• It is well known that GPCR responsiveness desensitizes after

  2021-12-21

  

  It is well known that GPCR responsiveness desensitizes after prolonged exposure to agonists through several mechanisms such as receptor phosphorylation, arrestin binding and internalization (Dhami and Ferguson, 2006). Therefore, in the present work we decided to study whether group I-mGluR signaling

• Increased expression of Glut is detected in a number

  2021-12-21

  

  Increased expression of Glut1 is detected in a number of cancer types including lung [7], brain [8], bladder [9], cervical [10], colorectal [11], esophageal [12], hepatocellular [13], head and neck [14], gastric [15], ovarian [16], renal cell [17], pancreatic [18], thyroid [19] and breast [20]. Over

• Although GLP has greater insulin releasing effects at

  2021-12-21

  

  Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts

• Our own search towards aryl imidazole derived GSMs led to

  2021-12-21

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• At present many methods have been applied

  2021-12-21

  

  At present, many methods have been applied for multiple detection. For example, Concanamycin A [[9], [10], [11]] is frequently used to detect multiple targets because of its exquisite sensitivity and specificity, but it is difficult to design experiments to test short-length oligonucleotides. Elect

• Conclusions br Author information The obtained models of com

  2021-12-21

  

  Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu

• However the clinical development of was

  2021-12-21

  

  However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this rece

• Introduction Thrombotic disorders including ischemic heart

  2021-12-21

  

  Introduction Thrombotic disorders including ischemic heart disease, deep venous thrombosis, and ischemic stroke represent one of the most common causes of death in the world [1]. All these conditions relate to states accompanied by a shift of hemostasis balance into a coagulation side because of va

• br Acknowledgement The authors would like to thank the Unive

  2021-12-20

  

  Acknowledgement The authors would like to thank the University of Johannesburg and the National Research Foundation for the financial support. Mr. D Harris and Dr. R Meyer from Shimadzu South Africa are thanked for their technical support. Prof Ian Dubery is thanked for access to the LC-MS instru

• Renal disease is characterized by aberrant

  2021-12-20

  

  Renal disease is characterized by aberrant fibrotic remodeling of renal tissue, elevated apoptosis in kidney tissue, and eventual organ failure. In addition, patients with renal disease are more likely to suffer from systemic hypertension due to oxidative damage (reviewed in Ref. [18]). Treatment of

• Cells undergoing EMT display a downregulation of E cadherin

  2021-12-20

  

  Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the 350 receptor cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens junctions are specialized

• Cells undergoing EMT display a downregulation of E cadherin

  2021-12-20

  

  Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the 350 receptor cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens junctions are specialized

• Our last area of exploration was the piperidine core

  2021-12-20

  

  Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th

• Additionally OsGly I overexpressing transgenic rice plants

  2021-12-20

  

  Additionally, OsGly I-overexpressing transgenic rice plants had higher grain yields than WT (Table 2). Although there were no significant differences in the number of effective panicles per plant, panicle length, grain numbers per panicle, or 1000-grain weight between WT and transgenic plants, the s

• br Xenobiotics and the Glucocorticoid

  2021-12-20

  

  Xenobiotics and the Glucocorticoid Receptor Conclusion Transparency document Acknowledgements The author wishes to thank Professor Wilhelm Engström from the Swedish University of Agricultural Sciences (Department of Biomedical Sciences and Veterinary Public Health) for his proof reading

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