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Bruton’s tyrosine kinase inhibition reduces disease severity in a model of secondary progressive autoimmune demyelination
Bruton’s tyrosine kinase (BTK) is an emerging target in multiple sclerosis (MS). Alongside its role in B cell receptor signaling and B cell...
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Interaction of the chemotherapeutic agent oxaliplatin and the tyrosine kinase inhibitor dasatinib with the organic cation transporter 2
Oxaliplatin (OHP) is effective in colorectal cancer treatment but induces peripheral neurotoxicity (OHP-induced peripheral neurotoxicity, OIPN),...
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HER Receptor, Current, and Emerging Therapeutic Targets
The human epidermal growth factor receptor (HER/ErbB) family consists of four members: HER-1 or epidermal growth factor receptor (EGFR), HER-2,...
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Playing Hide-and-Seek with Tyrosine Kinase Inhibitors: Can We Overcome Administration Challenges?
Tyrosine kinase inhibitors (TKIs) have demonstrated significant efficacy against various types of cancers through molecular targeting mechanisms....
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Impact of therapeutic inhibition of oncogenic cell signaling tyrosine kinase on cell metabolism: in vivo-detectable metabolic biomarkers of inhibition
BackgroundInhibition of kinases is the ever-expanding therapeutic approach to various types of cancer. Typically, assessment of the treatment...
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Mitochondrial Dysfunction in Cardiotoxicity Induced by BCR-ABL1 Tyrosine Kinase Inhibitors -Underlying Mechanisms, Detection, Potential Therapies
The advent of BCR-ABL tyrosine kinase inhibitors (TKIs) targeted therapy revolutionized the treatment of chronic myeloid leukemia (CML) patients....
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Discovery of mobocertinib, a new irreversible tyrosine kinase inhibitor indicated for the treatment of non-small-cell lung cancer harboring EGFR exon 20 insertion mutations
Epidermal growth factor receptor (EGFR) is essential for normal cellular functions. Mutations of EGFR’s kinase domain can cause dysregulation leading...
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Inhibition of MER proto-oncogene tyrosine kinase by an antisense oligonucleotide enhances treatment efficacy of immunoradiotherapy
BackgroundThe combination of radiotherapy and immunotherapy (immunoradiotherapy) has been increasingly used for treating a wide range of cancers....
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Fyn Kinase in Alzheimer’s Disease: Unraveling Molecular Mechanisms and Therapeutic Implications
Alzheimer’s disease, characterized by the accumulation of abnormal protein aggregates and neuronal damage in the brain, leads to a gradual decline in...
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AXL receptor tyrosine kinase: a possible therapeutic target in acute promyelocytic leukemia
BackgroundAcute promyelocytic leukemia (APL) is a subset of acute myeloid leukemia (AML) which is characterized by the fusion of promyelocytic...
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The G Protein–Coupled Receptor PAC1 Regulates Transactivation of the Receptor Tyrosine Kinase HER3
Peptide G protein–coupled receptors (GPCRs) for pituitary adenylate cyclase activating polypeptide (PACAP) regulate the growth of non-small cell lung...
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Dual Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors: The Quest for a Disease-Modifying Treatment for Alzheimer’s Disease
Alzheimer’s disease (AD) is a multifactor disease that is a most familiar form of dementia. Neurofibrillary tangles (NFTs) and amyloid-β (Aβ) are the...
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Lymphocyte-Specific Protein Tyrosine Kinase Contributes to Spontaneous Regression of Liver Fibrosis may by Interacting with Suppressor of Cytokine Signaling 1
Quiescent hepatic stellate cells (qHSCs), converted to myofibroblasts, produce fibrous scars, which is an essential event during liver fibrogenesis....
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The Ephrin tyrosine kinase a3 (EphA3) is a novel mediator of RAGE-prompted motility of breast cancer cells
BackgroundThe receptor for advanced glycation-end products (RAGE) and its ligands have been implicated in obesity and associated inflammatory...
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Elucidating the phosphoregulatory network of predominant phosphosite in AXL kinase: an integrative bioinformatic approach
AXL is a tumor-associated macrophage (TAM) family receptor tyrosine kinase (RTK). TAM receptors have been implicated in various cellular processes,...
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Anti-angiogenic therapy using the multi-tyrosine kinase inhibitor Regorafenib enhances tumor progression in a transgenic mouse model of ß-cell carcinogenesis
BackgroundPancreatic neuroendocrine tumors (PNETs) represent a distinct hypervascularized tumor entity, often diagnosed at metastatic stage....
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Pirtobrutinib inhibits wild-type and mutant Bruton’s tyrosine kinase-mediated signaling in chronic lymphocytic leukemia
Pirtobrutinib (LOXO-305), a reversible inhibitor of Bruton’s tyrosine kinase (BTK), was designed as an alternative strategy to treat...
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PP121, a dual inhibitor of tyrosine and phosphoinositide kinases, relieves airway hyperresponsiveness, mucus hypersecretion and inflammation in a murine asthma model
BackgroundTyrosine kinase and phosphoinositide kinase pathways play important roles in asthma formation. As a dual tyrosine and phosphoinositide...
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HER2-positive breast cancer and tyrosine kinase inhibitors: the time is now
Human epidermal growth factor receptor 2 (HER2) positive breast cancer accounts for 20–25% of all breast cancers. Multiple HER2-targeted therapies...
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Recent Advances in FDA-Approved Kinase Inhibitors Targeting Lung Cancer
Lung cancer is a chronic deadly disease and is implicated with highest mortality rate among all cancers since years. Kinase are the...