PubMed Journals Articles About "Tyrosine Kinase Inhibitors Cancer" RSS

09:11 EDT 1st April 2015 | BioPortfolio

Tyrosine Kinase Inhibitors Cancer PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Tyrosine Kinase Inhibitors Cancer articles that have been published worldwide.

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Showing "Tyrosine kinase inhibitors Cancer" PubMed Articles 1–25 of 20,000+

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Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors from the Natural Origin: A Recent Perspective.

Overexpression of epidermal growth factor receptor (EGFR) is seen in number of human tumors like prostate, colon, breast and ovarian. Their expression is correlated with vascularity and often difficult to diagnose. Though a number of active inhibitors and anticancer drugs against EGFR-tyrosine kinase are known, increase in resistance together with many side effects designate the need for new and improved treatments. Natural products and their analoges have significant contribution in the cancer drug discove...

Recent advances in irreversible kinase inhibitors.

Despite concerns of off-target selectivity and cytotoxicity, there has been a resurgence in interest in irreversible kinase inhibitors resulting in more than 60 disclosed patent and patent applications over the past 4 years. Many of these inhibitors possess several key advantages over their reversible counterparts. The patent literature from 2010 to 2013 has been reviewed and novel irreversible kinase inhibitors for Bruton's tyrosine kinase, epidermal growth factor receptor, Janus kinase 3, phosphoinsitide ...

Different efficacy of EGFR tyrosine kinase inhibitors and prognosis in patients with subtypes of EGFR-mutated advanced non-small cell lung cancer: a meta-analysis.

Nearly 85 % of lung-cancer-specific epidermal growth factor receptor (EGFR) sensitive mutations comprise a substitution at position 858 (21L858R) and deletion mutants in exon 19 (19del). The aim of this study was to assess the role of EGFR mutation subtypes in predicting the efficacy of EGFR tyrosine kinase inhibitors (EGFR TKIs) and the prognosis of patients with advanced non-small cell lung cancer (NSCLC).

Nomogram Predicting Clinical Outcomes in Non-Small Cell Lung Cancer Patients Treated with Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors.

The aim of this study was to develop a pragmatic nomogram for prediction of progression free survival (PFS) for the epidermal growth factor (EGFR) tyrosine kinase inhibitor (TKI) in EGFR mutant non-small cell lung cancer (NSCLC).

Meta-Analysis of EGFR Tyrosine Kinase Inhibitors Compared with Chemotherapy as Second-Line Treatment in Pretreated Advanced Non-Small Cell Lung Cancer.

Since efficacy and safety of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) versus chemotherapy in the treatment of patients with pretreated advanced non-small cell lung cancer (NSCLC) remain controversial, we performed a meta-analysis to compare them.

Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.

A new chimeric fusion transcript of KIF5B (the kinesin family 5B gene) and the RET (Rearranged during Transcription) oncogene, KIF5B-RET, was found in 1~2% of lung adenocarcinomas (LADCs) in late 2011. Several related clinical trials for non-small cell lung cancer (NSCLC) with KIF5B-RET rearrangements have been swiftly initiated by the discovery of KIF5B-RET fusion gene using existing RET inhibitors such as lenvatinib, vandetanib, sunitinib, ponatinib, cabozatinib, and AUY922. Anti-RET activity and their st...

The tyrosine kinase inhibitor nilotinib has antineoplastic activity in prostate cancer cells but up-regulates the ERK survival signal-Implications for targeted therapies.

Novel therapeutic options beyond hormone ablation and chemotherapy are urgently needed for patients with advanced prostate cancer. Tyrosine kinase inhibitors (TKIs) are an attractive option as advanced prostate cancers show a highly altered phosphotyrosine proteome. However, despite favorable initial clinical results, the combination of the TKI dasatinib with docetaxel did not result in improved patient survival for reasons that are not known in detail.

Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer.

Introduction: EGFR has been implicated in various malignancies such as NSCLC, breast, head and neck, and pancreatic cancer. Numerous drugs have been developed in order to target the tyrosine domain of EGFR as an approach in cancer treatment. Areas covered: This article focuses on the different generations of EGFR tyrosine kinase inhibitors (TKIs). This spans from the emergence of the first-generation EGFR-TKIs to overcoming drug resistance using second-generation EGFR-TKIs and to reducing adverse effect (AE...

Unexpected off-targets and paradoxical pathway activation by kinase inhibitors.

Protein kinase inhibitors are an increasingly important class of targeted anti-cancer therapeutics. More than two dozen new drugs of this class have entered routine clinical use over the past decade. This review article focuses on how the development of methods to study the kinome- and proteome-wide selectivity of kinase inhibitors, in conjunction with advances in the structural understanding of kinase inhibitor binding modes, has resulted in a better appreciation of the mechanism of action of clinical kina...

Repositioning of Tyrosine Kinase Inhibitors as Antagonists of ATP-Binding Cassette Transporters in Anticancer Drug Resistance.

The phenomenon of multidrug resistance (MDR) has attenuated the efficacy of anticancer drugs and the possibility of successful cancer chemotherapy. ATP-binding cassette (ABC) transporters play an essential role in mediating MDR in cancer cells by increasing efflux of drugs from cancer cells, hence reducing the intracellular accumulation of chemotherapeutic drugs. Interestingly, small-molecule tyrosine kinase inhibitors (TKIs), such as AST1306, lapatinib, linsitinib, masitinib, motesanib, nilotinib, telatini...

Tyrosine Kinase Inhibitors as Reversal Agents for ABC Transporter Mediated Drug Resistance.

Tyrosine kinases (TKs) play an important role in pathways that regulate cancer cell proliferation, apoptosis, angiogenesis and metastasis. Aberrant activity of TKs has been implicated in several types of cancers. In recent years, tyrosine kinase inhibitors (TKIs) have been developed to interfere with the activity of deregulated kinases. These TKIs are remarkably effective in the treatment of various human cancers including head and neck, gastric, prostate and breast cancer and several types of leukemia. How...

Primary and Secondary Resistance to Tyrosine Kinase Inhibitors in Lung Cancer.

Background: Tyrosine kinase inhibitors (TKI) have emerged as important therapeutic agents for the treatment of several types of cancer including lung cancer. Recent research attempts show that only a small population of cancer patients responds to TKI and furthermore, these patients eventually develop resistance. Studies support the classification of resistance in primary and secondary resistance. Materials and Methods: In the present study the differentiation between primary and secondary resistance to TKI...

Icotinib, a selective EGF receptor tyrosine kinase inhibitor, for the treatment of non-small-cell lung cancer.

ABSTRACT  Advanced non-small-cell lung cancer (NSCLC) is the main cause for cancer-related mortality. Treatments for advanced NSCLC are largely palliative and a benefit plateau appears to have reached with the platinum-based chemotherapy regimens. EGF receptor (EGFR) tyrosine kinase inhibitors gefitinib, erlotinib and afatinib came up with prolonged progression-free survival and improved quality of life, especially in EGFR-mutated patients. Icotinib is an oral selective EGFR tyrosine kinase, which was app...

Bruton's tyrosine kinase inhibitors: lessons learned from bench-to-bedside (first) studies.

Targeted inhibitors of B-cell receptor signaling have emerged as the most promising therapeutic options against non-Hodgkin's lymphoma. The inhibitor agents that target Bruton's tyrosine kinase (BTK) have elicited particularly high enthusiasm given the unprecedented positive responses observed in Phase I trials. The sheer amount of clinical data published since last year now requires reinterpretation in light of recently published findings on BTK.

Imatinib: a breakthrough of targeted therapy in cancer.

Deregulated protein tyrosine kinase activity is central to the pathogenesis of human cancers. Targeted therapy in the form of selective tyrosine kinase inhibitors (TKIs) has transformed the approach to management of various cancers and represents a therapeutic breakthrough. Imatinib was one of the first cancer therapies to show the potential for such targeted action. Imatinib, an oral targeted therapy, inhibits tyrosine kinases specifically BCR-ABL, c-KIT, and PDGFRA. Apart from its remarkable success in CM...

The Efficacy of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer Harboring Wild-type Epidermal Growth Factor Receptor: A Meta-analysis of 25 RCTs.

To determine the efficacy of first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in advanced non-small cell lung cancer (NSCLC) patients with wild-type (WT) EGFR tumors, we performed an indirect meta-analysis to assess the treatment effects of EGFR-TKIs in such patients.

Tyrosine Kinase Inhibition Regulates Early Systemic Immune Changes and Modulates the Neuroimmune Response in α-Synucleinopathy.

Neuro-inflammation is common in α-Synucleinopathies and Tauopathies; and evidence suggests a link between the tyrosine kinase Abl and neurodegeneration. Abl upregulates α-Synuclein and promotes Tau hyper-phosphorylation (p-Tau), while Abl inhibitors facilitate autophagic clearance.

Rapid Evaluation of Tyrosine Kinase Activity of Membrane-Integrated Human Epidermal Growth Factor Receptor Using the Yeast Gγ Recruitment System.

Epidermal growth factor receptor (EGFR) is a member of the receptor tyrosine kinase family and plays key roles in the regulation of fundamental cellular processes, including cell proliferation, migration, differentiation, and survival. Deregulation of EGFR tyrosine kinase activity is involved in the development and progression of human cancers. In the present study, we attempted to develop a method to evaluate the tyrosine kinase activity of human EGFR using the yeast Gγ recruitment system. Autophosphoryla...

Cyclin-dependent kinase 4/6 inhibitors in breast cancer therapy.

To review the latest preclinical and clinical findings on the role of cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors in breast cancer and update on the studies investigating the predictive biomarkers of response to CDK4/6 inhibitors.

Tyrosine kinase inhibitors improve long-term outcome of allogeneic hematopoietic stem cell transplantation for adult patients with Philadelphia chromosome positive acute lymphoblastic leukemia.

This study aimed to determine the impact of tyrosine-kinase inhibitors given pre- and post-allogeneic stem cell transplantation on long term outcome of patients allografted for Philadelphia chromosome-positive acute lymphoblastic leukemia. This retrospective analysis from the Acute Leukemia Working Party of EBMT included 473 de novo Philadelphia chromosome-positive acute lymphoblastic leukemia patients in first complete remission who underwent an allogeneic stem cell transplantation using an human leucocyte...

Rationale for co-targeting IGF-1R and ALK in ALK fusion-positive lung cancer.

Crizotinib, a selective tyrosine kinase inhibitor (TKI), shows marked activity in patients whose lung cancers harbor fusions in the gene encoding anaplastic lymphoma receptor tyrosine kinase (ALK), but its efficacy is limited by variable primary responses and acquired resistance. In work arising from the clinical observation of a patient with ALK fusion-positive lung cancer who had an exceptional response to an insulin-like growth factor 1 receptor (IGF-1R)-specific antibody, we define a therapeutic synergi...

Current Molecularly Targeting Therapies in NSCLC and Melanoma.

Surgery, radiation therapy, and chemotherapy are the traditional options to control tumor progression. However, these strategies are fraught with harmful side effects and are ineffective in metastatic and advanced cancers. Biomarkers that are overexpressed in cancers and are involved in cell growth, proliferation, migration, and survival have recently become the focus of new molecular targeting therapies. Novel therapies targeting biomarkers have roles in tumorigenesis that are overexpressed in cancers may ...

A kinase-independent function of AKT promotes cancer cell survival.

The serine-threonine kinase AKT regulates proliferation and survival by phosphorylating a network of protein substrates. Here we describe a kinase-independent function of AKT. In cancer cells harboring gain-of-function alterations in MET, HER2, or Phosphatidyl-Inositol-3-Kinase (PI3-K), catalytically-inactive AKT (K179M) protected from druginduced cell death in a PH-domain dependent manner. An AKT kinase domain mutant found in human melanoma (G161V) lacked enzymatic activity in-vitro and in AKT1/AKT2 double...

An Interaction Map of Small-molecule Kinase Inhibitors with Anaplastic Lymphoma Kinase (ALK) Mutants in ALK-positive Non-Small Cell Lung Cancer.

Human anaplastic lymphoma kinase (ALK) has become a well-established target for the treatment of ALK-positive non-small cell lung cancer (NSCLC). Here, we have profiled seven small-molecule inhibitors, including 2 that are approved drugs, against a panel of clinically relevant mutations in ALK tyrosine kinase (TK) domain, aiming at a comprehensive understanding of molecular mechanism and biological implication underlying inhibitor response to ALK TK mutation. We find that (i) the gatekeeper mutation L1196M ...

Safety and activity of temsirolimus and bevacizumab in patients with advanced renal cell carcinoma previously treated with tyrosine kinase inhibitors: a phase 2 consortium study.

Bevacizumab or temsirolimus regimens have clinical activity in the first-line treatment of advanced renal cell carcinoma (RCC). This phase I/II trial was conducted to determine the safety of combining both agents and its efficacy in RCC patients who progressed on at least one prior anti-VEGF receptor tyrosine kinase inhibitor (RTKI) agent.


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