103,527 results match your criteria receptor tyrosine

EGFR Aggregation in the Brain.

ACS Chem Neurosci 2021 May 12. Epub 2021 May 12.

Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.

Recent findings showed that preformed fibrils (PFFs) of misfolded proteins, including α-synuclein (α-syn) and amyloid-β (Aβ), activate EGFR in cell cultures and animal models of amyloid propagation. Comparing these supramolecular structures to normal EGFR ligands such as EGF and HB-EGF suggests that these PFFs might trigger the formation of high order clustering of EGFR that stimulates the aggregation of EGFR tyrosine kinase domain (EGFR-TKD) which is known to form fibrils. Subsequently, self-assembled fibril of EGFR-TKDs itself can serve as a seed to induce aggregation of monomeric forms of misfolded proteins in cytoplasm or endosomes. Read More

View Article and Full-Text PDF

Sirtuin1 and Chronic Myeloid Leukemia: a Comprehensive Glance at Drug Resistance.

Clin Lab 2021 May;67(5)

Background: Chronic myeloid leukemia (CML) is a myeloproliferative disorder, which is caused by BCR-ABL fusion that has tyrosine kinase activity. The emergence of the first generation of tyrosine kinase inhibitors increased survival in patients. CML patients remain in silent phase for a long time by using drugs such as imatinib. Read More

View Article and Full-Text PDF

A non-small cell lung cancer (NSCLC) patient with leptomeningeal metastasis harboring rare epidermal growth factor receptor (EGFR) mutations G719S and L861Q benefited from doubling dosage of osimertinib: a case report.

Ann Palliat Med 2021 May 8. Epub 2021 May 8.

Department of Neuro-Oncology, Guangdong Sanjiu Brain Hospital, Guangzhou, China.

Leptomeningeal metastasis (LM) is a rare but lethal complication of advanced non-small cell lung cancer (NSCLC) that has a devastating impact on patient survival and quality of life. Osimertinib, an irreversible tyrosine kinase inhibitor, is approved as a therapy for advanced NSCLC with epidermal growth factor receptor (EGFR) mutation. However, the efficacy and optimal dosage of osimertinib in the treatment of NSCLC patients with LM who harbor uncommon EGFR mutations have yet to be fully investigated. Read More

View Article and Full-Text PDF

Successful osimertinib rechallenge following subsequent chemotherapy regimen in a patient with metastatic non-small cell lung carcinoma: a case report.

Ann Palliat Med 2021 Apr 21. Epub 2021 Apr 21.

Department of Respiratory Disease, Daping Hospital, Army Medical University, Chongqing, China.

Although tyrosine kinase inhibitors (TKIs) targeting epidermal growth factor receptor (EGFR) have a favorable and durable treatment response, almost all patients will eventually acquire resistance and develop disease progression. Re-administration of first and second-generation EGFR TKIs has been successfully executed in advanced non-small cell lung cancer (NSCLC) subsequent to EGFR-TKI resistance. However, osimertinib rechallenge following osimertinib resistance in EGFR T790M-negative patient is less explored. Read More

View Article and Full-Text PDF

Insulin-Like Growth Factors-1 Receptor (IGF-1R) Expression and the Phosphorylation of Endogenous Substrates Lead to Maturation of the Pacific oyster, .

Dev Reprod 2021 Mar 31;25(1):67-72. Epub 2021 Mar 31.

Dept. of Fisheries Biology, Pukyong National University, Busan 48513, Korea.

This study investigated the IGF-1 signal in specific tissues using Pacific oysters artificially matured via water temperature elevation. Pacific oysters were subjected to water temperature elevation from March to June, and 20 were randomly sampled each month. The condition index (CI) and tissue weight rate (TWR) were examined by measuring shell length, shell height, shell width, and soft tissue weight. Read More

View Article and Full-Text PDF

Long-term response to osimertinib in elderly patients with lung adenocarcinoma harbouring de novo T790M: a case report and literature review.

Respirol Case Rep 2021 Jun 4;9(6):e00759. Epub 2021 May 4.

Department of Respiratory Medicine and Allergology Sapporo Medical University School of Medicine Sapporo Japan.

Osimertinib is a potent and irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that selectively acts on both EGFR-sensitive and T790M-resistant mutations. Patients with pre-treatment T790M mutations (de novo T790M) respond poorly to existing EGFR-TKIs, whereas osimertinib has positive effects. However, the safety data for first-line osimertinib treatment in patients aged >75 years are insufficient. Read More

View Article and Full-Text PDF

A Case of Delayed Diagnostic Pulmonary Tuberculosis during Targeted Therapy in an EGFR Mutant Non-Small Cell Lung Cancer Patient.

Caibao Jin Bin Yang

Case Rep Oncol 2021 Jan-Apr;14(1):659-663. Epub 2021 Apr 6.

Department of Thoracic Oncology, Hubei Cancer Hospital, Wuhan, China.

The coexistence of lung cancer and pulmonary tuberculosis (TB) is rare, and the clinical and radiological features are always similar between lung cancer and pulmonary TB. In the present case, a non-small cell lung cancer patient with an epidermal growth factor receptor (EGFR)-sensitive mutation was diagnosed with pulmonary TB during the treatment of tyrosine kinase inhibitor (TKI) because of the discrepant and confusing responses among different lesions. Therefore, we should combine clinical and radiological characteristics with pathological and microbiological tests to confirm the diagnosis of TB or lung cancer. Read More

View Article and Full-Text PDF

Acute Generalized Exanthematous Pustulosis Caused by Erlotinib in a Patient with Lung Cancer.

Case Rep Oncol 2021 Jan-Apr;14(1):599-603. Epub 2021 Mar 29.

Division of Hematology, Respiratory Medicine and Oncology, Department of Internal Medicine, Faculty of Medicine, Saga University, Saga, Japan.

Acute generalized exanthematous pustulosis (AGEP) is a rare drug-related adverse skin reaction caused mainly by antibiotics. Erlotinib is an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) used to treat lung cancer. A 69-year-old woman with primary lung cancer (adenocarcinoma, cT3N1M1b, stage IVB) developed erythema and multiple skin pustules on her abdomen and both thighs after 7 weeks of erlotinib treatment. Read More

View Article and Full-Text PDF

Clonal Upregulation of Effector Cytotoxic T Lymphocytes in a Patient with Multiple Tyrosine Kinase Inhibitor-Refractory Chronic Myeloid Leukemia with Long-Term Survival.

Case Rep Oncol 2021 Jan-Apr;14(1):493-499. Epub 2021 Mar 22.

Department of Hematology, Japanese Red Cross Nagasaki Genbaku Hospital, Nagasaki, Japan.

We present the case of a patient with multiple tyrosine kinase inhibitor (TKI)-refractory chronic phase chronic myeloid leukemia (CP-CML) with a T315I mutation of . Dasatinib, a second-generation TKI, was administered as the initial treatment but achieved neither a cytogenetic nor molecular response. A mutational analysis of revealed that the patient had a T315I mutation. Read More

View Article and Full-Text PDF

Combination of Crizotinib and Osimertinib in T790M+ EGFR-Mutant Non-Small Cell Lung Cancer with Emerging MET Amplification Post-Osimertinib Progression in a 10-Year Survivor: A Case Report.

Case Rep Oncol 2021 Jan-Apr;14(1):477-482. Epub 2021 Mar 18.

Department of Thoracic Oncology, Thoraxklinik, University of Heidelberg, Heidelberg, Germany.

Tyrosine kinase inhibitors (TKIs) represent the standard treatment for patients with non-small cell lung cancer (NSCLC) harboring epidermal growth factor receptor (EGFR) mutations. The duration of the response is, however, limited in time owing to the development of resistance mechanisms to both first- and second-generation agents such as oncogene amplification. This report describes the successful results obtained with the combination of the third-generation TKI osimertinib with the multitargeted TKI and MET inhibitor crizotinib in a patient with EGFR-mutant NSCLC with emerging MET amplification with a tolerable toxicity profile. Read More

View Article and Full-Text PDF

Gαi1 Promoted Proliferation, Migration and Invasion via Activating the Akt-mTOR/Erk-MAPK Signaling Pathway in Renal Cell Carcinoma.

Onco Targets Ther 2021 4;14:2941-2952. Epub 2021 May 4.

Department of Urology, The Second Affiliated Hospital of Nantong University, Nantong, People's Republic of China.

Background: Renal cell carcinoma (RCC) accounts for about 2-3% of all adult malignancies. G protein alpha inhibitory subunit 1 (Gαi1) plays a key role in mediating PI3K-Akt signaling upon activation of receptor tyrosine kinases (RTKs). However, little is known about its expression, regulation and biological function in RCC. Read More

View Article and Full-Text PDF

Activation of transmembrane receptor tyrosine kinase DDR1-STAT3 cascade by extracellular matrix remodeling promotes liver metastatic colonization in uveal melanoma.

Signal Transduct Target Ther 2021 May 12;6(1):176. Epub 2021 May 12.

State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic Center, Sun Yat-sen University, Guangzhou, China.

Colonization is believed a rate-limiting step of metastasis cascade. However, its underlying mechanism is not well understood. Uveal melanoma (UM), which is featured with single organ liver metastasis, may provide a simplified model for realizing the complicated colonization process. Read More

View Article and Full-Text PDF

[The Significance of Surgical Biopsy in Case of the Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for the Treatment of Postoperative Recurrence of Lung Cancer].

Kyobu Geka 2021 Feb;74(2):87-91

Department of Thoracic Surgery, Iwate Prefectural Isawa Hospital, Oshu, Japan.

To evaluate the clinical features of patients who developed resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) administered for postoperative recurrence of lung cancer, we assessed eight patients who underwent surgical biopsy or sampling for the detection of T790M mutation under general anesthesia from 2017 to 2019 in our hospital. All 8 patients had undergone lobectomy with nodal dissection for lung cancer of pathological stageⅠB/Ⅲ/Ⅳa (4/3/1 patients). The median disease-free survival was 29 months (range:11~110 months). Read More

View Article and Full-Text PDF
February 2021

A key requirement for synaptic Reelin signaling in ketamine-mediated behavioral and synaptic action.

Proc Natl Acad Sci U S A 2021 May;118(20)

Department of Pharmacology, Vanderbilt University, Nashville, TN 37240-7933;

Ketamine is a noncompetitive -methyl-D-aspartate (NMDA) receptor antagonist that produces rapid antidepressant action in some patients with treatment-resistant depression. However, recent data suggest that ∼50% of patients with treatment-resistant depression do not respond to ketamine. The factors that contribute to the nonresponsiveness to ketamine's antidepressant action remain unclear. Read More

View Article and Full-Text PDF

Identifying potential drug targets and candidate drugs for COVID-19: biological networks and structural modeling approaches.

F1000Res 2021 18;10:127. Epub 2021 Feb 18.

Centre of Interdisciplinary Science-Computational Life Sciences, College of Chemistry and Chemical Engineering,, Henan University of Technology, Zhengzhou, Henan, 450001, China.

Coronavirus (CoV) is an emerging human pathogen causing severe acute respiratory syndrome (SARS) around the world. Earlier identification of biomarkers for SARS can facilitate detection and reduce the mortality rate of the disease. Thus, by integrated network analysis and structural modeling approach, we aimed to explore the potential drug targets and the candidate drugs for coronavirus medicated SARS. Read More

View Article and Full-Text PDF
February 2021

A network analysis of angiogenesis/osteogenesis-related growth factors in bone tissue engineering based on in-vitro and in-vivo data: A systems biology approach.

Tissue Cell 2021 May 1;72:101553. Epub 2021 May 1.

Department of Tissue Engineering and Applied Cell Sciences, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Iran; Regenerative Medicine Group (REMED), Universal Scientific Education and Research Network (USERN), Tehran, Iran. Electronic address:

The principal purpose of tissue engineering is to stimulate the injured or unhealthy tissues to revive their primary function through the simultaneous use of chemical agents, cells, and biocompatible materials. Still, choosing the appropriate protein as a growth factor (GF) for tissue engineering is vital to fabricate artificial tissues and accelerate the regeneration procedure. In this study, the angiogenesis and osteogenesis-related proteins' interactions are studied using their related network. Read More

View Article and Full-Text PDF

An updated review of the treatment landscape for advanced gastrointestinal stromal tumors.

Cancer 2021 May 11. Epub 2021 May 11.

Oncology and Palliative Care, Sarcoma Center, Helios Klinikum Berlin-Buch, Berlin, Germany.

Before the introduction of tyrosine kinase inhibitors (TKIs), the overall survival of patients with advanced or metastatic gastrointestinal stromal tumors (GISTs) was 10 to 20 months because of the lack of approved therapies. In the last 20 years, a treatment algorithm for patients with advanced GISTs, which includes imatinib, sunitinib, and regorafenib as first-, second-, and third-line therapies, respectively, has been established. Recently, 2 new TKIs have been approved: ripretinib for fourth-line therapy and avapritinib as first-line therapy in patients harboring platelet-derived growth factor receptor α (PDGFRA) exon 18 D842V mutations. Read More

View Article and Full-Text PDF

Mushrooms are potential foods against cancer: identified by molecular docking and molecular dynamics simulation.

Nat Prod Res 2021 May 11:1-6. Epub 2021 May 11.

BCDA College of Pharmacy & Technology, Jessore Road South, Hridaypur, Kolkata, West Bengal, India.

Epidermal Growth Factor Receptor (EGFR) is a promising drug target for the discovery of cancer chemotherapeutics. EGFR tyrosine kinase inhibitors become resistant due to mutation after a certain period of clinical application. The objective of the present study is to identify edible mushrooms as EGFR inhibitors. Read More

View Article and Full-Text PDF

GlcNAc is a mast-cell chromatin-remodeling oncometabolite that promotes systemic mastocytosis aggressiveness.

Blood 2021 May 11. Epub 2021 May 11.

Centre de Recherche en Cancérologie de Marseille - Inserm U1068, CNRS UMR7258, Aix-Marseille Université, Institut Paoli-Calmettes, Marseille, France.

Systemic mastocytosis (SM) is a KIT-driven hematopoietic neoplasm characterized by the excessive accumulation of neoplastic mast cells (MCs) in various organs and, mainly, the bone marrow (BM). Multiple genetic and epigenetic mechanisms contribute to the onset and severity of SM. However, little is known to date about the metabolic underpinnings underlying SM aggressiveness, which has thus far impeded the development of strategies to leverage metabolic dependencies when existing KIT-targeted treatments fail. Read More

View Article and Full-Text PDF

Orthotopic model of lung cancer: isolation of bone micro-metastases after tumor escape from Osimertinib treatment.

BMC Cancer 2021 May 10;21(1):530. Epub 2021 May 10.

INSERM U1242 COSS, Université Rennes 1, Clcc Eugène Marquis, Rennes, France.

Background: Osimertinib is a third generation tyrosine kinase inhibitor (TKI) that targets the epidermal growth factor receptor (EGFR) in lung cancer. However, although this molecule is not subject to some of the resistance mechanisms observed in response to first generation TKIs, ultimately, patients relapse because of unknown resistance mechanisms. New relevant non-small cell lung cancer (NSCLC) mice models are therefore required to allow the analysis of these resistance mechanisms and to evaluate the efficacy of new therapeutic strategies. Read More

View Article and Full-Text PDF

Food reward depends on TLR4 activation in dopaminergic neurons.

Pharmacol Res 2021 May 7:105659. Epub 2021 May 7.

Guangdong Provincial Key Laboratory of Animal Nutrition Control, Guangzhou, Guangdong 510642, China; National Engineering Research Center for Breeding Swine Industry, College of Animal Science, South China Agricultural University, Guangzhou, Guangdong 510642, China. Electronic address:

The rising prevalence of obesity and being overweight is a worldwide health concern. Food reward dysregulation is the basic factor for the development of obesity. Dopamine (DA) neurons in the ventral tegmental area (VTA) play a vital role in food reward. Read More

View Article and Full-Text PDF

Improving laboratory diagnostics in myasthenia gravis.

Expert Rev Mol Diagn 2021 May 10. Epub 2021 May 10.

Autoimmunity Laboratory, IRCCS Ospedale Policlinico San Martino, Largo Rosanna Benzi, 10, 16132 Genova (GE), Italy.

: Myasthenia gravis (MG) is a prototypical autoimmune disease, characterized by pathogenic autoantibodies targeting structures of the neuromuscular junction. Radioimmunoprecipitation assays (RIPAs) represent the gold standard for their detection. However, new methods are emerging to complement, or overcome RIPAs, also with the perspective of eliminating the use of radioactive reagents. Read More

View Article and Full-Text PDF

Real-World Utilization of EGFR TKIs and Prognostic Factors for Survival in EGFR-Mutated Non-Small Cell Lung Cancer Patients with Brain Metastases.

Int J Cancer 2021 May 10. Epub 2021 May 10.

Department of Medical Oncology, Cancer Hospital of the University of Chinese Academy of Sciences, Zhejiang Cancer Hospital, Institute of Cancer Research and Basic Medical Sciences of Chinese Academy of Sciences, Hangzhou, China.

Brain metastases (BMs) cause morbidity and mortality in patients with non-small cell lung cancer (NSCLC). The optimal management of epidermal growth factor receptor (EGFR)-mutated NSCLC with BM is debatable. We aimed to investigate the impact of different treatments among patients with EGFR-mutated NSCLC. Read More

View Article and Full-Text PDF

Cardiovascular Toxicities of Antiangiogenic Tyrosine Kinase Inhibitors: A Retrospective, Pharmacovigilance Study.

Target Oncol 2021 May 10. Epub 2021 May 10.

Leviev Heart Center, Sheba Medical Center, Ramat Gan, Israel.

Background: Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors (TKIs) are an essential therapeutic option in the management of various solid tumors, particularly renal cell carcinoma (RCC). However, post-marketing data regarding their potential cardiovascular toxicities are scant.

Objective: To identify and characterize cardiovascular adverse events (CVAEs) of VEGFR-TKIs indicated for RCC. Read More

View Article and Full-Text PDF

A possible way to prevent the progression of bone lesions in multiple myeloma via Src-homology-region-2-domain-containing-phosphatase-1 activation.

J Cell Biochem 2021 May 10. Epub 2021 May 10.

Department of Molecular Immunology and Inflammation, Research Institute National Center for Global Health and Medicine, Tokyo, Japan.

On the basis of our recent findings, in which multiple receptor-mediated mast cell functions are regulated via a common signaling cascade, we posit that the formation and functioning of osteoclasts are also controlled by a similar common mechanism. These cells are derived from the same granulocyte/monocyte progenitors and share multiple receptors except those that are cell-specific. In both types of cells, all known receptors reside in lipid rafts, form multiprotein complexes with recruited signaling molecules, and are internalized upon receptor engagement. Read More

View Article and Full-Text PDF

Study of EGFR mutations in head and neck squamous cell carcinomas.

Autops Case Rep 2021 Apr 15;11:e2021251. Epub 2021 Apr 15.

INHS ASVINI, Department of Pathology, Colaba, Mumbai, India.

Introduction: Squamous carcinoma is the commonest malignancy of the head and neck region. It is associated with high morbidity and mortality. Epidermal growth factor receptor (EGFR) regulates downstream signaling pathways through its tyrosine kinase (TK) domains that play a role in cell proliferation and survival. Read More

View Article and Full-Text PDF

Case Report: Outcome of Osimertinib Treatment in Lung Adenocarcinoma Patients With Acquired KRAS Mutations.

Front Oncol 2021 22;11:630256. Epub 2021 Apr 22.

Department of Thoracic Oncology, Cancer Center, West China Hospital, Sichuan University, Chengdu, China.

Background: Osimertinib belongs to the third-generation epidermal growth factor receptor tyrosine kinase inhibitor that has shown positive effects in treating lung adenocarcinoma cancer. However, the subsequent resistance to Osimertinib has become a clinical challenge.

Case Presentation: We present two lung adenocarcinoma cases that developed a resistance to Osimertinib. Read More

View Article and Full-Text PDF

Diagnostic Value of Circulating Progranulin and Its Receptor EphA2 in Predicting the Atheroma Burden in Patients with Coronary Artery Disease.

Dis Markers 2021 21;2021:6653501. Epub 2021 Apr 21.

Department of Pharmacy, Zhongshan Hospital, Fudan University, Shanghai, China.

Background: Progranulin (PGRN) and its potential receptor Eph-receptor tyrosine kinase-type A2 (EphA2) are inflammation-related molecules that present on the atherosclerotic plaques. However, the roles of circulating PGRN and EphA2 in coronary artery disease (CAD) remain unclear.

Objective: To study the clinical significance of circulating PGRN and EphA2 levels in Chinese patients undergoing coronary angiography. Read More

View Article and Full-Text PDF

Gallic acid suppresses colon cancer proliferation by inhibiting SRC and EGFR phosphorylation.

Exp Ther Med 2021 Jun 16;21(6):638. Epub 2021 Apr 16.

School of Life Sciences, Yantai University, Yantai, Shandong 264005, P.R. China.

The aim of the present study was to investigate the effects of gallic acid (GA) on the proliferation and apoptosis of colon cancer cells and to further clarify the mechanism of GA function associated with SRC and EGFR phosphorylation. HCT116 and HT29 cells were treated with different concentrations of GA for 24 h. Cell proliferation and apoptosis were analyzed using plate clone formation and flow cytometry assays, respectively. Read More

View Article and Full-Text PDF

Targeting PAR2 Overcomes Gefitinib Resistance in Non-Small-Cell Lung Cancer Cells Through Inhibition of EGFR Transactivation.

Front Pharmacol 2021 22;12:625289. Epub 2021 Apr 22.

School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, China.

Drug resistance can notably restrict clinical applications of gefitinib that is a commonly used EGFR-tyrosine kinase inhibitors (EGFR-TKIs) for non-small cell lung cancer (NSCLC). The attempts in exploring novel drug targets and reversal strategies are still needed, since gefitinib resistance has not been fully addressed. Protease-activated receptor 2 (PAR2), a G protein-coupled receptor, possesses a transactivation with EGFR to initiate a variety of intracellular signal transductions, but there is a lack of investigations on the role of PAR2 in gefitinib resistance. Read More

View Article and Full-Text PDF