PubMed Journals Articles About "Tyrosine Kinase Inhibitors Cancer" 
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Showing "Tyrosine kinase inhibitors Cancer" PubMed Articles 1–25 of 48,000+
Ponatinib in refractory Philadelphia chromosome-positive leukemias.
Resistance to tyrosine kinase inhibitors in patients with chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph-positive ALL) is frequently caused by mutations in the BCR-ABL kinase domain. Ponatinib (AP24534) is a potent oral tyrosine kinase inhibitor that blocks native and mutated BCR-ABL, including the gatekeeper mutant T315I, which is uniformly resistant to tyrosine kinase inhibitors.
Membrane receptors with tyrosine kinase activity and cytoplasmic tyrosine kinases have emerged as important potential targets in oncology. Starting from basic structures such as anilino-quinazoline, numerous compounds have been synthesised, with the help of tyrosine kinase crystallography, which has allowed to optimise protein-ligand interactions. The catalytic domains of all kinases present similar three-dimensional structures, which explains that it may be difficult to identify molecules having a high spe...
Potential Therapies for Anaplastic Lymphoma Kinase-Driven Tumors in Children: Progress to Date.
Anaplastic lymphoma kinase (ALK) is an oncogenic tyrosine kinase that is deregulated due to a variety of molecular mechanisms in pediatric cancer. They include chromosomal translocations, activation mutations, and gene amplifications. Since the initial discovery of ALK as an oncogenic tyrosine kinase involved in the chromosomal translocation t(2, 5)(p23;q35) in 1994, more than 20 translocation partners of ALK have been identified in various cancers. Furthermore, deregulation of ALK tyrosine kinase activity...
Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain.
Erlotinib and gefitinib, tyrosine kinase inhibitors used to block epidermal growth factor receptor (EGFR) signaling in cancer, are thought to bind only the active conformation of the EGFR tyrosine kinase domain (EGFR-TKD). Through parallel computational and crystallographic studies, we show here that erlotinib also binds the inactive EGFR-TKD conformation, which may have significant implications for its use in EGFR-mutated cancers.
Will Kinase Inhibitors Make it as Glioblastoma Drugs?
Kinase inhibitors have emerged as effective cancer therapeutics in a variety of human cancers. Glioblastoma (GBM), the most common malignant brain tumor in adults, represents a compelling disease for kinase inhibitor therapy because the majority of these tumors harbor genetic alterations that result in aberrant activation of growth factor signaling pathways. Attempts to target the Ras-Phosphatidylinositol 3-kinase (PI3K)-mammalian Target of Rapamycin (mTOR) axis in GBM with first generation receptor tyrosin...
Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.
A series of azulene-based derivatives were synthesized as potent inhibitors for receptor tyrosine kinases such as FMS-like tyrosine kinase 3 (FLT-3). Systematic side chain modification of prototype 1a was carried out through SAR studies. Analogue 22 was identified from this series and found to be one of the most potent FLT-3 inhibitors, with good pharmaceutical properties, superior efficacy, and tolerability in a tumor xenograft model.
Rational design of highly selective spleen tyrosine kinase inhibitors.
A novel approach to design selective spleen tyrosine kinase (Syk) inhibitors is described. Inhibition of spleen tyrosine kinase has attracted much attention as a mechanism for the treatment of autoimmune diseases such as asthma, rheumatoid arthritis, and SLE. Fostamatinib, a Syk inhibitor that successfully completed phase II clinical trials, also exhibits some undesirable side effects. More selective Syk inhibitors could offer safer, alternative treatments. Through a systematic evaluation of the kinome, we...
Small molecule inhibitors of the IGF-1R/IR axis for the treatment of cancer.
Introduction: The IGF-1 receptor (IGF-1R) is a receptor tyrosine kinase and is well established as a key regulator of tumor cell growth and survival. There is also a growing body of data to support a role for the structurally and functionally related insulin receptor (IR) in human cancer. Bidirectional crosstalk between IGF-1R and IR is observed, where specific inhibition of either receptor confers a compensatory increase in the activity for the reciprocal receptor, therefore dual inhibition of both IGF-1R...
Targeting non-malignant disorders with tyrosine kinase inhibitors.
Receptor and non-receptor tyrosine kinases are involved in multiple proliferative signalling pathways. Imatinib, one of the first tyrosine kinase inhibitors (TKIs) to be approved, revolutionized the treatment of chronic myelogenous leukaemia, and other TKIs with different spectra of kinase inhibition are used to treat renal cell carcinoma, non-small-cell lung cancer and colon cancer. Studies also support the potential use of TKIs as anti-proliferative agents in non-malignant disorders such as cardiac hypert...
In order to identify therapeutic targets and prognostic markers for basal breast cancers, breast cancer cell lines were subjected to mass spectrometry-based profiling of protein tyrosine phosphorylation events. This revealed that luminal and basal breast cancer cells exhibit distinct tyrosine phosphorylation signatures that depend on pathway activation as well as protein expression. Basal breast cancer cells are characterized by elevated tyrosine phosphorylation of Met, Lyn, EphA2, EGFR and FAK, and Src fam...
The Philadelphia chromosome is the most common cytogenetic abnormality found in adult patients diagnosed with acute lymphoblastic leukemia. The result of this abnormality is the BCR-ABL protein, a constitutively active kinase involved in cell signaling and survival. When managed with multiagent chemotherapy regimens alone, patients have traditionally had an inferior outcome in terms of remission duration and overall survival when compared with patients who are Philadelphia chromosome-negative. Small-molecul...
Tyrosine Kinase Inhibitors, Pancreatic Hyperenzymemia and Acute Pancreatitis: A Review.
The advent of new drugs can rapidly increase the number of substances causing acute pancreatitis. This is the case of tyrosine kinase inhibitors; these drugs are currently used for chronic myeloid leukemia, gastrointestinal stromal tumors, unresectable hepatocellular carcinomas and advanced renal cell carcinomas that have been reported to cause acute pancreatitis or asymptomatic elevations of serum pancreatic enzymes. Of the classes of drugs capable of inducing acute pancreatitis, we aimed to evaluate, in w...
MET and KRAS Gene Amplification Mediates Acquired Resistance to MET Tyrosine Kinase Inhibitors.
The establishment of the role of MET in human cancer has led to the development of small-molecule inhibitors, many of which are currently in clinical trials. Thus far, nothing is known about their therapeutic efficacy and the possible emergence of resistance to treatment, a problem that has been often observed with other receptor tyrosine kinase (RTK) inhibitors. To predict mechanisms of acquired resistance, we generated resistant cells by treating MET-addicted cells with increasing concentrations of the ME...
Smac mimetics: implications for enhancement of targeted therapies in leukemia.
Drug resistance is a growing concern with clinical use of tyrosine kinase inhibitors. Utilizing in vitro models of intrinsic drug resistance and stromal-mediated chemoresistance, as well as functional mouse models of progressive and residual disease, we attempted to develop a potential therapeutic approach designed to suppress leukemia recurrence following treatment with selective kinase inhibitors. The novel inhibitor of apoptosis (IAP), LCL161, was observed to potentiate the effects of tyrosine kinase inh...
Optimization of our bis-anilino-pyrimidine series of EphB4 kinase inhibitors led to the discovery of compound 12 which incorporates a key m-hydroxymethylene group on the C4 aniline. 12 displays a good kinase selectivity profile, good physical properties and pharmacokinetic parameters, suggesting it is a suitable candidate to investigate the therapeutic potential of EphB4 kinase inhibitors.
KIT and KIT: from biology to clinical use.
Scientific knowledge on gastrointestinal stromal tumors (GIST) has highly progressed over the last 10 years. The molecular bases of oncogenic transformation, KIT activating mutations, were identified in 1998 by Hirota et al. The product of KIT proto-oncogene, KIT protein, is a transmembrane receptor with tyrosine kinase activity. Tyrosine kinase inhibitors targeting these mutated activated kinases, namely imatinib and more recently sunitinib, nilotinib, masitinib or sorafenib, have deeply modified GIST pro...
Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the properties of this series. The structure-activity relationships against IGF-1R kinase activity as well as inhibition of the hERG ion channel are discussed.
BACKGROUND: Src tyrosine kinase and matrix metalloproteinase play the pivotal roles in lung cancer invasion and metastasis. The aim of this study is to evaluate the effect of Src tyrosine kinase inhibition on secretion of matrix metalloproteinase 2 (MMP-2) and matrix metalloproteinase 9 (MMP-9) by non-small cell lung cancer (NSCLC) cells. METHODS: ELISA was used to examine the activity of MMP-2 and MMP-9 produced by NSCLC cells (PC14PE6, H226, PC-9, A549) as well as the effect of Src tyrosine kinase inhibit...
ROS receptor tyrosine kinase: a new potential target for anticancer drugs.
ROS kinase is one of the last two remaining orphan receptor tyrosine kinases with an as yet unidentified ligand. The normal functions of human ROS kinase in different body tissues have not been fully identified so far. However, the ectopic expression, as well as the production of variable mutant forms of ROS kinase has been reported in a number of cancers, such as glioblastoma multiforme, and non-small cell lung cancer, suggesting a role for ROS kinase in deriving such tumors. It is thought also that c-ROS...
Increasing numbers of tyrosine kinase inhibitors (TKIs) were studied and approved for therapy of malignancies and other diseases. The aim of this study was to develop and validate a specific, simple and rapid quantification method for various TKIs in human plasma.
Receptor-guided 3D-QSAR approach for the discovery of c-kit tyrosine kinase inhibitors.
Studies of the the three-dimensional quantitative structure-activity relationships for ninety-five c-kit tyrosine kinase inhibitors were performed. Based on a co-crystallized compound (1 T46), known inhibitors were aligned with c-kit by induced-fit docking, and multiple training/test set splitting was performed to validate the selected pharmacophore model. The best pharmacophore model consisted of five features: one hydrogen-bond donor and four aromatic rings. Reliable statistics were obtained (R...
Flavonoids as receptor tyrosine kinase FLT3 inhibitors.
The Fms-like tyrosine kinase 3 (FLT3), a receptor tyrosine kinase, is involved in the proliferation, differentiation and apoptosis of hematopoietic cells. FLT3 is highly overexpressed in acute myeloid leukemia (AML) of the majority of patients. Screening for flavonoids including flavones, flavanones, flavonols, and flavanonols disclosed that luteolin was potent FLT3 enzyme inhibitor. Furthermore, luteolin suppressed cell proliferation in MV4;11 cells with constitutively activated FLT3.
The presence of epidermal growth factor receptor (EGFR) somatic mutations in non-small cell lung cancer patients is associated with response to treatment with EGFR-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib and erlotinib. More than one hundred mutations in the kinase domain of EGFR have been identified. In particular there are many variations of deletion mutations in exon 19. In this study, we examined the differences in sensitivity to gefitinib, erlotinib and afatinib of several exon 19 muta...
BACKGROUND:: Atypical teratoid/rhaboid tumors (AT/RTs) and extracranial malignant rhabdoid tumors are highly malignant neoplasms with a dismal prognosis. These tumors predominantly affect infants and targeted, adjuvant treatment approaches would be highly desirable. METHODS:: In the current study, the authors investigated the expression and functional role of tyrosine kinases in 2 malignant rhabdoid tumor cell lines (A204 and G401) and in a series of 5 AT/RTs and 18 malignant rhabdoid tumors (13 rhabdoid tu...
Importance of the field: Bruton's tyrosine kinase (BTK) has emerged as a new anti-apoptotic molecular target for the treatment of B-lineage leukemias and lymphomas. Preclinical and early clinical results indicate that BTK inhibitors may be useful in the treatment of leukemias and lymphomas. BTK inhibitors may also be helpful in prevention and treatment of thromboembolic complications as well as inflammatory disorders. Areas covered in this review: We provide a comprehensive review of the target diseases for...
