The Experts below are selected from a list of 285 Experts worldwide ranked by ideXlab platform
Xiao’ao Long - One of the best experts on this subject based on the ideXlab platform.
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Wnt/β-catenin signaling pathway inhibits the proliferation and apoptosis of U87 glioma Cells via different mechanisms.
PloS one, 2017Co-Authors: Liyang Gao, Bing Chen, Fan Yang, Xuecheng Cen, Zhuangbing Liao, Xiao’ao LongAbstract:The Wnt signaling pathway is necessary for the development of the central nervous system and is associated with tumorigenesis in various cancers. However, the mechanism of the Wnt signaling pathway in glioma Cells has yet to be elucidated. Small-molecule Wnt modulators such as ICG-001 and AZD2858 were used to inhibit and stimulate the Wnt/β-catenin signaling pathway. Techniques including Cell proliferation Assay, colony formation Assay, Matrigel Cell invasion Assay, Cell Cycle Assay and Genechip microarray were used. Gene Ontology Enrichment Analysis and Gene Set Enrichment Analysis have enriched many biological processes and signaling pathways. Both the inhibiting and stimulating Wnt/β-catenin signaling pathways could influence the Cell Cycle, moreover, reduce the proliferation and survival of U87 glioma Cells. However, Affymetrix expression microarray indicated that biological processes and networks of signaling pathways between stimulating and inhibiting the Wnt/β-catenin signaling pathway largely differ. We propose that Wnt/β-catenin signaling pathway might prove to be a valuable therapeutic target for glioma.
H. Phillip Koeffler - One of the best experts on this subject based on the ideXlab platform.
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SAHA, a HDAC inhibitor, has profound anti-growth activity against non-small Cell lung cancer Cells
Oncology reports, 2006Co-Authors: Naoki Komatsu, Norihiko Kawamata, Seisho Takeuchi, Dong Yin, Wenwen Chien, Carl W. Miller, H. Phillip KoefflerAbstract:Current chemotherapy of advanced non-small Cell lung cancer (NSCLC) produces only a modest increase in survival time. New approaches are needed for this disease. The development of lung cancer is associated with silencing tumor suppressor genes that can occur not only by deletion or mutation, but also by epigenetic changes including histone deacetylation of key lysines. Histone deacetylase inhibitor (HDACI) increases histone acetylation, resulting in DNA with a more open chromatin that favors transcription. We found that the HDACI, suberoylanilide hydroxamic acid (SAHA), suppressed Cell growth of five non-small Cell lung cancer Cell lines in a dose-dependent manner (50% growth inhibition approximately 2 microM). Cell Cycle Assay by fluorescence-activated Cell sorting (FACS) demonstrated that SAHA induced a significant G0-G1 growth arrest of NSCLC Cells. Protein Assay by Western blot analysis showed that SAHA induced expression of p21WAF1. These results demonstrated that administration of SAHA may be a novel approach to the treatment of non-small Cell lung cancer.
Liyang Gao - One of the best experts on this subject based on the ideXlab platform.
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Wnt/β-catenin signaling pathway inhibits the proliferation and apoptosis of U87 glioma Cells via different mechanisms.
PloS one, 2017Co-Authors: Liyang Gao, Bing Chen, Fan Yang, Xuecheng Cen, Zhuangbing Liao, Xiao’ao LongAbstract:The Wnt signaling pathway is necessary for the development of the central nervous system and is associated with tumorigenesis in various cancers. However, the mechanism of the Wnt signaling pathway in glioma Cells has yet to be elucidated. Small-molecule Wnt modulators such as ICG-001 and AZD2858 were used to inhibit and stimulate the Wnt/β-catenin signaling pathway. Techniques including Cell proliferation Assay, colony formation Assay, Matrigel Cell invasion Assay, Cell Cycle Assay and Genechip microarray were used. Gene Ontology Enrichment Analysis and Gene Set Enrichment Analysis have enriched many biological processes and signaling pathways. Both the inhibiting and stimulating Wnt/β-catenin signaling pathways could influence the Cell Cycle, moreover, reduce the proliferation and survival of U87 glioma Cells. However, Affymetrix expression microarray indicated that biological processes and networks of signaling pathways between stimulating and inhibiting the Wnt/β-catenin signaling pathway largely differ. We propose that Wnt/β-catenin signaling pathway might prove to be a valuable therapeutic target for glioma.
Naoki Komatsu - One of the best experts on this subject based on the ideXlab platform.
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SAHA, a HDAC inhibitor, has profound anti-growth activity against non-small Cell lung cancer Cells
Oncology reports, 2006Co-Authors: Naoki Komatsu, Norihiko Kawamata, Seisho Takeuchi, Dong Yin, Wenwen Chien, Carl W. Miller, H. Phillip KoefflerAbstract:Current chemotherapy of advanced non-small Cell lung cancer (NSCLC) produces only a modest increase in survival time. New approaches are needed for this disease. The development of lung cancer is associated with silencing tumor suppressor genes that can occur not only by deletion or mutation, but also by epigenetic changes including histone deacetylation of key lysines. Histone deacetylase inhibitor (HDACI) increases histone acetylation, resulting in DNA with a more open chromatin that favors transcription. We found that the HDACI, suberoylanilide hydroxamic acid (SAHA), suppressed Cell growth of five non-small Cell lung cancer Cell lines in a dose-dependent manner (50% growth inhibition approximately 2 microM). Cell Cycle Assay by fluorescence-activated Cell sorting (FACS) demonstrated that SAHA induced a significant G0-G1 growth arrest of NSCLC Cells. Protein Assay by Western blot analysis showed that SAHA induced expression of p21WAF1. These results demonstrated that administration of SAHA may be a novel approach to the treatment of non-small Cell lung cancer.
Ahmed Kamal - One of the best experts on this subject based on the ideXlab platform.
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development and biological evaluation of imidazothiazole propenones as tubulin inhibitors that effectively triggered apoptotic Cell death in alveolar lung cancer Cell line
ChemistrySelect, 2017Co-Authors: Ibrahim Bin Sayeed, Koteswara Rao Garikapati, Venkata Krishna Kanth Makani, Apoorva Nagarajan, Mohd Adil Shareef, Abdallah Alarifi, Manika Palbhadra, Ahmed KamalAbstract:A new class of imidazothiazole-propenones was synthesized and investigated for their anti-proliferative activity against various human cancer Cell lines. Promising activities were observed in five congeners 8 k, 8 l, 8 n, 8 o and 8 v with interesting cytotoxicity profiles. The detailed biological aspects of these congeners towards human lung cancer Cell line (A549) were studied. Cell Cycle Assay revealed that these molecules arrested Cell growth in G2/M phase of the Cell Cycle in a concentration-dependent manner and lead to apoptotic Cell death, confirmed by caspase-3 activation Assay. Further, the tubulin polymerization inhibition analysis results suggested that these congeners exhibited significant inhibitory effect on the tubulin assembly. Western blotting displayed that pro-apoptotic proteins were markedly up regulated resulting in apoptosis. The investigations displayed that such congeners containing imidazothiazole-propenone have the potential in the development of newer chemotherapeutic agents.
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Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
Bioorganic & medicinal chemistry, 2016Co-Authors: G. Bharath Kumar, Mohd Adil Shareef, Anver Basha Shaik, V. Lakshma Nayak, Ibrahim Bin Sayeed, Vangala Santhosh Reddy, Rasala Mahesh, Mirza Feroz Baig, A. Ravikumar, Ahmed KamalAbstract:A series of phenstatin/isocombretastatin-oxindole conjugates was synthesized and tested for their cytotoxic activity against five human cancer Cells such as prostate (DU-145), lung (A549), colon (HT-29), breast (MCF-7), liver (HepG2) cancer Cells with IC50 values ranging from 0.049 to 38.90 μM. Amongst them, two conjugates (5c and 5d) showed broad spectrum of antiproliferative efficacy on lung cancer Cells with an IC50 value of 79 nM and 93 nM, respectively, whereas on colon cancer Cells with an IC50 values 45 nM and 49 nM, respectively. In addition, Cell Cycle Assay revealed that these conjugates (5c and 5d) arrest at the G2/M phase and leads to apoptotic Cell death which was confirmed by Annexin V-FITC and mitochondrial membrane depolarization. Further, the tubulin polymerization Assay analysis results suggest that these conjugates particularly 5c and 5d exhibit significant inhibitory effect on the tubulin assembly with an IC50 value of 1.23 μM and 1.01 μM, respectively. Molecular docking studies indicated that these compounds (5c and 5d) occupy the colchicine binding site of the tubulin.
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Pyrazole–oxadiazole conjugates: synthesis, antiproliferative activity and inhibition of tubulin polymerization
Organic & biomolecular chemistry, 2014Co-Authors: Ahmed Kamal, Anver Basha Shaik, Sowjanya Polepalli, Vangala Santosh Reddy, G. Bharath Kumar, Soma Gupta, K. V. S. Rama Krishna, Ananthamurthy Nagabhushana, Rakesh K. Mishra, Nishant JainAbstract:A number of pyrazole-oxadiazole conjugates were synthesized and evaluated for their ability to function as antiproliferative agents on various human cancer Cell lines. These conjugates are comprised of pyrazole and oxadiazole scaffolds closely attached to each other without any spacer as two structural classes. The Type I class has a trimethoxy substituent and the type II class has a 3,4-(methylenedioxy) substituent on their A rings. Among these conjugates 11a, 11d and 11f manifest potent cytotoxicity with IC50 values ranging from 1.5 μM to 11.2 μM and inhibit tubulin polymerization with IC50 values of 1.3 μM, 3.9 μM and 2.4 μM respectively. The Cell Cycle Assay showed that treatment with these conjugates results in accumulation of Cells in the G2/M phase and disrupts the microtubule network. Elucidation of zebrafish embryos revealed that the conjugates cause developmental defects. Molecular docking simulations determined the binding modes of these potent conjugates at the colchicine site of tubulin.