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- Volume 19, Issue 28, 2012
Current Medicinal Chemistry - Volume 19, Issue 28, 2012
Volume 19, Issue 28, 2012
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Ligands for Fluorescence Correlation Spectroscopy on G Protein-Coupled Receptors
Authors: D. Jakobs, T. Sorkalla and H. HaberleinG protein-coupled receptors (GPCRs) comprise a large protein family of transmembrane receptors involved in many physiological processes. They are engaged in various transduction processes of extracellular signals into intracellular responses. Due to their involvement in numerous diseases they represent an important pharmacological target. Fluorescence correlation spectroscopy (FCS) poses a very sensitive analytical tech Read More
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Activatable Fluorescent Probes: A New Concept in Optical Molecular Imaging
Authors: E. Lacivita, M. Leopoldo, F. Berardi, N. A. Colabufo and R. PerroneActivatable fluorescent probes share the unique feature of being turned on only under specific conditions: they are "silent" when not interacting with a specific target protein, microenvironment, or reactive species. Several activatable fluorescence probes have demonstrated their potential in cell biology study, disease study and diagnosis, and even in the rapidly expanding field of image-guided surgery. In this review, we will su Read More
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Recent Advances in Receptor-Targeted Fluorescent Probes for In Vivo Cancer Imaging
Authors: M. Bai and D. J. BornhopReceptor-targeted optical imaging of cancer is emerging as an attractive strategy for early cancer diagnosis and surgical guidance. The success of such strategy depends largely upon the development of receptor-targeted fluorescent probes with high specificity and binding affinity to the target receptors. Recently, a host of such probes have been reported to target cancer-specific receptors, such as somatostatin receptors (SST Read More
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Recent Advances in Optical Cancer Imaging of EGF Receptors
Authors: G. Kramer-Marek, M. R. Longmire, P. L. Choyke and H. KobayashiEpidermal growth factor (EGF) receptors are commonly expressed on the cell membrane of cancer cells and activity of these receptors results in accelerated cell growth and carcinogenesis. A variety of targeted molecules have been developed to block ligand binding and/or inhibit the function of these receptor tyrosine kinases, and several have proven therapeutic benefits. Along with the advent of new therapeutic agents com Read More
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Near Infrared Receptor-Targeted Nanoprobes for Early Diagnosis of Cancers
More LessThe success of detecting cancer at early stages relies greatly on the sensitivity and specificity of in vivo molecular imaging. Optical imaging with near infrared (NIR) luminescent molecular nanoprobes currently attracts much attention because of many advantages of this imaging modality. It provides real time imaging with relatively inexpensive cost, produces images with high sensitivity and spatial resolution, and avoids expo Read More
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Noninvasive Fluorescence Imaging in Animal Models of Stroke
Authors: N. Stemmer, J. Mehnert, J. Steinbrink and A. WunderNoninvasive fluorescence imaging (NFI) is a powerful tool to study physiology and pathophysiology in animal disease models. NFI has been successfully applied in a number of animal disease models including cancer, arthritis, and stroke. Furthermore, several applications in humans have been described. NFI is widely available in research laboratories because it has a number of advantages: It uses non-ionizing radiation an Read More
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The Bioisosteric Concept Applied to Cannabinoid Ligands
Authors: C. Mugnaini, S. Pasquini and F. CorelliBioisosterism is widely used in medicinal chemistry as an approach aimed at either rationally modifying a hit compound into a more potent and/or selective molecule or a lead compound into a more drug-like one. Two different cannabinoid receptors have been cloned from mammalian tissues, the CB1 receptor, mostly expressed in brain, and the CB2 receptor, mostly expressed in the immune system, both regulating a variety o Read More
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L-Type Voltage-Dependent Calcium Channels As Therapeutic Targets for Neurodegenerative Diseases
Authors: T. Yagami, H. Kohma and Y. YamamotoCa2+ is a highly versatile intracellular second messenger in the central nervous system, and regulates many complicated cellular processes, including excitation, plasticity and apoptosis. Influx of Ca2+ from the extracellular fluid is required for sustained elevation of the cytosolic Ca2+ concentration and full activation of Ca2+-dependent processes. Voltage-dependent Ca2+ channels (VDCCs) serve as the principal route Read More
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2-Arylindoles: A Privileged Molecular Scaffold with Potent, Broad-Ranging Pharmacological Activity
Authors: S. Lal and T. J. SnapePrivileged structures bind to multiple receptors with high affinity, thus aiding the development of novel biologically active compounds. Indoles are classed as privileged structures, and as a result of the indole nucleus being present in a broad range of biologically active molecules, it has been suggested that indoles probably represent the most important of all structural classes in drug discovery. Amongst the indole class of co Read More
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Modulation of Poly(A)-specific Ribonuclease (PARN): Current Knowledge and Perspectives
Authors: N. A.A. Balatsos, P. Maragozidis, D. Anastasakis and C. StathopoulosDeadenylation is the exoribonucleolytic shortening of eukaryotic poly(A) tails. It is often the first and rate-limiting step for mRNA decay and translational silencing. The process is catalysed by a diversity of deadenylases, which provide robust and flexible means to control mRNA levels and gene expression. Poly(A)-specific ribonuclease (PARN) is a major mammalian deadenylase and the only known to concurrently bind the 5 Read More
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Role of Oxidative Stress and Molecular Changes in Liver Fibrosis: A Review
Authors: V. Sanchez-Valle, N. C. Chavez-Tapia, M. Uribe and N. Mendez-SanchezLiver fibrosis represents a health problem with significant morbidity and mortality that affects 100 million people worldwide. It is a final pathway to several chronic liver diseases and is characterized by excess collagen and accumulation of extracellular matrix in response to chronic hepatocellular damage. Clinical and experimental data suggest that oxidative stress (OS) mediates the progression of fibrosis, and that Read More
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New Clinical Perspectives of Hypolipidemic Drug Therapy in Severe Hypercholesterolemia
Authors: C. Stefanutti, C. Morozzi and S. Di GiacomoPatients with homozygous familial hypercholesterolemia (HoFH) represent the most severe patients within the spectrum of dyslipidemias. Untreated Low-Density Lipoprotein Cholesterol (LDL-C) levels in these patients are usually in the range 500 to 1200 mg/dL. Moreover, these patients exhibit a scarce responsiveness or even non responsiveness to oral lipid lowering agents. Patients with heterozygous familial hypercholesterolemi Read More
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Therapeutic Potential of Cholesteryl O-acyl α-glucoside Found in Helicobacter pylori
Authors: M. Shimamura and H. HidakaSteryl glycosides are derivatives of sterols where the 3β-hydroxy group is glycosylated. Some of them are further converted to steryl O-acyl glycosides. Steryl glycosides and their derivatives are widely distributed in plants, algae, and fungi, but are relatively rarely distributed in bacteria and animals. Accumulating evidence suggests that glycosylation of sterols not only modifies physicochemical properties of cell membra Read More
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State of the Art of the Therapeutic Perspective of Sorafenib Against Hematological Malignancies
Authors: G. Zauli, R. Voltan, V. Tisato and P. SecchieroThe bi-aryl urea multi-kinase inhibitor Sorafenib (BAY 43-9006, Nexavar) was initially approved for the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma. Eleven years after its first description in PubMed, the therapeutic potential of Sorafenib has been evaluated in an increasing number of studies, mainly focused on solid tumors. More recently, the potential usefullness of Sorafenib has s Read More
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Protocatechuic Acid Alkyl Esters: Hydrophobicity As a Determinant Factor for Inhibition of NADPH Oxidase
This study presents the increased efficiency of NADPH oxidase inhibition produced by esterification of protocatechuic acid (P0). Alkyl esters bearing chain lengths of 4 (P4), 7 (P7) and 10 (P10) carbons were synthesized and their oxidation potential, hydrophobicity, antiradical activity, inhibition of superoxide anion (O2 °-), and the abilities to affect hypochlorous acid (HOCl) production by leukocytes and inhibit myeloperoxidase (MPO Read More
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Volumes & issues
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Volume 32 (2025)
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Volume 31 (2024)
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Volume 30 (2023)
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Volume 29 (2022)
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Volume 28 (2021)
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Volume 27 (2020)
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Volume 26 (2019)
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Volume 25 (2018)
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Volume 24 (2017)
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Volume 23 (2016)
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Volume 22 (2015)
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Volume 21 (2014)
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Volume 20 (2013)
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Volume 19 (2012)
- Issue 36
- Issue 35
- Issue 34
- Issue 33
- Issue 32
- Issue 31
- Issue 30
- Issue 29
- Issue 28
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- Issue 12
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- Issue 10
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- Issue 7
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- Issue 1
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Volume 18 (2011)
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Volume 17 (2010)
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Volume 16 (2009)
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Volume 15 (2008)
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Volume 14 (2007)
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Volume 13 (2006)
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Volume 12 (2005)
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Volume 11 (2004)
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Volume 10 (2003)
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Volume 9 (2002)
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Volume 8 (2001)
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Volume 7 (2000)
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