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- Volume 5, Issue 3, 2012
Current Molecular Pharmacology - Volume 5, Issue 3, 2012
Volume 5, Issue 3, 2012
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GRK2 and Beta-Arrestins in Cardiovascular Disease: Established and Emerging Possibilities for Therapeutic Targeting
Authors: Alicia N. Harvey, Kristy Nguyen and Anastasios LymperopoulosHeptahelical G protein-coupled receptors, such as the β-adrenergic and the angiotensin II type 1 receptors, are the most diverse and therapeutically important family of receptors in the human genome, playing major roles in the physiology of various organs/tissues including the heart and blood vessels. Ligand binding activates heterotrimeric G proteins that transmit intracellular signals by regulating effector enzy Read More
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Crosstalk Signalling Role in Modulation of Drugs Side Effects
Authors: Susanna P. Garamszegi and Nandor GaramszegiTumourigenesis is regulated by the complex cell-matrix signalling interactions that incorporate feedback mechanisms from constantly evolving microenvironments. Under normal circumstances, these matrix signalling processes together with infiltrating immune cells tightly control the extent of tissue remodelling. They are the key elements of regulated homeostatic repair of local matrix architecture and biological function. In Read More
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Parkinson's Disease: A Role for the Immune System
Authors: Dwight C. German, Todd Eagar and Patricia K. SonsallaParkinson's disease (PD) is a progressive neurodegenerative disorder associated with the loss of catecholaminergic neurons in several brain regions. The motor symptoms of the disease are related to degeneration of the midbrain dopaminergic neurons, which occurs some time after the disease has begun. Both the innate and adaptive immune systems appear to play a role in the neurodegenerative process, and may con Read More
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G-Protein Coupled Receptor Resensitization - Appreciating the Balancing Act of Receptor Function
G-protein coupled receptors (GPCRs) are seven transmembrane receptors that are pivotal regulators of cellular responses including vision, cardiac contractility, olfaction, and platelet activation. GPCRs have been a major target for drug discovery due to their role in regulating a broad range of physiological and pathological responses. GPCRs mediate these responses through a cyclical process of receptor activation (initiation of Read More
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microRNA, Cancer and Cancer Chemoprevention
Authors: Xun Che and Chuanshu HuangmicroRNA(miRNA) is a kind of non-coding RNA that has a regulatory function on coding RNA. miRNA can target the 3' UTR of mRNA and inhibit its gene expression by either inhibiting its translation or promoting its degradation. miRNAs are thus considered to be oncogenic or antineoplastic, depending on their downstream target mRNAs. Besides their clinical application in cancer treatment, diagnosis, and prognosis, miRNA h Read More
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Molecular Mechanisms Mediating Nociceptin/Orphanin FQ Receptor Signaling, Desensitization and Internalization
Authors: Monica Baiula, Andrea Bedini and Gioia CarbonariIn 1994, the isolation of an opioid receptor-related clone soon led to the isolation and characterization of a novel neuropeptide, termed nociceptin or orphanin FQ (N/OFQ). This heptadecapeptide binds to the N/OFQ receptor (NOP) with high affinity, but does not interact directly with classical opioid receptors. The regional distribution of N/OFQ and of its receptor suggest any possible involvement of this neurotransmission syste Read More
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Bevacizumab and Angiogenesis Inhibitors in the Treatment of CNS Metastases: The Road less Travelled
Authors: Irina Veytsman, Jeanny B. Aragon-Ching and Sandra M. SwainThe incidence of central nervous system (CNS) metastases secondary to solid tumors is increasing. As more effective systemic therapy is being used in patients with solid tumors, patients with cancer live longer and are ultimately at higher risk for CNS metastases. However, CNS metastases remain challenging to treat because of limited available therapeutic options. This article reviews mechanisms of CNS metastases, the us Read More
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Estrogen Receptor Expression and its Relevant Signaling Pathway in Prostate Cancer: A Target of Therapy
Authors: Yasuhiro Nakamura, Keely M McNamara and Hironobu SasanoEstrogens have been recently postulated as potential agents in the development and progression of prostate cancer. Previous studies have demonstrated presence of both variants of estrogen receptor (ER); ER alpha (ERα) and ER beta (ERβ) in differing proportions between normal prostate and prostate cancer. It has been previously suggested that estrogens may either accelerate or inhibit growth of prostate cance Read More
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