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- Aldskogius, Håkan
(författare)
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Regulation of microglia : potential new drug targets in the CNS.
- 2001
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Ingår i: Expert opinion on therapeutic targets. - 1472-8222 .- 1744-7631. ; 5:6, s. 655-668
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Tidskriftsartikel (refereegranskat)abstract
- Microglia respond to any disturbance in the CNS which poses a threat to physiological homeostasis. Although these responses are secondary, mainly to neuronal alterations, the way the microglial response evolves in many situations promotes further damage to the CNS. The list of clinical conditions in which this situation is a major problem is continuously growing and includes neurodegenerative diseases, stroke, trauma, demyelinating disorders and neuropathic pain. The significance of microglia for the pathogenesis of neurological and neuropsychiatric conditions has led to a rapidly expanding search for therapeutic possibilities to regulate microglial activity. As will be clear from this review, treatments which are currently available appear to offer some positive effects but are still far from satisfactory. A major challenge is to understand the mechanisms that determine whether activated microglia will develop into a cytotoxic or a cytoprotective component.
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| 4. |
- Di Gennaro, A, et al.
(författare)
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Targeting leukotriene B4 in inflammation
- 2014
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Ingår i: Expert opinion on therapeutic targets. - : Informa UK Limited. - 1744-7631 .- 1472-8222. ; 18:1, s. 79-93
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Tidskriftsartikel (refereegranskat)
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| 5. |
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| 6. |
- Edvinsson, Lars
(författare)
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Novel migraine therapy with calcitonin gene-regulated peptide receptor antagonists
- 2007
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Ingår i: Expert Opinion on Therapeutic Targets. - : Informa Healthcare. - 1472-8222 .- 1744-7631. ; 11:9, s. 1179-1188
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Forskningsöversikt (refereegranskat)abstract
- Primary headaches, for example, migraine and cluster headaches represent the most prevalent neurological disorders, affecting up to 15 - 20% of the adult population. There is a clear association between head pain and the release of calcitonin gene-related peptide (CGRP). In this review the role of CGRP in human cranial circulation is described and the role for specific CGRP antagonism elucidated. It is well known that triptans (5-HT1B/1D agonist) alleviate headache in part through normalisation of CGRP levels. The central role of CGRP in migraine pathophysiology has resulted in the development of small-molecule CGRP antagonists with no cardiovascular side effects. Such compounds have high selectivity for human CGRP receptors and are efficacious in the relief of acute migraine attacks. Research indicates that they effect the abluminal side of the blood-brain barrier and that they are not vasoconstrictive, providing a new dimension in therapy.
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| 7. |
- Ekman, Simon, et al.
(författare)
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Hsp90 as a therapeutic target in patients with oesophageal carcinoma
- 2010
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Ingår i: Expert opinion on therapeutic targets. - : Informa Healthcare. - 1472-8222 .- 1744-7631. ; 14:3, s. 317-328
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Forskningsöversikt (refereegranskat)abstract
- Importance of the field: Oesophageal carcinoma has a poor prognosis with a 5-year overall survival rate of only 10 - 20%. The disease is often diagnosed at a late stage, when dissemination may already have occurred, contributing to the poor prognosis. However, recent developments in targeted therapy now offer new possibilities in the treatment arsenal. Heat shock protein 90 (Hsp90) has been demonstrated to protect oncogenic variants of signalling molecules from degradation, thus promoting cell growth and survival. Hsp90 has been found to be abundantly expressed in oesophageal cancer and may serve as a therapeutic target in the treatment of this disease. Areas covered in this review: We have summarised available data concerning the role of Hsp90 in oesophageal carcinoma as well as available information on other tumour types. What the reader will gain: To be able to elaborate on the molecular mechanisms of action of Hsp90 and discuss state-of-the-art of clinical trials involving Hsp90 inhibitors in malignancies, with a special emphasis on oesophageal cancer. Take home message: Preclinical studies on Hsp90 inhibition in oesophageal cancer are promising and it is anticipated that in the near future clinical trials with Hsp90 inhibitors will be initiated also for oesophageal cancer, using the experience from other trials.
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| 8. |
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| 9. |
- Freimann, Krista, et al.
(författare)
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Galanin receptors as a potential target for neurological disease
- 2015
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Ingår i: Expert opinion on therapeutic targets. - : Informa UK Limited. - 1472-8222 .- 1744-7631. ; 19:12, s. 1665-1676
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Forskningsöversikt (refereegranskat)abstract
- INTRODUCTION: Galanin is a 29/30 amino acid long neuropeptide that is widely expressed in the brains of many mammals. Galanin exerts its biological activities through three different G protein-coupled receptors, GalR1, GalR2 and GalR3. The widespread distribution of galanin and its receptors in the CNS and the various physiological and pharmacological effects of galanin make the galanin receptors attractive drug targets.AREAS COVERED: This review provides an overview of the role of galanin and its receptors in the CNS, the involvement of the galaninergic system in various neurological diseases and the development of new galanin receptor-specific ligands.EXPERT OPINION: Recent advances and novel approaches in migrating the directions of subtype-selective ligand development and chemical modifications of the peptide backbone highlight the importance of the galanin neurochemical system as a potential target for drug development.
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