine Kinase Inhibitors: Difference in Efficacy and Resistance

(2013) Kyle W. Robinson et al.   Current Oncology Reports

ADME of Biologics—What Have We Learned from Small Molecules?

(2012) Thomayant Prueksaritanont et al.   AAPS Journal

Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation

(2012) Yao Dai et al.   CLINICAL & EXPERIMENTAL METASTASIS

Crenolanib Inhibits the Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors

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

Trastuzumab emtansine for advanced HER2-positive breast cancer and beyond: genome landscape-based targets

(2012) William CS Cho et al.   Expert Review of Anticancer Therapy

Expression pattern and targeting of HER family members and IGF-IR in pancreatic cancer

(2012) N Ioannou   Frontiers in Bioscience-Landmark

Novel targeted agents for the treatment of advanced breast cancer

(2012) Máximo de la Vega et al.   Future Medicinal Chemistry

Cediranib: a VEGF receptor tyrosine kinase inhibitor

(2012) Marina Sahade et al.   Future Oncology

LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models

(2012) S. Betty Yan et al.   INVESTIGATIONAL NEW DRUGS

Cediranib With mFOLFOX6 Versus Bevacizumab With mFOLFOX6 As First-Line Treatment for Patients With Advanced Colorectal Cancer: A Double-Blind, Randomized Phase III Study (HORIZON III)

(2012) Hans-Joachim Schmoll et al.   JOURNAL OF CLINICAL ONCOLOGY

Tivantinib for second-line treatment of advanced hepatocellular carcinoma: a randomised, placebo-controlled phase 2 study

(2012) Armando Santoro et al.   LANCET ONCOLOGY

Monoclonal antibodies against ROR1 induce apoptosis of chronic lymphocytic leukemia (CLL) cells

(2012) A H Daneshmanesh et al.   LEUKEMIA

Orphan receptor tyrosine kinases ROR1 and ROR2 in hematological malignancies

(2012) Amir Hossein Daneshmanesh et al.   LEUKEMIA & LYMPHOMA

MET: a promising anticancer therapeutic target

(2012) Solange Peters et al.   Nature Reviews Clinical Oncology

Mechanisms of intrinsic and acquired resistance to kinase-targeted therapies

(2012) Shubha Bagrodia et al.   Pigment Cell & Melanoma Research

ROR1 Is Expressed in Human Breast Cancer and Associated with Enhanced Tumor-Cell Growth

(2012) Suping Zhang et al.   PLoS One

Anticancer molecules targeting fibroblast growth factor receptors

(2012) Guang Liang et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Phase II trial of modified FOLFOX6 and erlotinib in patients with metastatic or advanced adenocarcinoma of the oesophagus and gastro-oesophageal junction

(2011) Z A Wainberg et al.   BRITISH JOURNAL OF CANCER

Targeting the HER/EGFR/ErbB Family to Prevent Breast Cancer

(2011) L. R. Howe et al.   Cancer Prevention Research

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

A Phase I Dose-Escalation Study of Tivantinib (ARQ 197) in Adult Patients with Metastatic Solid Tumors

(2011) L. S. Rosen et al.   CLINICAL CANCER RESEARCH

Biologic and Clinical Activity of Tivozanib (AV-951, KRN-951), a Selective Inhibitor of VEGF Receptor-1, -2, and -3 Tyrosine Kinases, in a 4-Week-On, 2-Week-Off Schedule in Patients with Advanced Solid Tumors

(2011) F. A. L. M. Eskens et al.   CLINICAL CANCER RESEARCH

Selectivity Filters to Edit Out Deleterious Side Effects in Kinase Inhibitors

(2011) Sean Sessel et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

BIBW 2992 in non-small cell lung cancer

(2011) Deepa S Subramaniam et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

A Novel Mode of Protein Kinase Inhibition Exploiting Hydrophobic Motifs of Autoinhibited Kinases

(2011) Sudharshan Eathiraj et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies

(2011) Fenlai Tan et al.   LUNG CANCER

Drug development to overcome resistance to EGFR inhibitors in lung and colorectal cancer

(2011) Rodrigo Dienstmann et al.   Molecular Oncology

Treatment of Non–Small-Cell Lung Cancer with Erlotinib or Gefitinib

(2011) Vince D. Cataldo et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Role of Irreversible HER Family Inhibition in the Treatment of Patients with Non-Small Cell Lung Cancer

(2011) E. Kwak   ONCOLOGIST

Development of Second-Generation VEGFR Tyrosine Kinase Inhibitors: Current Status

(2011) Pankaj Bhargava et al.   Current Oncology Reports

Durable Complete Response of Metastatic Gastric Cancer with Anti-Met Therapy Followed by Resistance at Recurrence

(2011) D. V. T. Catenacci et al.   Cancer Discovery

The novel receptor tyrosine kinase Axl is constitutively active in B-cell chronic lymphocytic leukemia and acts as a docking site of nonreceptor kinases: implications for therapy

(2010) A. K. Ghosh et al.   BLOOD

Effects of vatalanib on tumor growth can be potentiated by mTOR blockade in vivo

(2010) Agnes Jaeger-Lansky et al.   CANCER BIOLOGY & THERAPY

R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

(2010) S. J. Holland et al.   CANCER RESEARCH

The Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors Vatalanib and Pazopanib Potently Induce Apoptosis in Chronic Lymphocytic Leukemia Cells In vitro and In vivo

(2010) J. Paesler et al.   CLINICAL CANCER RESEARCH

Non-ATP Competitive Protein Kinase Inhibitors

(2010) L. Garuti et al.   CURRENT MEDICINAL CHEMISTRY

Aberrant expression of c-met and HGF/c-met pathway provides survival advantage in B-chronic lymphocytic leukemia

(2010) Emel Eksioglu-Demiralp et al.   CYTOMETRY PART B-CLINICAL CYTOMETRY

Taking aim at Mer and Axl receptor tyrosine kinases as novel therapeutic targets in solid tumors

(2010) Rachel MA Linger et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

A Phase II Trial of Erlotinib in Recurrent Squamous Cell Carcinoma of the Cervix

(2010) Russell J. Schilder et al.   INTERNATIONAL JOURNAL OF GYNECOLOGICAL CANCER

Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors

(2010) Qiong Zhao et al.   LUNG CANCER

ARQ 197, a Novel and Selective Inhibitor of the Human c-Met Receptor Tyrosine Kinase with Antitumor Activity

(2010) N. Munshi et al.   MOLECULAR CANCER THERAPEUTICS

Breakdown of endocytosis in the oncogenic activation of receptor tyrosine kinases

(2009) Jasmine V. Abella et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation

(2009) Y. Shiotsu et al.   BLOOD

A randomized, phase II, dose-finding study of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer

(2009) Olivier Rixe et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Phase II Study of Erlotinib in Patients With Locally Advanced or Metastatic Papillary Histology Renal Cell Cancer: SWOG S0317

(2009) Michael S. Gordon et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Study of the Safety, Tolerability, and Pharmacokinetics of Oral CP-868,596, a Highly Specific Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitor in Patients With Advanced Cancers

(2009) Nancy L. Lewis et al.   JOURNAL OF CLINICAL ONCOLOGY

Protein kinase inhibitors: contributions from structure to clinical compounds

(2009) Louise N. Johnson   QUARTERLY REVIEWS OF BIOPHYSICS

A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response

(2008) K. W. Pratz et al.   BLOOD

The Tyrosine Kinase Inhibitor Cediranib Blocks Ligand-Induced Vascular Endothelial Growth Factor Receptor-3 Activity and Lymphangiogenesis

(2008) C. A. Heckman et al.   CANCER RESEARCH

Met Receptor Contributes to Trastuzumab Resistance of Her2-Overexpressing Breast Cancer Cells

(2008) D. L. Shattuck et al.   CANCER RESEARCH

Anti-tumor activity and tumor vessel normalization by the vascular endothelial growth factor receptor tyrosine kinase inhibitor KRN951 in a rat peritoneal disseminated tumor model

(2008) Eri Taguchi et al.   CANCER SCIENCE

Kinase switching in mesenchymal-like non-small cell lung cancer lines contributes to EGFR inhibitor resistance through pathway redundancy

(2008) Stuart Thomson et al.   CLINICAL & EXPERIMENTAL METASTASIS

Unique Cell Surface Expression of Receptor Tyrosine Kinase ROR1 in Human B-Cell Chronic Lymphocytic Leukemia

(2008) S. Baskar et al.   CLINICAL CANCER RESEARCH

Role of platelet-derived growth factors in physiology and medicine

(2008) J. Andrae et al.   GENES & DEVELOPMENT

Ror1, a cell surface receptor tyrosine kinase is expressed in chronic lymphocytic leukemia and may serve as a putative target for therapy

(2008) Amir H. DaneshManesh et al.   INTERNATIONAL JOURNAL OF CANCER

Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor

(2008) A. J. Gonzales et al.   MOLECULAR CANCER THERAPEUTICS