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Author (up) Akhurst, R.J.; Hata, A. file  url
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  Title Targeting the TGFbeta signalling pathway in disease Type Journal Article
  Year 2012 Publication Nature Reviews. Drug Discovery Abbreviated Journal Nat Rev Drug Discov  
  Volume 11 Issue 10 Pages 790-811  
  Keywords Animals; Drug Delivery Systems/*methods; Humans; Protein Binding/physiology; Receptors, Transforming Growth Factor beta/antagonists & inhibitors/metabolism; Signal Transduction/drug effects/*physiology; Transforming Growth Factor beta/*antagonists & inhibitors/*physiology  
  Abstract Many drugs that target transforming growth factor-beta (TGFbeta) signalling have been developed, some of which have reached Phase III clinical trials for a number of disease applications. Preclinical and clinical studies indicate the utility of these agents in fibrosis and oncology, particularly in augmentation of existing cancer therapies, such as radiation and chemotherapy, as well as in tumour vaccines. There are also reports of specialized applications, such as the reduction of vascular symptoms of Marfan syndrome. Here, we consider why the TGFbeta signalling pathway is a drug target, the potential clinical applications of TGFbeta inhibition, the issues arising with anti-TGFbeta therapy and how these might be tackled using personalized approaches to dosing, monitoring of biomarkers as well as brief and/or localized drug-dosing regimens.  
  Call Number Serial 1548  
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Author (up) Cox, D.; Brennan, M.; Moran, N. file  url
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  Title Integrins as therapeutic targets: lessons and opportunities Type Journal Article
  Year 2010 Publication Nature Reviews. Drug Discovery Abbreviated Journal Nat Rev Drug Discov  
  Volume 9 Issue 10 Pages 804-820  
  Keywords Animals; Drug Delivery Systems/*methods/trends; Humans; Integrins/*antagonists & inhibitors/*chemistry/physiology; Neoplasms/drug therapy/metabolism; Structure-Activity Relationship  
  Abstract The integrins are a large family of cell adhesion molecules that are essential for the regulation of cell growth and function. The identification of key roles for integrins in a diverse range of diseases, including cancer, infection, thrombosis and autoimmune disorders, has revealed their substantial potential as therapeutic targets. However, so far, pharmacological inhibitors for only three integrins have received marketing approval. This article discusses the structure and function of integrins, their roles in disease and the chequered history of the approved integrin antagonists. Recent advances in the understanding of integrin function, ligand interaction and signalling pathways suggest novel strategies for inhibiting integrin function that could help harness their full potential as therapeutic targets.  
  Call Number Serial 1190  
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Author (up) Tse, M.T. file  url
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  Title G protein-coupled receptors: Breathing easier with bitter tastes Type Journal Article
  Year 2010 Publication Nature Reviews. Drug Discovery Abbreviated Journal Nat Rev Drug Discov  
  Volume 9 Issue 12 Pages 918-919  
  Keywords Agonists; COPD; Taste receptor  
  Abstract The discovery that inhaled agonists of bitter taste receptors in airway smooth muscle (ASM) can dilate airways, reported in Nature Medicine, has opened up a potential strategy for the treatment of chronic obstructive pulmonary disease (COPD) and asthma.First, a screen of isolated human ASM looking for new G protein-coupled receptor (GPCR) targets, which are the major receptor family controlling ASM relaxation and constriction, unexpectedly identified bitter taste receptors (the taste receptor type 2 (TAS2R) family) in this tissue.  
  Call Number Serial 170  
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