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- Volume 23, Issue 29, 2017
Current Pharmaceutical Design - Volume 23, Issue 29, 2017
Volume 23, Issue 29, 2017
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Protein Kinases as Tumor Biomarkers and Therapeutic Targets
Authors: Chuntao Quan, Juanjuan Xiao, Lin Liu, Qiuhong Duan, Ping Yuan and Feng ZhuOver the last three decades, neoplasms have become the largest cause of human mortality due to both high tumor incidence and mortality. Chemotherapy is one of the main therapies employed to treat neoplasms. Although classical genotoxic drugs, such as cyclophosphamide, 5-FU, cisplatin and doxorubicin have been applied in clinical settings and have achieved very good treatment efficacy, many cancer patients di Read More
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Protein Tyrosine Signaling and its Potential Therapeutic Implications in Carcinogenesis
Authors: Mihwa Kim, Minwoo Baek and Dae J. KimProtein tyrosine phosphorylation is a crucial signaling mechanism that plays a role in epithelial carcinogenesis. Protein tyrosine kinases (PTKs) control various cellular processes including growth, differentiation, metabolism, and motility by activating major signaling pathways including STAT3, AKT, and MAPK. Genetic mutation of PTKs and/or prolonged activation of PTKs and their downstream pathways can lead to the develop Read More
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Molecular Targeting of ERKs/RSK2 Signaling in Cancers
More LessAccumulating studies have provided concrete evidence that p90 ribosomal S6 kinase 2 (RSK2) is a key signaling molecule involved in cell proliferation, transformation, and cancer development. RSK2 is known to be an etiological gene of Coffin-Lowry Syndrome (CLS). Recently, signaling analysis and molecular biological approaches have provided concrete evidence that RSK2 plays an essential role in human cancers. Her Read More
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Role of Protein Kinases and Their Inhibitors in Radiation Response of Tumor Cells
Authors: Byeong M. Kim, Wonsuck Yoon, Jung-Hyun Shim, Haiyoung Jung, Ji H. Lim, Hyun-Jung Choi, MiRan Seo, Tae H. Lee and Sang-Hyun MinPhosphorylation, the addition of a phosphate group to a molecule, is an effective way of regulating the biological properties of that molecule. Protein phosphorylation is a post-translational modification of proteins and affects cellular signaling transduction. Protein kinases induce phosphorylation by catalyzing the transfer of phosphate groups to serine, threonine, and tyrosine residues on protein substrates. Consist Read More
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Protein Kinases as Targets for Opisthorchis viverrini- Associated Cholangiocarcinoma Therapy
Authors: Watcharin Loilome and Hasaya DokduangProtein kinases are enzymes that catalyze the transfer of phosphate from ATP to the serine/threonine or tyrosine residues of target molecules. These are key important mediators in a signaling cascade involved in several biological processes. Dysregulation of their activity has been found in various tumors. From the increased understanding of kinase structure and activation mechanisms emerged new strategies for targeting Read More
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Targeting Protein Kinases for the Treatment of Glioblastoma Multiforme: Linking Basic Studies to Clinical Applications
By Aidong ZhouGlioblastoma multiforme (GBM) is the most common malignant primary brain tumor in adults with intensive heterogeneity and one of the most lethal human cancers. Protein kinases control diverse cellular processes by coordinating different signaling pathways. Protein kinases are frequently dysregulated in human cancers, which contributes to tumor initiation and development. Thus, protein kinases are a growing drug target Read More
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Protein Kinase Inhibitors as Therapeutic Drugs in AML: Advances and Challenges
Authors: Yuan Ling, Zikang Zhang, Hua Zhang and Zunnan HuangAcute myeloid leukemia (AML) is a malignant blood disorder and the cure rate has been remarkably improved over the past decade. However, recurrent or refractory leukemia remains the major problem of the AML and no clearly effective therapy has been established so far. Traditional treatments such as chemotherapy and hematopoietic stem cell transplantation are both far dissatisfying the patients partly for their indi Read More
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Induction of Synthetic Lethality by Natural Compounds Targeting Cancer Signaling
Authors: Lee Farrand and Sanguine ByunDespite the breakthroughs that have been achieved, significant unmet needs relating to the inadequate efficacy and toxicity of currently-available cancer therapies remain. Kinase inhibitors are a class of agents that target signaling factors responsible for the survival of malignant cells, and may address at least some of these issues. The concept of synthetic lethality provides a potential solution to counteract pathway redundanci Read More
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Discovery and Development of ATP-Competitive mTOR Inhibitors Using Computational Approaches
More LessThe mammalian target of rapamycin (mTOR) is a central controller of cell growth, proliferation, metabolism, and angiogenesis. This protein is an attractive target for new anticancer drug development. Significant progress has been made in hit discovery, lead optimization, drug candidate development and determination of the three-dimensional (3D) structure of mTOR. Computational methods have been applied to acceler Read More
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GSK3 Inhibitors in the Therapeutic Development of Diabetes, Cancer and Neurodegeneration: Past, Present and Future
Authors: Mudasir Maqbool and Nasimul HodaGSK3 has gained a considerable attention of researchers in the late 1970s as an inevitable drug target to treat diabetes. Furthermore, it was found to have a key role in the development of diseases like cancer and neurodegeneration (ND). A broad spectrum of GSK3 inhibitors have been discovered from time to time in order to curb these diseases. Inhibition of GSK3 by insulin boosts the dephosphorylation of glycogen syn Read More
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Application of Kinase Inhibitors for Anti-aging Intervention
Authors: Mercedes Cano, Antonio Ayala, Francesco Marotta and Sandro ArguellesProtein phosphorylation, mediated by protein kinases, has important physiological and pathological implications in our lives. Targeting kinase is one of the most interesting of the emerging topics in the pharmaceutical industry, especially since there is a focus on cancer therapy. Given that kinases may be involved in the aging process the focus will be on using the kinase inhibitor for anti-aging intervention to enhance health Read More
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Protein Kinase Inhibitors as Potential Antimicrobial Drugs Against Tuberculosis, Malaria and HIV
Authors: Yong Cheng, Jeffrey S. Schorey, Cheng-Cai Zhang and Xuejuan TanInfectious diseases that are caused by pathogenic microbes such as bacteria, viruses, parasites or fungi remain the top major cause of death across the world, particularly in low income countries, and may be transmitted from person to person, or from insects or animals. In general, infectious diseases may be treated with antimicrobial agents including antibiotics, antiviral, antifungal or antiparasitic medications. The t Read More
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Class A GPCRs: Structure, Function, Modeling and Structure-based Ligand Design
Authors: Xiaojing Cong, Jeremie Topin and Jerome GolebiowskiG protein-coupled receptors (GPCRs), especially the class A, are the most heavily investigated drug targets in the pharmaceutical industry. Tremendous efforts have been made by both industry and academia to understand the molecular structure and function of this large family of transmembrane proteins. Our understanding in GPCR activation has evolved from the classical inactive-active two-state model to a com Read More
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Targeting CD147 is a Novel Strategy for Antitumor Therapy
Authors: ChengXiang Lian, Yeye Guo, Jianglin Zhang, Xiang Chen and Cong PengCD147 is a membrane protein belonging to immunoglobulin superfamily and expressed in the cell membrane, which is also named with an extracellular matrix metalloproteinase inducer (EMMPRIN) because this molecule induces adjacent fibroblasts or tumor cells to produce MMPs, facilitating tumor cells migration and invasion. Accumulating evidences have shown that CD147 is over-expressed in various tumors, incl Read More
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Dual Roles of Pin1 in Cancer Development and Progression
Authors: Hyeong-jun Han, Bu Y. Choi and Young-Joon SurhPin1 is a unique peptidyl-prolyl cis/trans isomerase (PPIase) that catalyzes the cis/trans isomerization of peptidyl-prolyl peptide bonds of its substrate proteins by binding to their specific phosphorylated Ser/Thr-Pro (pSer/Thr-Pro) motifs. This alters the conformation of target proteins and consequently affects their stability, intracellular localization, and/or biological functions. The abnormal overexpression of Pin1 is observe Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
- Issue 46
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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