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- Volume 13, Issue 4, 2013
Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 13, Issue 4, 2013
Volume 13, Issue 4, 2013
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A Small-molecule Inhibitor, 5'-O-Tritylthymidine, Targets FAK and Mdm-2 Interaction, and Blocks Breast and Colon Tumorigenesis in vivo
Authors: Vita M. Golubovskaya, Nadia L. Palma, Min Zheng, Baotran Ho, Andrew Magis, David Ostrov and William G. CanceFocal Adhesion Kinase (FAK) is overexpressed in many types of tumors and plays an important role in survival. We developed a novel approach, targeting FAK-protein interactions by computer modeling and screening of NCI small molecule drug database. In this report we targeted FAK and Mdm-2 protein interaction to decrease tumor growth. By macromolecular modeling we found a model of FAK and Mdm-2 interaction an Read More
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Mitoxantrone Targets the ATP-binding Site of FAK, Binds the FAK Kinase Domain and Decreases FAK, Pyk-2, c-Src, and IGF-1R In Vitro Kinase Activities
Authors: Vita M. Golubovskaya, Baotran Ho, Min Zheng, Andrew Magis, David Ostrov and William G. CanceFocal Adhesion Kinase (FAK) is a non-receptor kinase that is overexpressed in many types of tumors and plays a key role in cell adhesion, spreading, motility, proliferation, invasion, angiogenesis, and survival. Recently, FAK has been proposed as a target for cancer therapy, and we performed computer modeling and screening of the National Cancer Institute (NCI) small molecule compounds database to target the A Read More
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Upregulation of Focal Adhesion Kinase by 14-3-3ε via NFκB Activation in Hepatocellular Carcinoma
Authors: Bor-Sheng Ko, Yee-Jee Jan, Tzu-Ching Chang, Shu-Man Liang, Shyh-Chang Chen, Tzu-An Liu, Yao-Ming Wu, John Wang and Jun-Yang LiouFocal adhesion kinase (FAK) is implicated in cancer cell survival, proliferation and migration. Expression of FAK expression is elevated and associated with tumor progression and metastasis in various tumors, including hepatocellular carcinoma (HCC). Increased 14-3-3ε expression is shown to be a potential prognostic factor to predict higher risk of distant metastasis and worse overall survival in HCC. The aim of this st Read More
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Cell Survival Signaling in Neuroblastoma
Authors: Michael L. Megison, Lauren A. Gillory and Elizabeth A. BeierleNeuroblastoma is the most common extracranial solid tumor of childhood and is responsible for over 15% of pediatric cancer deaths. Neuroblastoma tumorigenesis and malignant transformation is driven by overexpression and dominance of cell survival pathways and a lack of normal cellular senescence or apoptosis. Therefore, manipulation of cell survival pathways may decrease the malignant potential of the Read More
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FAK and Nanog Cross Talk with p53 in Cancer Stem Cells
More LessThis review is focused on the role of Focal Adhesion Kinase (FAK) signaling in cancer stem cells. The recent data demonstrate the important role of FAK in cancer stem cell proliferation, differentiation, motility, and invasion. We showed recently that the transcription factor Nanog binds the FAK promoter and up-regulates FAK expression, and that FAK binds Nanog and phosphorylates it. This review discusses the interaction of FA Read More
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The Role of Focal Adhesion Kinase in Lung Cancer
By Grace K. DyFocal adhesion kinase (FAK) is a nonreceptor tyrosine kinase implicated in carcinogenesis through its pleitropic effects on cell proliferation, survival and metastasis. This article provides a summary of the existing data implicating FAK in lung cancer.
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FAK and HAS Inhibition Synergistically Decrease Colon Cancer Cell Viability and Affect Expression of Critical Genes
Authors: Melissa Heffler, Vita M. Golubovskaya, Jeffrey Conroy, Song Liu, Dan Wang, William G. Cance and Kelli B. DunnFocal adhesion kinase (FAK), hyaluronan (HA), and hyaluronan synthase-3 (HAS3) have been implicated in cancer growth and progression. FAK inhibition with the small molecule inhibitor Y15 decreases colon cancer cell growth in vitro and in vivo. HAS3 inhibition in colon cancer cells decreases FAK expression and activation, and exogenous HA increases FAK activation. We sought to determine the genes affected by H Read More
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Inhibiting the Interaction of cMET and IGF-1R with FAK Effectively Reduces Growth of Pancreatic Cancer Cells in vitro and in vivo
Pancreatic cancer is one of the most lethal diseases with no effective treatment. Previously, we have shown that FAK is overexpressed in pancreatic cancer and plays a key role in cancer cell survival and proliferation. FAK has been shown to interact with growth factor receptors including cMET and IGF-1R. As a novel therapeutic approach, we targeted the protein interaction of FAK with growth factor receptors to block tumor gro Read More
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Marine Natural Products and Related Compounds as Anticancer Agents: an Overview of their Clinical Status
Authors: Karina Petit and Jean-Francois BiardMarine ecosystems constitute a huge reservoir of biologically active secondary metabolites. Consequently during the last past few decades, several marine-derived molecules have been approved for anticancer treatment or are under clinical trials. This review reports the present state of the art of the sixteen molecules approved or currently on the clinical pipeline for anticancer chemotherapy. The molecules are classified accord Read More
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Synthesis and Anticancer Properties of a Novel Bis-intercalator
Authors: Wei Shen, Huimin Deng and Zhiqiang GaoA series of naphthalene diimide (ND)-based mono-, bis-, and tris-intercalators are synthesized and evaluated for their anticancer activities. All compounds show anticancer activities in the micromolar range. Among them the bis-intercalator is the most promising. Experimental results indicate that (i) target compounds intercalate DNA and (ii) the bis-intercalator with the optimal linker shows considerably more affinity to Read More
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Differential Binding Preference of Methylpheophorbide a and Its Diboronated Derivatives to Albumin and Low Density Lipoproteins
The tetrapyrrolic macrocycle and the functional groups at its periphery allow for a variety of modifications aimed at multifunctional therapeutic compounds. In particular, conjugation of boron polyhedra yields dual efficacy antitumor photo/ radiosensitizers. Structural optimization of these agents presumes the identification of macromolecules that bind and transport boronated tetrapyrroles. Using spectroscopic methods w Read More
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SJSZ Glycoprotein (38 kDa) Inhibits Cell Cycle and Oxidative Stress in N-Methyl-N`- nitro-N-nitrosoguanidine-induced ICR Mice
Authors: Jin Lee and Kye-Taek LimThe initiation stage of liver cancer is closely related to abnormal cell proliferation as observed for other types of carcinogenesis. Recently, we isolated a glycoprotein from Styrax japonica Siebold et al Zuccarini (SJSZ glycoprotein), which consists of a carbohydrate moiety (52.64%) and a protein moiety (47.36%). In this study, the antitumoric mechanism of SJSZ glycoprotein during the initiation stage in N-Methyl-N`-nitro-N Read More
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Antitumoral Activity of Indole-3-carbinol Cyclic tri- and Tetrameric Derivatives Mixture in Human Breast Cancer Cells: In Vitro and In Vivo Studies
Indole-3-carbinol (I3C) and its oligomeric derivatives have been widely studied for their chemopreventive and chemotherapeutic properties. We have previously shown that the I3C cyclic tetrameric derivative CTet inhibits breast cancer cell proliferation in vitro and in xenotrasplanted tumor. Here we report the antitumoral activity of a mixture of tri- and tetrameric cyclic I3C derivatives (CTr/CTet) both in vitro (MCF-7 and MDA- Read More
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Recombinant Snake Venom Cystatin Inhibits Tumor Angiogenesis in vitro and in vivo Associated with Downregulation of VEGF-A165, Flt-1 and bFGF
Authors: Qun Xie, Nanhong Tang, Rong Wan, Yuanlin Qi, Xu Lin and Jianyin LinPrevious studies have shown that recombinant snake venom cystatin (sv-cystatin) inhibits the invasion and metastasis of tumor cells in vitro and in vivo. The purpose of this study was to investigate the ability of recombinant sv-cystatin to inhibit tumor angiogenesis in vitro and in vivo, and the mechanisms underlying this effect. Recombinant sv-cystatin inhibited proliferation of human umbilical vein endothelial cells (HUVECs) at Read More
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N6-Isopentenyladenosine and its Analogue N6-Benzyladenosine Induce Cell Cycle Arrest and Apoptosis in Bladder Carcinoma T24 Cells
Cytokinins are phytohormones critically involved in the regulation of plant growth and development. They also affect the proliferation and differentiation of animal cells, thus representing new tools to treat diseases that involve dysfunctional cell growth and/or differentiation. Recently, by performing structure-function studies on human cells, we found that only N6-isopentenyladenosine and its benzyl analogue N6-benzyl Read More
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Volumes & issues
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Volume 25 (2025)
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Volume 24 (2024)
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Volume 23 (2023)
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Volume 22 (2022)
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Volume 21 (2021)
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Volume 20 (2020)
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Volume 19 (2019)
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Volume 18 (2018)
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Volume 17 (2017)
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Volume 16 (2016)
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Volume 15 (2015)
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Volume 14 (2014)
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Volume 13 (2013)
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Volume 12 (2012)
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Volume 11 (2011)
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Volume 10 (2010)
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Volume 9 (2009)
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Volume 8 (2008)
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Volume 7 (2007)
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Volume 6 (2006)
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