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IGF-1R

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https://www.readbyqxmd.com/read/28109944/synthesis-biological-evaluation-and-molecular-dynamics-md-simulation-studies-of-three-novel-f-18-labeled-and-focal-adhesion-kinase-fak-targeted-5-bromo-pyrimidines-as-radiotracers-for-tumor
#1
Yu Fang, Dawei Wang, Xingyu Xu, Jianping Liu, Aiqin Wu, Xiang Li, Qianqian Xue, Huan Wang, Hang Wang, Huabei Zhang
Focal adhesion kinase (FAK) is considered as an attractive target for oncology. A series of F-18 labeled 5-bromo-N(2)-(4-(2-fluoro-pegylated (FPEG))-3,5-dimethoxyphenyl)-N(4)-(4-methoxyphenyl)pyrimidine-2,4-diamine derivatives were prepared and evaluated as the FAK targeted radiotracers for the early diagnoses of tumor. For the study of the FAK targeted drug molecules, this was the first attempt to develop the tumor diagnostic imaging agents on the radiopharmaceutical level. They inhibited the activity of FAK with IC50 in the range of 91...
January 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28109147/-co-culture-with-umbilical-cord-mesenchymal-stem-cells-promotes-the-synthesis-and-mechnism-of-milk-protein-in-bovine-mammary-epithelial-cells
#2
Yankun Zhao, Wei Shao, Chenglong Luo, Kaile Wu, Xiong Yu
Objective To explore the possible mechanism of umbilical cord mesenchymal stem cells (UCMSCs) regulating milk protein synthesis in bovine mammary gland epithelial cells (BMECs). Methods UCMSCs and BMECs were co-cultured by double-chamber Transwell(TM), and other BMECs were cultured alone as a control group. Insulin like growth factor 1 receptor (IGF-1R) inhibitor AG1024 was used to treat cells. IGF-1, β casein (CSN2) and κ casein (CSN3) content in the supernatants were determined by ELISA; the relative expression abundance of Janus kinase and signal transducer and activator of transcription factor (JAK/STAT) signaling pathway-related genes were detected by quantitative real-time PCR (qRT-PCR); and after the cells were treated with JAK2 signal blocker AG490, qRT-PCR was performed to test the relative expression abundance of CSN2 and CSN3 mRNAs...
February 2017: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/28104361/igfbp-a-novel-target-of-lung-cancer
#3
REVIEW
QiongGe Hu, Yong Zhou, Kejing Ying, Wenjing Ruan
The insulin-like growth factor-1 receptor(IGF-1R) is a central component of lung cancer signal transduction pathways. A phase III study failed for carboplatin, paclitaxel, with or without figitumumab in first-line treating metastatic non-small cell lung cancer (NSCLC). There is an urgent need for a better understanding of signaling in IGF system. Insulin-like growth factor-binding proteins(IGFBPs) function as modulators for IGF signaling through sequestration of IGFs in serum and the extracellular fluid. IGFBPs can also act as transporters or modulators for IGF action and insulin action...
January 16, 2017: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/28101246/detection-of-microrna-200b-may-predict-the-inhibitory-effect-of-gefitinib-on-non-small-cell-lung-cancer-and-its-potential-mechanism
#4
Zhiwu Liu, Liqiong Yao, Bangyun Tan, Li Li, Baojin Chen
The present study aimed to investigate the association and underlying mechanisms between microRNA-200b level and the inhibitory effect of gefitinib on non-small cell lung cancer. In total, 100 patients (43 males and 57 females; median age, 63 years) with advanced non-small cell lung cancer (NSCLC) were selected. All patients were administered with gefitinib orally (250 mg/day) and the effect of gefitinib was evaluated according to the Response Evaluation Criteria in Solid Tumors guidelines. Tumor tissue and plasma samples were collected prior to and subsequent to therapy...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28097905/discovery-of-novel-dual-inhibitors-of-receptor-tyrosine-kinases-egfr-and-igf-1r
#5
Cornelius Hempel, Frank Totzke, Christoph Schächtele, Abdulkarim Najjar, Wolfgang Sippl, Christoph Ritter, Andreas Hilgeroth
Novel 4-benzylamino benzo-anellated pyrrolo[2,3-b]pyridines have been synthesized with varied substitution patterns both at the molecular scaffold of the benzo-anellated ring and at the 4-benzylamino residue. With a structural similarity to substituted thieno[2,3-d]pyrimidines as epidermal growth factor receptor (EGFR) inhibitors, we characterized the inhibition of EGFR for our novel compounds. As receptor heterodimerization gained certain interest as mechanism of cancer cells to become resistant against novel protein kinase inhibitors, we additionally measured the inhibition of insulin-like growth factor receptor IGF-1R which is a prominent receptor for such heterodimerizations with EGFR...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097474/igf-1r-regulates-the-extracellular-level-of-active-mmp-2-pathological-neovascularization-and-functionality-in-retinas-of-oir-mouse-model
#6
Valeria E Lorenc, Paula V Subirada Caldarone, María C Paz, Darío G Ferrer, José D Luna, Gustavo A Chiabrando, María C Sánchez
In ischemic proliferative diseases such as retinopathies, persistent hypoxia leads to the release of numerous neovascular factors that participate in the formation of abnormal vessels and eventually cause blindness. The upregulation and activation of metalloproteinases (MMP-2 and MMP-9) represent a final common pathway in this process. Although many regulators of the neovascular process have been identified, the complete role of the insulin-like growth factor 1 (IGF-1) and its receptor (IGF-1R) appears to be significantly more complex...
January 17, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28096479/igf-1-receptor-modulates-foxo1-mediated-tamoxifen-response-in-breast-cancer-cells
#7
Ali Vaziri-Gohar, Yan Zheng, Kevin D Houston
: Tamoxifen is a common adjuvant treatment for ERalpha-positive breast cancer patients, however acquired resistance abrogates the efficacy of this therapeutic approach. We recently demonstrated that G protein-coupled estrogen receptor 1 (GPER1) mediates tamoxifen action in breast cancer cells by inducing insulin-like growth factor binding protein-1 (IGFBP-1) to inhibit IGF-1-dependent signaling. To determine if dysregulation of IGFBP-1 induction is associated with tamoxifen resistance, IGFBP-1 transcription was measured in tamoxifen-resistant MCF-7 cells (TamR) after tamoxifen (Tam) treatment...
January 17, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28093198/mild-hypothermia-pretreatment-protects-hepatocytes-against-ischemia-reperfusion-injury-via-down-regulating-mir-122-and-igf-1r-akt-pathway
#8
Qi Xiao, Qi-Fa Ye, Wei Wang, Bi-Qi Fu, Zhi-Ping Xia, Zhong-Zhong Liu, Xing-Jian Zhang, Yan-Feng Wang
BACKGROUND: Mild hypothermia has been well known as an effective way to reduce ischemia reperfusion injury (IRI), while the mechanisms are still unclear. More and more evidences have indicated that miRNAs should been involved in the regulation of IRI and expecially some miRNAs have shown temp-responsiveness for temperature variation. Therefore, the role of miR-122 in mild hypothermia pretreatment after IRI was investigated. METHODS: We established a LO2 cell anoxia-reoxygenation injury model to simulate liver IRI...
January 13, 2017: Cryobiology
https://www.readbyqxmd.com/read/28092675/unbalancing-p53-mdm2-igf-1r-axis-by-mdm2-activation-restrains-the-igf-1-dependent-invasive-phenotype-of-skin-melanoma
#9
C Worrall, N Suleymanova, C Crudden, I Trocoli Drakensjö, E Candrea, D Nedelcu, S-I Takahashi, L Girnita, A Girnita
Melanoma tumors usually retain wild-type p53; however, its tumor-suppressor activity is functionally disabled, most commonly through an inactivating interaction with mouse double-minute 2 homolog (Mdm2), indicating p53 release from this complex as a potential therapeutic approach. P53 and the tumor-promoter insulin-like growth factor type 1 receptor (IGF-1R) compete as substrates for the E3 ubiquitin ligase Mdm2, making their relative abundance intricately linked. Hence we investigated the effects of pharmacological Mdm2 release from the Mdm2/p53 complex on the expression and function of the IGF-1R...
January 16, 2017: Oncogene
https://www.readbyqxmd.com/read/28088554/mir-99a-suppresses-proliferation-migration-invasion-and-induces-g1-phase-cell-cycle-arrest-via-targeting-igf-1r-pathway-in-renal-cell-carcinoma-786-0-and-os-rc-2-cells
#10
Bo Hao, Li Cui, Yi Gu, Bo Zhang, Min Wang, Hua Zhou, Renfang Xu, XiaoZhou He
OBJECTIVE: To explore the potential mechanism of microRNA-99a (miR-99a) and IGF-1R (insulin-like growth factor 1 receptor) accounting for RCC. MATERIALS AND METHODS: The RCC 786-O and OS-RC-2 cells were transfected with miR-99a mimics or small interfering RNA (siRNA) that silence the IGF-1R (IGF-1R-siRNA) to upregulate the expression of miR-99a and to downregulate the expression of IGF-1R. Real-time PCR and western-blot were used to detect the expression of proteins...
January 11, 2017: Urology
https://www.readbyqxmd.com/read/28063218/cyclic-glycine-proline-accelerates-mammary-involution-by-promoting-apoptosis-and-inhibiting-igf-1-function
#11
Gagandeep Singh-Mallah, Christopher D McMahon, Jian Guan, Kuljeet Singh
In rodents, post-lactational involution of mammary glands is characterized by the loss of mammary epithelial cells via apoptosis, which is associated with a decline in the expression of insulin-like growth factor-1 (IGF-1). Overexpression of IGF-1 delays involution by inhibiting apoptosis of epithelial cells and preserving the remaining secretory alveoli. Cyclic-glycine-proline (cGP), a metabolite of IGF-1, normalizes IGF-1 function under pathological conditions by regulating the bioavailability of IGF-1. The present study investigated the effect of cGP on the physiological decline in IGF-1 function during post-lactational mammary involution...
January 7, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28046018/co-targeting-igf-1r-and-autophagy-enhances-the-effects-of-cell-growth-suppression-and-apoptosis-induced-by-the-igf-1r-inhibitor-nvp-aew541-in-triple-negative-breast-cancer-cells
#12
Weibin Wu, Jieyi Ma, Nan Shao, Yawei Shi, Ruiming Liu, Wen Li, Yin Lin, Shenming Wang
BACKGROUND: Triple-negative breast cancer (TNBC) is the most intractable type of breast cancer, and there is a lack of effective targeted therapy. Insulin-like growth factor-1 receptor (IGF-1R) is reportedly a potential target for TNBC treatment. However, satisfying treatment outcomes in breast cancer patients have yet to be achieved with IGF-1R-targeted agents. METHODS: To confirm whether inhibiting IGF-1R could induce autophagy, we detected autophagy-related proteins by western blotting and immunofluorescence staining of LC3-II...
2017: PloS One
https://www.readbyqxmd.com/read/28034783/cerebellar-insulin-igf-1-signaling-in-diabetic-rats-effects-of-exercise-training
#13
Mariana Eiras Borges, Alessandra Mussi Ribeiro, José Rodrigo Pauli, Luciana Mendonça Arantes, Eliete Luciano, Leandro Pereira de Moura, José Alexandre Curiacos de Almeida Leme, Alessandra Medeiros, Natália Oliveira Bertolini, Clarice Yoshiko Sibuya, Ricardo José Gomes
The Diabetes Mellitus (DM) is a chronic disease associated with loss of brain regions such as the cerebellum, increasing the risk of developing neurodegenerative diseases such as Parkinson's disease (PD). In the brain of diabetic and PD organisms the insulin/IGF-1 signaling is altered. Exercise training is an effective intervention for the prevention of neurodegerative diseases since it release neurotrophic factors and regulating insulin/IGF-1 signaling in the brain. This study aimed to evaluate the proteins involved in the insulin/IGF-1 pathway in the cerebellum of diabetic rats subjected to exercise training protocol...
December 26, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27987211/inhibiting-thyrotropin-insulin-like-growth-factor-1-receptor-crosstalk-to-treat-graves-ophthalmopathy-studies-in-orbital-fibroblasts-in-vitro
#14
Robert F Place, Christine C Krieger, Susanne Neumann, Marvin C Gershengorn
BACKGROUND AND PURPOSE: Crosstalk between the thyrotropin (TSH) receptor (TSHR) and the insulin-like growth factor 1 receptor (IGF-1R) initiated by activation of TSHR may play a prominent role in the development of Graves' ophthalmopathy (GO). Specifically, we have shown that TSHR activation alone is sufficient to stimulate hyaluronan (HA) secretion, a major component of GO, through both IGF-1R-dependent and -independent pathways. Although an anti-IGF-1R antibody is in clinical trial, its effectiveness hinges on the relative importance of IGF-1R versus TSHR signaling in GO pathogenesis...
December 17, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27979966/insulin-like-growth-factor-1-receptor-signaling-is-required-for-optimal-atr-chk1-kinase-signaling-in-uvb-irradiated-human-keratinocytes
#15
Michael G Kemp, Dan F Spandau, Richard Simman, Jeffrey B Travers
Ultraviolet B (UVB) wavelengths of light induce the formation of photoproducts in DNA that are potentially mutagenic if not properly removed by the nucleotide excision repair machinery. As an additional mechanism to minimize the risk of mutagenesis, UVB-irradiated cells also activate a checkpoint signaling cascade mediated by the ATR (ataxia telangiectasia-mutated and rad3-related) and CHK1 (checkpoint kinase 1) kinases to transiently suppress DNA synthesis and cell cycle progression. Given that keratinocytes in geriatric skin display reduced activation of the insulin-like growth factor-1 receptor (IGF-1) and alterations in DNA repair rate, apoptosis, and senescence following UVB exposure, here we used cultured human keratinocytes in vitro and skin explants ex vivo to examine how IGF-1R activation status affects ATR-CHK1 kinase signaling and the inhibition of DNA replication following UVB irradiation...
December 15, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27951515/polyphenolics-from-mango-mangifera-indica-l-suppress-breast-cancer-ductal-carcinoma-in-situ-proliferation-through-activation-of-ampk-pathway-and-suppression-of-mtor-in-athymic-nude-mice
#16
Matthew J Nemec, Hyemee Kim, Alexandria B Marciante, Ryan C Barnes, Erik D Hendrick, William H Bisson, Stephen T Talcott, Susanne U Mertens-Talcott
The objective of this study was to assess the underlying mechanisms of mango polyphenol decreased cell proliferation and tumor volume in ductal carcinoma in situ breast cancer. We hypothesized that mango polyphenols suppress signaling along the AKT/mTOR axis while up-regulating AMPK. To test this hypothesis, mango polyphenols (0.8 mg gallic acid equivalents per day) and pyrogallol (0.2 mg/day) were administered for 4 weeks to mice xenografted with MCF10DCIS.com cells subcutaneously (n=10 per group). Tumor volumes were significantly decreased, both mango and pyrogallol groups displayed greater than 50% decreased volume compared to control...
November 15, 2016: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/27928806/-molecular-mechanism-of-gastrointestinal-stromal-tumors-and-progress-in-drug-research
#17
Jian Li
The functional mutation of c-kit and platelet-derived growth factor receptor α (PDGFRA) which encode proto-oncogene receptor tyrosine kinase are the crucial pathogeneses of gastrointestinal stromal tumors(GISTs). 80%-85% c-kit gene mutation including exon 11,exon 9,exon 13,exon 17 and 5%-10% PDGFRA gene mutation such as exon 18, exon 12 are examined in GISTs. Neither of c-kit or PDGFRA gene mutation are called wide type GISTs. The pathogeneses of wild type GISTs are not clear. The deficiency of succinate dehydrogenase B(SDHB)-related insulin-like growth factor 1(IGF-1R) activation, BRAF gene mutation and neurofibromatosis type 1 may be related to progression of wild type GISTs...
November 25, 2016: Zhonghua Wei Chang Wai Ke za Zhi, Chinese Journal of Gastrointestinal Surgery
https://www.readbyqxmd.com/read/27923328/modeling-stroma-induced-drug-resistance-in-a-tissue-engineered-tumor-model-of-ewing-sarcoma
#18
Marco Santoro, Brian A Menegaz, Salah-Eddine Lamhamedi-Cherradi, Eric R Molina, Danielle Wu, Waldemar Priebe, Joseph A Ludwig, Antonios G Mikos
Three-dimensional (3D) tumor models are gaining traction in the research community given their capacity to mimic aspects of the tumor microenvironment absent in monolayer systems. In particular, the ability to spatiotemporally control cell placement within ex vivo 3D systems has enabled the study of tumor-stroma interactions. Furthermore, by regulating biomechanical stimuli, one can reveal how biophysical cues affect stromal cell phenotype and how their phenotype impacts tumor drug sensitivity. Both tumor architecture and shear force have profound effects on Ewing sarcoma (ES) cell behavior and are known to elicit ligand-mediated activation of the insulin-like growth factor-1 receptor (IGF-1R), thereby mediating resistance of ES cells to IGF-1R inhibitors...
January 2017: Tissue Engineering. Part A
https://www.readbyqxmd.com/read/27903254/mir-96-mir-145-and-mir-9-expression-increases-and-igf-1r-and-foxo1-expression-decreases-in-peripheral-blood-mononuclear-cells-of-aging-humans
#19
Monika Budzinska, Magdalena Owczarz, Eliza Pawlik-Pachucka, Malgorzata Roszkowska-Gancarz, Przemyslaw Slusarczyk, Monika Puzianowska-Kuznicka
BACKGROUND: In mammals, the IGF-1 pathway affects the phenotype of aging. Since the function of the immune system is modulated by IGF-1, it is plausible that immunosenescence might in part result from altered control by this pathway. We therefore examined whether the expression of IGF-1R, FOXO1, and FOXO3a in peripheral blood mononuclear cells (PBMC) changes with age and if this might be due to changes in the expression of select miRNAs. METHODS: The expression of IGF-1R, FOXO1, FOXO3a, as well as of miR-9, miR-96, miR-99a, miR-132, miR-145, and miR-182 was examined in PBMC of young (27...
November 30, 2016: BMC Geriatrics
https://www.readbyqxmd.com/read/27895663/mir-30a-5p-overexpression-may-overcome-egfr-inhibitor-resistance-through-regulating-pi3k-akt-signaling-pathway-in-non-small-cell-lung-cancer-cell-lines
#20
Fei Meng, Fengfeng Wang, Lili Wang, S C Cesar Wong, William C S Cho, Lawrence W C Chan
Lung cancer is one of the most common deadly diseases worldwide, most of which is non-small cell lung cancer (NSCLC). The epidermal growth factor receptor (EGFR) mutant NSCLCs frequently respond to the EGFR tyrosine kinase inhibitors (EGFR-TKIs) treatment, such as Gefitinib and Erlotinib, but the development of acquired resistance limits the utility. Multiple resistance mechanisms have been explored, e.g., the activation of alternative tyrosine kinase receptors (TKRs) sharing similar downstream pathways to EGFR...
2016: Frontiers in Genetics
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