163,499 results match your criteria factor inhibitor


Geniposide exerts protective effects on spinal cord injury in rats by inhibiting the IKKs/NF-κB signaling pathway.

Int Immunopharmacol 2021 Sep 20;100:108158. Epub 2021 Sep 20.

Department of Medicine, Quzhou College of Technology, Quzhou, 324000, Zhejiang, China.

Background: Spinal cord injury (SCI) is a traumatic condition of the central nervous system , which can cause nerve injury and affect nerve regeneration, thus leading to severe dysfunction of motor and sensory pathways, and unfortunately these effects are irreversible. Inflammatory response constitutes one of the important mechanisms of spinal cord secondary injury. Geniposide (Gen) is reported to possess anti-inflammation and neuronal repair capacities. Read More

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September 2021

Cardio-protective effect of tetrahydrocurcumin, the primary hydrogenated metabolite of curcumin in vivo and in vitro: Induction of apoptosis and autophagy via PI3K/AKT/mTOR pathways.

Eur J Pharmacol 2021 Sep 20:174495. Epub 2021 Sep 20.

The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, PR China; State Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, PR China; Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome, Guangzhou, PR China. Electronic address:

Tetrahydrocurcumin (THC) is an essential metabolite of curcumin, a major active component of the Curcuma species, which have been used traditionally for the treatment of cardiovascular diseases. The PI3K/AKT/mTOR signaling pathways serve a vital role during myocardial ischemia-reperfusion (MI/R) injury. The aim of the present study was to investigate the cardioprotective potential and mechanism of THC. Read More

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September 2021

Working from within: how secretory leukocyte protease inhibitor regulates the expression of pro-inflammatory genes.

Biochem Cell Biol 2021 Sep 23. Epub 2021 Sep 23.

University of Manitoba, 8664, Department of Human Anatomy and Cell Science, Winnipeg, Manitoba, Canada;

Secretory leukocyte protease inhibitor (SLPI) is a small but powerful member of the serine protease inhibitor family, which includes proteins such as elafin and alpha1 anti-trypsin. These proteins all have similar structure and antiprotease abilities, but SLPI has been found to have an additional role as an anti-inflammatory factor. It can inhibit the production of pro-inflammatory cytokines in cells stimulated with lipopolysaccharide, prevent neutrophil infiltration in murine models of lung and liver injury, and regulate the activity of the transcription factor NF-κB. Read More

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September 2021

LncRNA ITSN1-2 knockdown inhibits OGD/R-induced inflammation and apoptosis in mouse hippocampal neurons via sponging miR-195-5p.

Neuroreport 2021 Sep 21. Epub 2021 Sep 21.

Department of Neurology Recovery Unit Department of Stomatology, PingXiang People's Hospital, Pingxiang, China.

Objective: The upregulation of long noncoding RNA intersectin 1-2 (lnc ITSN1-2) is associated with poor prognosis in acute ischemic stroke (AIS) patients, but the role and mechanism of lnc ITSN1-2 in AIS are rarely reported, which, thus, are highlighted in this study.

Methods: AIS cell model was constructed by oxygen glucose deprivation and reoxygenation (OGD/R). The quantitative real-time PCR was used to detect the expression of lnc ITSN1-2 in HT22 cells. Read More

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September 2021

Knockdown of circ_0004104 Alleviates Oxidized Low-Density Lipoprotein-Induced Vascular Endothelial Cell Injury by Regulating miR-100/TNFAIP8 Axis.

J Cardiovasc Pharmacol 2021 Aug;78(2):269-279

Department of Thoracic Surgery, General Hospital of Ningxia Medical University, Yinchuan, Ningxia, China.

Abstract: Coronary artery disease (CAD) is a common cardiovascular disease, mainly due to vascular endothelial cell (VEC) injury caused by atherosclerosis. Circular RNA has been shown to be involved in the regulation of various diseases. However, the role and mechanism of circ_0004104 in CAD are still unclear. Read More

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Long Noncoding RNA MALAT1 Regulates the Progression of Atherosclerosis by miR-330-5p/NF-κB Signal Pathway.

J Cardiovasc Pharmacol 2021 Aug;78(2):235-246

Department of Neurology, MinDong Hospital of Ningde City, Fuan City, Fujian Province, China.

Abstract: Long non-coding RNA metastasis-associated lung adenocarcinoma transcript 1 (MALAT1) was reported to be related to atherosclerosis (AS) progression. However, the underlying mechanism of MALAT1 in AS remains unknown. Quantitative real-time polymerase chain reaction was performed to detect the expression of MALAT1 and miR-330-5p. Read More

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gga-miR-142-3p negatively regulates Mycoplasma gallisepticum (HS strain)-induced inflammatory cytokine production via the NF-κB and MAPK signaling by targeting TAB2.

Inflamm Res 2021 Sep 23. Epub 2021 Sep 23.

Key Laboratory of Agricultural Animal Genetics, Breeding and Reproduction Ministry of Education, College of Animal Science and Technology and College of Veterinary Medicine, Huazhong Agricultural University, Wuhan, 430070, China.

Objective: Mycoplasma gallisepticum (MG), a notorious avian pathogen, leads to considerable economic losses in the poultry industry. MG infection is characterized by severe, uncontrollable inflammation and host DNA damage. Micro ribonucleic acids (miRNAs) have emerged as important regulators in microbial pathogenesis. Read More

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September 2021

Contribution of high fat diet induced PCSK9 upregulation to a mouse model of PCOS is mediated partly by SREBP2.

Reproduction 2021 Sep 1. Epub 2021 Sep 1.

L Yue, Department of physiology, Sichuan University, Chengdu, China.

The incidence of PCOS due to highfat diet (HFD) consumption has been increasing significantly. However, the mechanism by which an HFD contributes to the pathogenesis of PCOS has not been elucidated. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key protein that regulates cholesterol metabolism. Read More

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September 2021

Gabapentin Reduces Alcohol Intake in Rats by Regulating NF-κB Signaling Pathway Via PPAR γ.

Alcohol Alcohol 2021 Sep 22. Epub 2021 Sep 22.

Rehabilitation Department, Qingdao Mental Health Center, Shandong 266034, PR China.

Aims: Increasing preclinical and clinical reports have demonstrated the efficacy of gabapentin (GBP) in treating alcohol use disorder (AUD). However, the mechanism of the effects of GBP in AUD is largely unknown. Herein, we sought to investigate the effect of GBP in a rat model of AUD and explore the underlying mechanism. Read More

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September 2021

Systemic delivery of TNF-armed myxoma virus plus immune checkpoint inhibitor eliminates lung metastatic mouse osteosarcoma.

Mol Ther Oncolytics 2021 Sep 6;22:539-554. Epub 2021 Aug 6.

School of Life Sciences, Arizona State University, Tempe, AZ 85281, USA.

Solid cancers that metastasize to the lungs represent a major therapeutic challenge. Current treatment paradigms for lung metastases consist of radiation therapy, chemotherapies, and surgical resection, but there is no single treatment or combination that is effective for all tumor types. To address this, oncolytic myxoma virus (MYXV) engineered to express human tumor necrosis factor (vMyx-hTNF) was tested after systemic administration in an immunocompetent mouse K7M2-Luc lung metastatic osteosarcoma model. Read More

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September 2021

Overexpression of Circular RNA circ_0013587 Reverses Erlotinib Resistance in Pancreatic Cancer Cells Through Regulating the miR-1227/E-Cadherin Pathway.

Front Oncol 2021 6;11:754146. Epub 2021 Sep 6.

Department of Oncology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

Background: Erlotinib, a small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, demonstrated therapeutic efficacy against pancreatic cancer. However, acquired resistance to erlotinib in pancreatic cancer is widely observed, and the exact mechanisms have not been fully explored until now. We examined the role of circular RNA circ_0013587 in the acquired resistance to erlotinib in pancreatic cancer cells and explored the underlying mechanisms. Read More

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September 2021

Selective Histone Deacetylase Inhibitor ACY-241 (Citarinostat) Plus Nivolumab in Advanced Non-Small Cell Lung Cancer: Results From a Phase Ib Study.

Front Oncol 2021 6;11:696512. Epub 2021 Sep 6.

Virginia Cancer Specialists (VCS) Research Institute, Fairfax, VA, United States.

Background: Histone deacetylase (HDAC) overexpression has been documented in various cancers and may be associated with worse outcomes. Data from early-phase studies of advanced non-small cell lung cancer (NSCLC) suggest encouraging antitumor activity with the combination of an HDAC inhibitor and either platinum-based chemotherapy or an EGFR inhibitor; however, toxicity is a limiting factor in the use of pan-HDAC inhibitors. Selective inhibition of HDAC6 may represent a potential therapeutic target and preclinical studies revealed immunomodulatory effects with HDAC6 inhibition, suggesting the potential for combination with immune checkpoint inhibitors. Read More

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September 2021

Ubiquitin-specific protease 7 mediates platelet-derived growth factor-induced pulmonary arterial smooth muscle cells proliferation.

Pulm Circ 2021 Oct-Dec;11(4):20458940211046131. Epub 2021 Sep 16.

Department of Respiratory Medicine, the First Affiliated Hospital of Xi'an Jiao Tong University, Xi'an, People's Republic of China.

Pulmonary arterial hypertension is a devastating pulmonary vascular disease, in which the pathogenesis is complicated and unclear. Pulmonary arterial smooth muscle cells (PASMCs) proliferation is a key pathological feature of pulmonary arterial hypertension. It has been shown that ubiquitin-specific protease 7 (USP7) is involved in cancer cell proliferation via deubiquitinating and stabilizing E3 ubiquitin ligase mouse double minute 2 (MDM2). Read More

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September 2021

Paradoxical Augmentation of Experimental Spondyloarthritis by RORC Inhibition in HLA-B27 Transgenic Rats.

Front Immunol 2021 6;12:699987. Epub 2021 Sep 6.

Department of Clinical Immunology and Rheumatology, Amsterdam Rheumatology & Immunology Center (ARC), Amsterdam University Medical Centers (UMC), Location Academic Medical Center, University of Amsterdam, Amsterdam, Netherlands.

Objective: IL-17A plays a major role in the pathogenesis of spondyloarthritis (SpA). Here we assessed the impact of inhibition of RAR related orphan receptor-γ (RORC), the key transcription factor controlling IL-17 production, on experimental SpA in HLA-B27 transgenic (tg) rats.

Methods: Experimental SpA was induced by immunization of HLA-B27 tg rats with heat-inactivated . Read More

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September 2021

Efficacy and Prognosis of First-Line EGFR-Tyrosine Kinase Inhibitor Treatment in Older Adults Including Poor Performance Status Patients with -Mutated Non-Small-Cell Lung Cancer.

Cancer Manag Res 2021 15;13:7187-7201. Epub 2021 Sep 15.

School of Medicine for International Students, College of Medicine, I-Shou University, Kaohsiung, Taiwan.

Introduction: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) are standard first-line treatments for advanced -mutated non-small-cell lung cancer (NSCLC) patients. The efficacy of EGFR-TKIs in older patients including poor Eastern Cooperative Oncology Group (ECOG) performance status (PS) is seldom investigated.

Methods: We enrolled patients 65 years or older with -mutated Stage IIIB-IV NSCLC and evaluated the efficacy and prognosis of first-line EGFR-TKI treatment. Read More

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September 2021

Clinical and Pathologic Complete Response to Gefitinib in a Patient with SqCLC Harboring EGFR p.E746_S752delinsV Mutation.

Onco Targets Ther 2021 15;14:4805-4808. Epub 2021 Sep 15.

Department of Thoracic Surgery, Guangdong Provincial People's Hospital, Guangdong Academy of Medical Sciences, Guangzhou, 510080, People's Republic of China.

Development of targeted therapies for squamous cell lung cancer (SqCLC) is currently limited by the prevalence of activating mutations and their predicting power of treatment efficacy. In the present study, we describe a case of treatment-naïve stage IIIB SqCLC that harbored a rare epidermal growth factor receptor (EGFR) p.E746_S752delinsV mutation with clinical complete response to neoadjuvant gefitinib. Read More

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September 2021

LC-MS/MS Estimation of Rociletinib Levels in Human Liver Microsomes: Application to Metabolic Stability Estimation.

Drug Des Devel Ther 2021 15;15:3915-3925. Epub 2021 Sep 15.

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Background: Rociletinib (CO-1686; RLC) is a new, small molecule that is orally administered to inhibit mutant-selective covalent inhibitor of most epidermal growth factor receptor (EGFR)-mutated forms, including T790M, L858R, and exon 19 deletions, but not exon 20 insertions. Non-small-cell lung cancer (NSCLC) with a gene mutation that encodes EGFR is sensitive to approved EGFR inhibitors, but usually resistance develops, which is frequently mediated by T790M EGFR mutation. RLC is an EGFR inhibitor found to be active in preclinical models of EGFR-mutated NSCLC with or without T790M. Read More

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September 2021

Pharmacological inhibition of MyD88 suppresses inflammation in tubular epithelial cells and prevents diabetic nephropathy in experimental mice.

Acta Pharmacol Sin 2021 Sep 22. Epub 2021 Sep 22.

Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, 325035, China.

Emerging evidence shows that chronic inflammation mediated by toll-like receptors (TLRs) contributes to diabetic nephropathy. Myeloid differentiation primary-response protein-88 (MyD88) is an essential adapter protein of all TLRs except TLR3 in innate immunity. It is unclear whether MyD88 could be a therapeutic target for diabetic nephropathy. Read More

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September 2021

GPCR-mediated EGFR transactivation ameliorates skin toxicities induced by afatinib.

Acta Pharmacol Sin 2021 Sep 22. Epub 2021 Sep 22.

School of Biomedical Engineering, Shanghai Jiao Tong University, Shanghai, 200240, China.

Many G-protein-coupled receptor (GPCR) agonists have been studied for transactivating epidermal growth factor receptor (EGFR) signaling through extracellular or intracellular pathways. Accumulated evidence has confirmed that GPCR transactivation participates in various diseases. However, the clinical application of GPCR transactivation has not been explored, and more translational studies are needed to develop therapies to target GPCR-mediated EGFR transactivation. Read More

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September 2021

Targeting the IGF-axis potentiates immunotherapy for pancreatic ductal adenocarcinoma liver metastases by altering the immunosuppressive microenvironment.

Mol Cancer Ther 2021 Sep 22. Epub 2021 Sep 22.

Department of Surgery, Medicine and Oncology, McGill University Health Centre

Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive malignancy, resistant to chemotherapy and associated with high incidence of liver metastases and poor prognosis. Using murine models of aggressive PDAC, we show here that in mice bearing hepatic metastases, treatment with the IGF-Trap, an inhibitor of type 1 insulin like growth factor receptor (IGF-IR) signaling, profoundly altered the local, immunosuppressive tumor microenvironment in the liver, curtailing the recruitment of myeloid derived suppressor cells, reversing innate immune cell polarization and inhibiting metastatic expansion. Significantly, we found that immunotherapy with anti PD-1 antibodies also reduced the growth of experimental PDAC liver metastases, and this effect was enhanced when combined with IGF-Trap treatment, resulting in further potentiation of a T cell response. Read More

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September 2021

miR-186-3p attenuates the tumorigenesis of cervical cancer via targeting insulin-like growth factor 1 to suppress PI3K-Akt signaling pathway.

Bioengineered 2021 Dec;12(1):7079-7092

Department of Radiotherapy, The First Affiliated Hospital of Hebei North University, Zhangjiakou, Hebei, China.

miR-186-3p acts as a tumor suppressor in various cancers. This study aimed to explore the expression levels of miR-186-3p and its role in cervical cancer. We analyzed the effects of miR-186-3p and insulin-like growth factor 1 (IGF1) on the proliferation, invasion, and apoptosis of cervical cancer cells in vitro by regulating the PI3K/Akt signaling pathway. Read More

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December 2021

Liraglutide reduces plasma PCSK9 in patients with type 2 diabetes not treated with statins.

Diabetes Metab 2021 Sep 19:101284. Epub 2021 Sep 19.

University of Burgundy, INSERM LNC UMR1231, Dijon, France; CHU Dijon, Department of Biochemistry, Dijon, France.

Aim: Dyslipidaemia in type 2 diabetes mellitus (T2DM), which increases cardiovascular risk, includes abnormal metabolism of low-density lipoproteins (LDL). Our group has recently shown that liraglutide increases LDL catabolism in patients with T2DM and that it reduces the expression of PCSK9 (a major inhibitor of LDL-receptor expression) in vitro and in mice. This prompted us to study the effect of liraglutide on plasma PCSK9 level in patients with T2DM. Read More

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September 2021

Application of Topical Lidocaine for Pain Relief in the Setting of Targeted Therapy-Induced Onycholysis: A Case Report.

J Palliat Med 2021 Sep 22. Epub 2021 Sep 22.

Department of Pharmacy, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, USA.

Selective pan fibroblast growth factor receptor (FGFR) inhibitors have been linked to severe onycholysis, the uncomfortable separation of the nail plate from the nail bed. Recommendations to assist with FGFR inhibitor onycholysis vary based on the severity. We hypothesized that the application of topical lidocaine to mimic a digital nerve block would be beneficial in addition to traditional supportive care interventions and subsequently report its immediate and continued efficacy for targeted therapy-induced onycholysis. Read More

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September 2021

Inhibition of NFAT suppresses foam cell formation and the development of diet-induced atherosclerosis.

FASEB J 2021 Oct;35(10):e21951

Department of Cardiology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

Deciphering the molecular and cellular processes involved in foam cell formation is critical for us to understand the pathogenesis of atherosclerosis. Nuclear factor of activated T cells (NFAT) is a transcription factor originally identified as a key player in the differentiation of T cells and maturation of immune system. Nowadays it has been brought into attention that NFAT also regulates multiple pathophysiological processes and targeted intervention in NFAT may be effective in the treatment of some cardiovascular diseases. Read More

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October 2021

Tumor Necrosis Factor-alpha utilizes MAPK/NFκB pathways to induce cholesterol-25 hydroxylase for amplifying pro-inflammatory response via 25-hydroxycholesterol-integrin-FAK pathway.

PLoS One 2021 22;16(9):e0257576. Epub 2021 Sep 22.

Department of Veterinary Microbiology and Pathology, College of Veterinary Medicine, Washington State University, Pullman, Washington, United States of America.

Exaggerated inflammatory response results in pathogenesis of various inflammatory diseases. Tumor Necrosis Factor-alpha (TNF) is a multi-functional pro-inflammatory cytokine regulating a wide spectrum of physiological, biological, and cellular processes. TNF induces Focal Adhesion Kinase (FAK) for various activities including induction of pro-inflammatory response. Read More

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September 2021

Drug combination screening as a translational approach toward an improved drug therapy for chordoma.

Cell Oncol (Dordr) 2021 Sep 22. Epub 2021 Sep 22.

Center for Medical Research, Medical University of Graz, Graz, Austria.

Purpose: Drug screening programmes have revealed epidermal growth factor receptor inhibitors (EGFRs) as promising therapeutics for chordoma, an orphan malignant bone tumour, in the absence of a known genetic driver. Concurrently, the irreversible EGFR afatinib (Giotrif®) is being evaluated in a multicentric Phase II trial. As tyrosine kinase inhibitor (TKI) monotherapies are invariably followed by resistance, we aimed to evaluate potential therapeutic combinations with EGFRs. Read More

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September 2021

EGFR-mediated epidermal stem cell motility drives skin regeneration through COL17A1 proteolysis.

J Cell Biol 2021 Nov 22;220(11). Epub 2021 Sep 22.

Department of Stem Cell Biology, Medical Research Institute, Tokyo Medical and Dental University, Tokyo, Japan.

Skin regenerative capacity declines with age, but the underlying mechanisms are largely unknown. Here we demonstrate a functional link between epidermal growth factor receptor (EGFR) signaling and type XVII collagen (COL17A1) proteolysis on age-associated alteration of keratinocyte stem cell dynamics in skin regeneration. Live-imaging and computer simulation experiments predicted that human keratinocyte stem cell motility is coupled with self-renewal and epidermal regeneration. Read More

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November 2021

Risk of cancer after initiation of targeted therapies in patients with rheumatoid arthritis and a prior cancer: systematic review with meta-analysis.

Arthritis Care Res (Hoboken) 2021 Sep 21. Epub 2021 Sep 21.

Department of Rheumatology, Montpellier University Hospital, University of Montpellier-Nimes, Montpellier, France.

Objective: To determine the risk of recurrent or a new malignancy with exposure to targeted disease-modifying anti-rheumatic drugs (DMARDs) in adults with rheumatoid arthritis (RA), axial spondyloarthritis (AS), or psoriatic arthritis (PsA) and a history of cancer.

Methods: We performed a systematic search of the literature for articles published up to June 2019 that investigated adults with RA, AS or PsA who had a history of cancer and received biologic or targeted synthetic DMARDs (bDMARDs or tsDMARDs. We compared the risk of relapse or occurrence of new cancer between patients with and without bDMARDs. Read More

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September 2021

Predictive factors of survival outcomes in first-line therapy for metastatic castration-resistant prostate cancer.

Int J Urol 2021 Sep 22. Epub 2021 Sep 22.

Department of Urology, Graduate School of Medical Sciences, Kyushu University, Japan.

Objectives: To investigate predictive factors of survival of metastatic castration-resistant prostate cancer patients undergoing first-line treatment with androgen receptor pathway inhibitors or docetaxel.

Methods: Japanese patients with metastatic castration-resistant prostate cancer treated with androgen receptor pathway inhibitor or docetaxel between 2008 and 2018 were included. The differential impact of various clinicopathological factors on the outcome, including progression-free survival and overall survival, was compared between treatment with androgen receptor pathway inhibitor and docetaxel. Read More

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September 2021

[Bax inhibitor-1 inhibits calcification of vascular smooth muscle cells ].

Nan Fang Yi Ke Da Xue Xue Bao 2021 Aug;41(8):1177-1182

Department of Cardiology, First Medical Center, General Hospital of PLA, Beijing 100853, China.

Objective: To investigate the effect of Bax inhibitor-1(BI-1)on calcification of vascular smooth muscle cells(VSMCs).

Methods: VSMCs were isolated from the thoracic aorta of SD rats.VSMCs or BI-1-overexpressing VSMCs(transfected with a BI-1-overexpressing plasmid) were cultured in normal medium or calcified medium containing β-glycerophosphate and calcium chloride, and the cell calcification was examined with Alizarin red staining. Read More

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