Definition Tyrosine kinase inhibitors ( TKIs ) are small molecules that bind to and inhibit the activity of tyrosine kinases. The latter are enzymes that catalyze the phosphorylation of a protein on the tyrosine residue using adenosine triphosphate as a substrate. The activities of tyrosine kinases ...
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 ...
In the human genome, ninety tyrosine kinases have been identified, including fifty-six receptor tyrosine kinases and thirty-two cellular tyrosine kinases.4Tyrosine kinase inhibitors (TKIs) used as targeted therapies are designed to perturb the cellular pathways that regulate malignant cell growth.1TKI ...
Tyrosine kinase inhibitors Small moleculetyrosine kinase inhibitors(TKIs) have demonstratedantitumor activity. They not only target theVEGF receptor(VEGFR), but also inhibit platelet-derived growth factor receptor (PDGFR),fibroblast growth factor receptor(FGFR),epidermal growth factor receptor(EGFR), rearran...
Tyrosine kinases are implicated in tumorigenesis and progression, and have emerged as major targets for drug discovery. Tyrosine kinase inhibitors (TKIs) inhibit corresponding kinases from phosphorylating tyrosine residues of their substrates and then block the activation of downstream signaling pathways. Ove...
Tyrosine kinases are implicated in tumorigenesis and progression, and have emerged as major targets for drug discovery. Tyrosine kinase inhibitors (TKIs) inhibit corresponding kinases from phosphorylating tyrosine residues of their substrates and then block the activation of downstream signaling pathways. Ove...
The goal of this work is to determine the role of the autoimmune cells in multiple sclerosis (MS) induction and the immunomodulatory mechanism of therapy with tyrosine kinase inhibitors (TKIs) in MS attenuation. Samples (5 × 10(5) cells per well) of C6 and primary rat astrocytes were...
Over the last ten years, several new and therapeutically relevant cancer drugs targeting tyrosine kinase signaling pathways have been developed. Tyrosine kinase inhibitors (TKIs) are a pharmaceutical class of small molecules, orally available, well-tolerated, worldwide approved drugs for the treatment of...
Resistance to tyrosine kinase inhibitors (TKIs) has been a major challenge for targeted therapies that impairs their clinical efficacies. Methods Eighty-six NSCLC patients were categorized into three cohorts based on the time of detecting MET tyrosine kinase domain (TKD) mutations (cohort 1: at ...
The clinical benefit of tyrosine kinase inhibitors (TKIs)-based systemic therapy for advanced hepatocellular carcinoma (HCC) is limited due to drug resistance. Here, we uncover that lipid metabolism reprogramming mediated by unconventional prefoldin RPB5 interactor (URI) endows HCC with resistance to TK...