Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Matilde Caivano"'
Autor:
Mao Xiang Chen, Matilde Caivano, Sumitra Ramachandran, Emma Ward, Sandy Toh, Mahmood Ahmed, A. Richard Rutter, Kirsten L. Searle, Yannick M. L. Lacroix
Publikováno v:
ASSAY and Drug Development Technologies. 16:445-455
Mitochondrial permeability transition pore (mPTP) formation is well documented in isolated mitochondria. However, convincing detection of mPTP in whole cells remains elusive. In this study, we describe a high-throughput assay for Ca2+-activated mPTP
Autor:
Diane M. Coe, Simon J. F. Macdonald, Davina Humphreys, Philip Alan Skone, Haydn Terence Jones, George Hardy, Iain M. McLay, Annette Miles-Williams, David House, Matilde Caivano, Iain Uings, Keith Biggadike, Margaret Clackers, Vicki Weller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4846-4850
Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NFκB agonist activity was optimised in an iterative process from pIC50 7.5 (for 7), to pIC50 10.1 (for 38E1). An explanation for the SAR observed based is presented a
Autor:
Bajin Han, Ryan P. Trump, Timothy M. Willson, Jean-Baptiste E. GlaxoSmithKline Blanc, Peter Brown, David W. Gray, Matilde Caivano, Eugene L. Stewart, Philip Stewart Turnbull, William J. Hoekstra
Publikováno v:
Journal of Combinatorial Chemistry. 9:107-114
We describe the design, using shape comparison and fast docking computer algorithms, and rapid parallel synthesis of a 1300 member array based on GSK7721, a 4-aminobenzonitrile androgen receptor (AR) antagonist identified by focused screening of the
Publikováno v:
Journal of Biological Chemistry. 276:48693-48701
Prostaglandins are important mediators of activated macrophage functions, and their inducible synthesis is mediated by cyclooxygenase-2 (COX-2). Here, we make use of the murine macrophage cells RAW264 as well as of immortalized macrophages derived fr
Publikováno v:
Journal of Biological Chemistry. 276:40769-40777
Cyclooxygenase-2 (COX-2) is the rate-limiting enzyme for the inducible synthesis of prostaglandins, and its up-regulated activity is thought to play a pathological role in diseases such as inflammatory bowel disease, rheumatoid arthritis, and cancer.
Autor:
Matilde Caivano
Publikováno v:
FEBS Letters. 429:249-253
Bacterial lipopolysaccharide (LPS) in the presence of interferon gamma (IFNgamma) stimulates the synthesis of the cationic amino acid transporter 2B (CAT-2B) and inducible nitric oxide synthetase (iNOS) in RAW264 macrophages, which are thought to und
Autor:
Paul W. Smith, Poonam Shah, William Cairns, Mythily Vimal, Matilde Caivano, David Brown, Nicolas Bertheleme, Stephen P. Watson, Joseph Rimland, Iain Uings, Rosemary Z. Sasse, Pier D’Alessandro, Ryan P. Trump, Dino Montanari, David Standing, David N. Smith, David W. Gray, Sheraz Gul, Suchete S. Hunjan, Angela Dunne
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure–activity relationships and the process of optimisation of an initial HTS hit are also descri
Publikováno v:
The international journal of neuropsychopharmacology. 1(1)
Pharmacological investigations have suggested the involvement of the cAMP transduction pathway in the action of antidepressant drugs and in the pathophysiology of mood disorders. We have extended these studies to determine the time-related effects of
Autor:
Matilde Caivano, Philip Cohen
Publikováno v:
Journal of immunology (Baltimore, Md. : 1950). 164(6)
LPS stimulation of RAW264 macrophages triggered the activation of mitogen- and stress-activated protein kinases-1 and -2 (MSK1, MSK2) and their putative substrates, the transcription factors cyclic AMP response element-binding protein (CREB) and acti
Autor:
Mike Hutton, Vivienne F. Murphy, G.W. Roberts, Karen Duff, Matilde Caivano, John B. Davis, John Hardy, Amanda J. L. Barton, Laura G. Bresciani, Eric Karran, Carol W. Gray, Robin V. Ward
Publikováno v:
Neurodegeneration : a journal for neurodegenerative disorders, neuroprotection, and neuroregeneration. 5(4)
Presenilin-1 (PS-1) has been identified as the protein encoded by the chromosome 14 locus that, when mutated, leads to familial Alzheimer's disease (FAD). Using PS-1 transfected SHSY5Y neuroblastoma cells, we have demonstrated by immunodetection, usi