Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Mansoor Chishty"'
Autor:
Eliezer Masliah, Birgit Hutter-Paier, Katharina Strempfl, Miriam Holztrattner, Julia Garnweidner-Raith, Michael S. Unger, Nadine Pillichshammer, Thomas K. Felder, Edward Rockenstein, Johannes Attems, Julia Marschallinger, Iris Leister, Mary Johnson, Barbara Altendorfer, Mansoor Chishty, Ludwig Aigner
Publikováno v:
Neurotherapeutics
Dementia with Lewy bodies (DLB) represents a huge medical need as it accounts for up to 30% of all dementia cases, and there is no cure available. The underyling spectrum of pathology is complex and creates a challenge for targeted molecular therapie
Autor:
David E. Hibbs, Stephen J. Fuller, James O'Brien-Brown, Leanne Stokes, Michael Kassiou, Melissa L. Barron, Kristen K. Skarratt, Danielle J. Vugts, Eryn L. Werry, Mansoor Chishty, Albert D. Windhorst, Shane M. Wilkinson, Jennifer Ong, Bieneke Janssen
Publikováno v:
ACS Chemical Neuroscience, 8(11), 2374-2380. American Chemical Society
Wilkinson, S M, Barron, M L, O'Brien-Brown, J, Janssen, B, Stokes, L, Werry, E L, Chishty, M, Skarratt, K K, Ong, J A, Hibbs, D E, Vugts, D J, Fuller, S, Windhorst, A D & Kassiou, M 2017, ' Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X 7 Receptor Antagonist ', ACS Chemical Neuroscience, vol. 8, no. 11, pp. 2374-2380 . https://doi.org/10.1021/acschemneuro.7b00272
Wilkinson, S M, Barron, M L, O'Brien-Brown, J, Janssen, B, Stokes, L, Werry, E L, Chishty, M, Skarratt, K K, Ong, J A, Hibbs, D E, Vugts, D J, Fuller, S, Windhorst, A D & Kassiou, M 2017, ' Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X 7 Receptor Antagonist ', ACS Chemical Neuroscience, vol. 8, no. 11, pp. 2374-2380 . https://doi.org/10.1021/acschemneuro.7b00272
Adamantanyl benzamide 1 was identified as a potent P2X7R antagonist but failed to progress further due to poor metabolic stability. We describe the synthesis and SAR of a series of bioisosteres of benzamide 1 to explore improvements in the pharmacolo
Autor:
Jeroen J.M. Hoozemans, Rostislav V Shevchenko, Ger T. Molenaar, Veerle Baekelandt, Sylvie Chalon, Aurélie Doméné, Guy Bormans, Adriana Maggi, Wissam Beaino, Michael Kassiou, Adriaan A. Lammertsma, Uta Funke, Shane M. Wilkinson, Robert C. Schuit, Alessandro Villa, Esther J.M. Kooijman, Johan van den Hoek, Bieneke Janssen, Anke Van der Perren, Mansoor Chishty, Danielle J. Vugts, Albert D. Windhorst, Dieter Ory
Publikováno v:
Scientific Reports, Vol 8, Iss 1, Pp 1-10 (2018)
Janssen, B, Vugts, D J, Wilkinson, S M, Ory, D, Chalon, S, Hoozemans, J J M, Schuit, R C, Beaino, W, Kooijman, E J M, Van Den Hoek, J, Chishty, M, Doméné, A, Van Der Perren, A, Villa, A, Maggi, A, Molenaar, G T, Funke, U, Shevchenko, R V, Baekelandt, V, Bormans, G, Lammertsma, A A, Kassiou, M & Windhorst, A D 2018, ' Identification of the allosteric P2X 7 receptor antagonist [ 11 C]SMW139 as a PET tracer of microglial activation ', Scientific Reports, vol. 8, no. 1, 6580 . https://doi.org/10.1038/s41598-018-24814-0
Scientific Reports, 8(1):6580. Nature Publishing Group
Janssen, B, Vugts, D J, Wilkinson, S M, Ory, D, Chalon, S, Hoozemans, J J M, Schuit, R C, Beaino, W, Kooijman, E J M, Van Den Hoek, J, Chishty, M, Doméné, A, Van Der Perren, A, Villa, A, Maggi, A, Molenaar, G T, Funke, U, Shevchenko, R V, Baekelandt, V, Bormans, G, Lammertsma, A A, Kassiou, M & Windhorst, A D 2018, ' Identification of the allosteric P2X 7 receptor antagonist [ 11 C]SMW139 as a PET tracer of microglial activation ', Scientific Reports, vol. 8, no. 1, 6580 . https://doi.org/10.1038/s41598-018-24814-0
Scientific Reports, 8(1):6580. Nature Publishing Group
The P2X7 receptor plays a significant role in microglial activation, and as a potential drug target, the P2X7 receptor is also an interesting target in positron emission tomography. The current study aimed at the development and evaluation of a poten
Autor:
Bieneke, Janssen, Danielle J, Vugts, Shane M, Wilkinson, Dieter, Ory, Sylvie, Chalon, Jeroen J M, Hoozemans, Robert C, Schuit, Wissam, Beaino, Esther J M, Kooijman, Johan, van den Hoek, Mansoor, Chishty, Aurélie, Doméné, Anke, Van der Perren, Alessandro, Villa, Adriana, Maggi, Ger T, Molenaar, Uta, Funke, Rostislav V, Shevchenko, Veerle, Baekelandt, Guy, Bormans, Adriaan A, Lammertsma, Michael, Kassiou, Albert D, Windhorst
Publikováno v:
Scientific Reports
The P2X7 receptor plays a significant role in microglial activation, and as a potential drug target, the P2X7 receptor is also an interesting target in positron emission tomography. The current study aimed at the development and evaluation of a poten
Autor:
Shane M, Wilkinson, Melissa L, Barron, James, O'Brien-Brown, Bieneke, Janssen, Leanne, Stokes, Eryn L, Werry, Mansoor, Chishty, Kristen K, Skarratt, Jennifer A, Ong, David E, Hibbs, Danielle J, Vugts, Stephen, Fuller, Albert D, Windhorst, Michael, Kassiou
Publikováno v:
ACS chemical neuroscience. 8(11)
Adamantanyl benzamide 1 was identified as a potent P2X
Publikováno v:
NeuroRX. 2:554-571
Summary: The worldwide market for therapies for CNS disorders is worth more than $50 billion and is set to grow substantially in the years ahead. This is because: 1) the incidence of many CNS disorders (e.g., Alzheimer’s disease, stroke, and Parkin
Publikováno v:
Journal of Drug Targeting. 12:265-272
A number of nucleoside analogues, consisting of antiviral compounds and agents designed as adenosine A1 receptor agonists, were examined for nucleoside transporter affinity using an in vitro model of the blood-brain barrier (BBB), the rat brain endot
Publikováno v:
NeuroReport. 14:1087-1090
Multiple nucleoside transport systems exist in the body yet the subtypes functional at the blood-brain barrier (BBB) have not been fully investigated. We have employed RBE4 immortalised rat brain endothelial cells to functionally identify the carrier
Publikováno v:
Glia. 39:99-104
The blood-brain barrier (BBB) is formed by the presence of tight junction complexes between brain endothelial cells that restrict paracellular permeability. As a consequence, a number of transport proteins are expressed on cerebral endothelial cells
S-adenosylmethionine is substrate for carrier mediated transport at the blood-brain barrier in vitro
Publikováno v:
Brain research. 942(1-2)
S-adenosylmethionine (SAM) is the sole methyl donor in the CNS where it is involved in a multitude of biochemical reactions. Peripherally administered SAM has been shown to increase SAM levels in cerebrospinal fluid and is reported to be effective in