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https://www.readbyqxmd.com/read/29758406/molecular-dynamics-guided-development-of-indole-based-dual-inhibitors-of-egfr-t790m-and-c-met
#1
Pankaj Kumar Singh, Om Silakari
Secondary acquired mutation in EGFR, i.e. EGFR T790M and amplification of c-MET form the two key components of resistant NSCLC. Thus, previously published pharmacophore models of EGFR T790M and c-MET were utilized to screen an in-house database. On the basis of fitness score, indole-pyrimidine scaffold was selected for further evaluation. Derivatives of indole-pyrimidine scaffold with variedly substituted aryl substitutions were sketched and then docked in both the targets. These docked complexes were then subjected to molecular dynamic simulations, to study the stability of the complexes and evaluate orientations of the designed molecules in the catalytic domain of the selected kinases...
April 25, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29695634/tumor-independent-host-secretomes-induced-by-angiogenesis-and-immune-checkpoint-inhibitors
#2
Michalis Mastri, Christina R Lee, Amanda Tracz, Robert S Kerbel, Melissa Dolan, Yuhao Shi, John M L Ebos
The levels of various circulating blood proteins can change in response to cancer therapy. Monitoring therapy-induced secretomes (TIS) may have use as biomarkers for establishing optimal biological effect (such as dosing) or identifying sources of toxicity and drug resistance. While TIS can derive from tumor cells directly, non-tumor 'host' treatment responses can also impact systemic secretory programs. For targeted inhibitors of the tumor microenvironment, including antiangiogenic and immune-checkpoint therapies, host TIS could explain unexpected collateral 'side-effects' of treatment...
April 25, 2018: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/29675102/synergistic-antitumor-effects-of-cmet-inhibitor-in-combination-with-anti-vegf-in-colorectal-cancer-patient-derived-xenograft-models
#3
Xiangheng Chen, Zhonghai Guan, Jun Lu, Haohao Wang, Zhongkun Zuo, Fei Ye, Jiangsheng Huang, Lisong Teng
cMet signaling pathway is involved in the resistance to anti-VEGF therapy and cMet overexpression is associated with tumor progression and poor prognosis. In this study, the expression of cMet in 146 Chinese colorectal cancer (CRC) patients was examined by immunohistochemistry staining. Our data demonstrated that cMet overexpression rate was 42.5% (62/146) and cMet overexpression was closely correlated with distant metastasis of CRC. Using CRC patient-derived xenograft (PDX) mouse models we investigated antitumor activity of a novel selective cMet inhibitor volitinib alone or in combination with anti-VEGF inhibitor apatinib in vivo ...
2018: Journal of Cancer
https://www.readbyqxmd.com/read/29627496/simvastatin-inhibits-sonic-hedgehog-signaling-and-stemness-features-of-pancreatic-cancer
#4
Yefeng Yin, Li Liu, Zhefu Zhao, Libo Yin, Nathalie Bauer, Clifford C Nwaeburu, Jury Gladkich, Wolfgang Gross, Thilo Hackert, Carsten Sticht, Norbert Gretz, Oliver Strobel, Ingrid Herr
Pancreatic ductal adenocarcinoma (PDA) has poor therapeutic options. Recent patient studies indicate that cholesterol-lowering statins have anti-tumor capacities. We examined several established and primary PDA and normal cell lines as well as PDA patient tissues (n = 68). We found that simvastatin inhibited viability, stemness, tumor growth and metastasis and that it enhanced the efficacy of gemcitabine. These changes were associated with modulation of Shh-related gene expression. Overexpression of Shh prevented the anti-cancer effect of simvastatin, and inhibition of Shh mimicked the simvastatin effect...
April 5, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29616327/whole-exome-sequencing-identifies-key-mutated-genes-in-t790m-wildtype-cmet-unamplified-lung-adenocarcinoma-with-acquired-resistance-to-first-generation-egfr-tyrosine-kinase-inhibitors
#5
Chenguang Li, Hailin Liu, Bin Zhang, Liqun Gong, Yanjun Su, Zhenfa Zhang, Changli Wang
PURPOSE: Lung cancer is the leading cause of cancer-related death worldwide. Lung adenocarcinoma harboring EGFR-activating mutations will inevitably acquire resistance to first-generation EGFR tyrosine kinase inhibitors (TKIs). EGFR T790M mutation and cMET amplification are common mechanisms. Further study is needed to explore unknown genomic alterations contributing to drug resistance. METHODS: Tumor and blood samples from 69 stage IIIB-IV NSCLC patients defined as acquired resistance to first-generation EGFR TKIs (gefitinib, erlotinib or ecotinib) were collected...
April 3, 2018: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/29602831/bioengineered-ncrnas-selectively-change-cellular-mirnome-profiles-for-cancer-therapy
#6
Pui Yan Ho, Zhijian Duan, Neelu Batra, Joseph L Jilek, Mei-Juan Tu, Jing-Xin Qiu, Zihua Hu, Theodore Wun, Primo N Lara, Ralph W DeVere White, Hong-Wu Chen, Ai-Ming Yu
Noncoding RNAs (ncRNAs) produced in live cells may better reflect intracellular ncRNAs for research and therapy. Attempts were made to produce biological ncRNAs, but at low yield or success rate. Here we first report a new ncRNA bioengineering technology, using more stable ncRNA carrier (nCAR) containing a pre-miR-34a derivative identified by rational design and experimental validation. This approach offered a remarkable higher-level expression (40-80% of total RNAs) of recombinant ncRNAs in bacteria, and gave an 80% success rate (33 out of 42 ncRNAs)...
March 30, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29568363/targeting-angiogenesis-in-multiple-myeloma-by-the-vegf-and-hgf-blocking-darpin-%C3%A2-protein-mp0250-a-preclinical-study
#7
Luigia Rao, Kim De Veirman, Donato Giannico, Ilaria Saltarella, Vanessa Desantis, Maria Antonia Frassanito, Antonio Giovanni Solimando, Domenico Ribatti, Marcella Prete, Andreas Harstrick, Ulrike Fiedler, Hendrik De Raeve, Vito Racanelli, Karin Vanderkerken, Angelo Vacca
The investigational drug MP0250 is a multi-specific DARPin® molecule that simultaneously binds and neutralizes VEGF and HGF with high specificity and affinity. Here we studied the antiangiogenic effects of the MP0250 in multiple myeloma (MM). In endothelial cells (EC) isolated from bone marrow (BM) of MM patients (MMEC) MP0250 reduces VEGFR2 and cMet phosphorylation and affects their downstream signaling cascades. MP0250 influences the secretory profile of MMEC and inhibits their in vitro angiogenic activities (spontaneous and chemotactic migration, adhesion, spreading and capillarogenesis)...
March 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29561907/pilates-training-improves-5-km-run-performance-by-changing-metabolic-cost-and-muscle-activity-in-trained-runners
#8
Paula Finatto, Edson Soares Da Silva, Alexandre B Okamura, Bruna P Almada, Henrique B Oliveira, Leonardo A Peyré-Tartaruga
PURPOSE: Strength training improves distance running economy and performance. This finding is based predominantly on maximal and explosive strength programmes applied to locomotor muscles, particularly on the lower limbs. It is not certain whether a minimization of metabolic cost (Cmet) and an improvement in running performance is feasible with strength training of the postural and trunk muscles. METHODS: Using kinematic, neuromuscular and metabolic measurements of running at two different speeds before and after a 12-week Pilates training programme, we tested the hypothesis that core training might improve the running Cmet and performance of trained runners...
2018: PloS One
https://www.readbyqxmd.com/read/29532881/vegf-pathway-targeting-drugs-induce-evasive-adaptation-by-activation-of-neuropilin-1-cmet-in-colon-cancer-cells
#9
Chisato Tomida, Naoko Yamagishi, Hikaru Nagano, Takayuki Uchida, Ayako Ohno, Katsuya Hirasaka, Takeshi Nikawa, Shigetada Teshima-Kondo
Anti-angiogenic therapies targeting vascular endothelial growth factor (VEGF) and its receptor (VEGF-R) are important treatments for a number of human malignancies, including colorectal cancers. However, there is increasing evidence that VEGF/VEGF-R inhibitors promote the adaptive and evasive resistance of tumor cells to the therapies. The mechanism by which the cancer cells become resistant remains unclear. One potential mechanism is that VEGF/VEGF-R blockers directly act on tumor cells independently of anti-angiogenic effects...
April 2018: International Journal of Oncology
https://www.readbyqxmd.com/read/29507702/does-molecular-profiling-of-tumors-using-the-caris-molecular-intelligence-platform-improve-outcomes-for-cancer-patients
#10
Philip Carter, Costi Alifrangis, Biancastella Cereser, Pramodh Chandrasinghe, Lisa Del Bel Belluz, Thomas Herzog, Joel Levitan, Nina Moderau, Lee Schwartzberg, Neha Tabassum, Jinrui Wen, Jonathan Krell, Justin Stebbing
We evaluated the effect of tailoring treatments based on predictions informed by tumor molecular profiles across a range of cancers, using data from Caris Life Sciences. These included breast carcinoma, colorectal adenocarcinoma, female genital tract malignancy, lung non-small cell lung cancer, neuroendocrine tumors, ovarian surface epithelial carcinomas, and urinary tract cancers. Molecular profiles using mostly immunohistochemistry (IHC) and DNA sequencing for tumors from 841 patients had been previously used to recommend treatments; some physicians followed the suggestions completely while some did not...
February 6, 2018: Oncotarget
https://www.readbyqxmd.com/read/29492214/genetic-alterations-in-main-candidate-genes-during-melanoma-progression
#11
Maria Cristina Sini, Valentina Doneddu, Panagiotis Paliogiannis, Milena Casula, Maria Colombino, Antonella Manca, Gerardo Botti, Paolo A Ascierto, Amelia Lissia, Antonio Cossu, Giuseppe Palmieri
Cutaneous melanoma is a common and aggressive human skin cancers. Much is actually known about the molecular mechanisms underlying melanoma pathogenesis. The aim of the study was to evaluate any possible correlation between mutations in main growth-controlling genes ( BRAF, NRAS, CDKN2A ) and copy number variations in frequently amplified candidate genes ( MITF, EGFR, CCND1, cMET, and cKIT ) during melanoma initiation and progression. A large series of primary and secondary melanoma tissue samples ( N = 274) from 232 consecutively-collected patients of Italian origin as well as 32 tumor cell lines derived from primary and metastatic melanomas underwent mutation screening and fluorescence in situ hybridization (FISH) analysis...
February 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29485312/deciphering-ppar%C3%AE-activation-in-cardiometabolic-syndrome-studies-by-in-silico-and-in-vivo-experimental-assessment
#12
Rohini Agrawal, Virendra Nath, Harish Kumar, Vipin Kumar
Cardiometabolic syndrome (CMetS) is a consolidation of metabolic disorders characterized by insulin resistance, dyslipidemia and hypertension. Curcumin, a natural bioactive compound, has been shown to possess notable anti-oxidant activity and it has also been included as a super natural herb in the super natural herbs database. Most of the beneficial effects of Curcumin are possibly due to activation of the nuclear receptor, peroxisome proliferator-activated receptor gamma (PPARγ). The present study investigates molecular interactions of curcumin with PPARγ protein through molecular docking and molecular dynamics (MD) simulation studies...
April 2018: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/29475913/expression-and-clinical-significance-of-claudin-7-pdl-1-pten-c-kit-c-met-c-myc-alk-ck5-6-ck17-p53-egfr-ki67-p63-in-triple-negative-breast-cancer-a-single-centre-prospective-observational-study
#13
Chloe Constantinou, Savvas Papadopoulos, Eirini Karyda, Athanasios Alexopoulos, Niki Agnanti, Anna Batistatou, Haris Harisis
BACKGROUND/AIM: To explore the relationship between p53, p63, c-kit, Ki67, cMet, claudin7, CK5/6, CK17, AR, PTEN, EGFR, ALK, PDL-1 and c-MYC expression with the clinicopathological features of triple- negative breast cancer. MATERIALS AND METHODS: Immunohistochemistry was performed in 84 triple-negative breast cancer samples. RESULTS: A statistically significant relationship between tumour grade and claudin-7 (p=0.004) and between protein p53 and positive lymph nodes (p=0...
March 2018: In Vivo
https://www.readbyqxmd.com/read/29464045/pathological-and-functional-significance-of-semaphorin-5a-in-pancreatic-cancer-progression-and-metastasis
#14
Sugandha Saxena, Yuri Hayashi, Lingyun Wu, Mohammad Awaji, Pranita Atri, Michelle L Varney, Abhilasha Purohit, Satyanarayana Rachagani, Surinder K Batra, Rakesh K Singh
Semaphorin-5A (SEMA5A) has differential cell surface expression between normal and cancer cells and represents an attractive target for therapeutic intervention in pancreatic cancer (PC). In this study, we delineated the pathological expression and significance of SEMA5A during PC progression and metastasis. We utilized human tissue microarrays and different PC mouse models (Pdx1-cre; LSL- Kras(G12D) , Pdx1-Cre; LSL-Kras(G12D) ; LSL-p53(R172H) and RIP1-Tag2) to analyze SEMA5A expression during PC progression...
January 19, 2018: Oncotarget
https://www.readbyqxmd.com/read/29440379/targeting-the-cmet-pathway-augments-radiation-response-without-adverse-effect-on-hearing-in-nf2-schwannoma-models
#15
Yingchao Zhao, Pinan Liu, Na Zhang, Jie Chen, Lukas D Landegger, Limeng Wu, Fu Zhao, Yanxia Zhao, Yanling Zhang, Jing Zhang, Takeshi Fujita, Anat Stemmer-Rachamimov, Gino B Ferraro, Hao Liu, Alona Muzikansky, Scott R Plotkin, Konstantina M Stankovic, Rakesh K Jain, Lei Xu
Neurofibromatosis type II (NF2) is a disease that needs new solutions. Vestibular schwannoma (VS) growth causes progressive hearing loss, and the standard treatment, including surgery and radiotherapy, can further damage the nerve. There is an urgent need to identify an adjunct therapy that, by enhancing the efficacy of radiation, can help lower the radiation dose and preserve hearing. The mechanisms underlying deafness in NF2 are still unclear. One of the major limitations in studying tumor-induced hearing loss is the lack of mouse models that allow hearing testing...
February 27, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29416033/supramolecular-aptamer-nano-constructs-for-receptor-mediated-targeting-and-light-triggered-release-of-chemotherapeutics-into-cancer-cells
#16
Deepak K Prusty, Volker Adam, Reza M Zadegan, Stephan Irsen, Michael Famulok
Platforms for targeted drug-delivery must simultaneously exhibit serum stability, efficient directed cell internalization, and triggered drug release. Here, using lipid-mediated self-assembly of aptamers, we combine multiple structural motifs into a single nanoconstruct that targets hepatocyte growth factor receptor (cMet). The nanocarrier consists of lipidated versions of a cMet-binding aptamer and a separate lipidated GC-rich DNA hairpin motif loaded with intercalated doxorubicin. Multiple 2',6'-dimethylazobenzene moieties are incorporated into the doxorubicin-binding motif to trigger the release of the chemotherapeutics by photoisomerization...
February 7, 2018: Nature Communications
https://www.readbyqxmd.com/read/29377771/physical-activity-body-mass-index-and-clustered-metabolic-risk-in-u-s-adolescents-2007-2012-nhanes
#17
Bethany D Williams, Susan B Sisson, Chris A Ardern, Katrina D DuBose, Tammie M Johnson, M Ryan Richardson, James R Churilla
BACKGROUND: While studies to date have shown that children and adolescents who meet the current physical activity (PA) recommendations and maintain a healthy body weight demonstrate significantly lower cardiometabolic risk, there are some studies that suggest that the relationship between PA and metabolic risk may be mediated by adiposity. The aim of the present study was to examine variation in clustered metabolic risk (cMetS) in adolescents classified as not overweight/active (NOA), not overweight/not active (NONA), overweight/active (OA), and overweight/not active (ONA)...
March 2018: Metabolic Syndrome and related Disorders
https://www.readbyqxmd.com/read/29324814/comprehensive-molecular-profiling-of-advanced-metastatic-olfactory-neuroblastomas
#18
Jasmina Topcagic, Rebecca Feldman, Anatole Ghazalpour, Jeffrey Swensen, Zoran Gatalica, Semir Vranic
Olfactory neuroblastoma (ONB) is a rare, locally aggressive, malignant neoplasm originating in the olfactory epithelium in the nasal vault. The recurrence rate of ONB remains high and there are no specific treatment guidelines for recurrent/metastatic ONBs. This study retrospectively evaluated 23 ONB samples profiled at Caris Life Sciences (Phoenix, Arizona) using DNA sequencing (Sanger/NGS [Illumina], n = 15) and gene fusions (Archer FusionPlex, n = 6), whole genome RNA microarray (HumanHT-12 v4 beadChip, Illumina, n = 4), gene copy number assays (chromogenic and fluorescent in situ hybridization), and immunohistochemistry...
2018: PloS One
https://www.readbyqxmd.com/read/29285843/exosomes-serve-as-nanoparticles-to-suppress-tumor-growth-and-angiogenesis-in-gastric-cancer-by-delivering-hepatocyte-growth-factor-sirna
#19
Haiyang Zhang, Yi Wang, Ming Bai, Junyi Wang, Kegan Zhu, Rui Liu, Shaohua Ge, JiaLu Li, Tao Ning, Ting Deng, Qian Fan, Hongli Li, Wu Sun, Guoguang Ying, Yi Ba
Exosomes derived from cells have been found to mediate signal transduction between cells and to act as efficient carriers to deliver drugs and small RNA. Hepatocyte growth factor (HGF) is known to promote the growth of both cancer cells and vascular cells, and the HGF-cMET pathway is a potential clinical target. Here, we characterized the inhibitory effect of HGF siRNA on tumor growth and angiogenesis in gastric cancer. In addition, we showed that HGF siRNA packed in exosomes can be transported into cancer cells, where it dramatically downregulates HGF expression...
March 2018: Cancer Science
https://www.readbyqxmd.com/read/29285491/detection-of-met-amplification-in-gastroesophageal-tumor-specimens-using-iqfish
#20
Jan Trøst Jørgensen, Karsten Bork Nielsen, Jens Mollerup, Anna Jepsen, Ning Go
Background: The gene mesenchymal epithelial transition factor ( MET ) is a proto-oncogene that encodes a transmembrane receptor with intrinsic tyrosine kinase activity known as Met or cMet. MET is found to be amplified in several human cancers including gastroesophageal cancer. Methods: Here we report the MET amplification prevalence data from 159 consecutive tumor specimens from patients with gastric (G), gastroesophageal junction (GEJ) and esophageal (E) adenocarcinoma, using a novel fluorescence in situ hybridization (FISH) assay, MET /CEN-7 IQFISH Probe Mix [an investigational use only (IUO) assay]...
December 2017: Annals of Translational Medicine
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