Zobrazeno 1 - 10
of 16
pro vyhledávání: '"José Manuel Bartolomé-Nebreda"'
Autor:
Sebastiaan Bijttebier, Dina Rodrigues Martins, Liesbeth Mertens, Karolien Grauwen, Wouter Bruinzeel, Roland Willems, José Manuel Bartolomé-Nebreda, Clara Theunis, Alexis Bretteville, Andreas Ebneth, Lieve Dillen
Publikováno v:
Journal of Proteome Research. 22:1309-1321
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::93055646cca8e6b19373c144611dd86f
https://doi.org/10.1021/acs.jproteome.2c00822
https://doi.org/10.1021/acs.jproteome.2c00822
Autor:
José Manuel Bartolomé-Nebreda, Adriana Ingrid Velter, Peter Jacobus Johannes Antonius Buijnsters, Andrés A. Trabanco
Publikováno v:
Expert Opinion on Therapeutic Patents. 31:1117-1154
Introduction: O-GlcNAcylation is a highly abundant post-translational modification of multiple proteins, including the microtubule-binding protein tau, governed by just two enzymes’ concerted actio...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ee8ef238f0aa8391ae62a82b47711df
https://doi.org/10.1080/13543776.2021.1947242
https://doi.org/10.1080/13543776.2021.1947242
Autor:
Francisca Delgado, Jordi Royes, Alcira del Cerro, Fulgencio Tovar, Juan Antonio Vega, Paul Shaffer, Andrés A. Trabanco, Elena Fernández, Alexis Bretteville, Gary Tresadern, Andreas Ebneth, José Manuel Bartolomé-Nebreda, Carlos M Martínez-Viturro, Liesbeth Mertens, Marijke Somers, Aránzazu García Molina, José Manuel Alonso
Publikováno v:
Journal of Medicinal Chemistry. 63:14017-14044
O-GlcNAcylation is a post-translational modification of tau understood to lower the speed and yield of its aggregation, a pathological hallmark of Alzheimer's disease (AD). O-GlcNAcase (OGA) is the only enzyme that removes O-linked N-acetyl-d-glucosa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d6809022dc4f30d2c2ddc4a4e35ae8f
https://doi.org/10.1021/acs.jmedchem.0c01479
https://doi.org/10.1021/acs.jmedchem.0c01479
Autor:
Carlos M. Martínez-Viturro, Colleen M. Niswender, Thomas M. Bridges, Claire Mackie, María Luz Martín-Martín, Miguel-Angel Pena, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones, José Manuel Bartolomé-Nebreda, Thomas Steckler, Silvia López, Han Min Tong, Hilde Lavreysen, J. Scott Daniels, Sergio A. Alonso de Diego, Jesús Alcázar, P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:429-434
As part of our efforts to identify a suitable back-up compound to our recently disclosed mGlu5 positive allosteric modulator (PAM) clinical candidate VU0490551/JNJ-46778212, this letter details the investigation and challenges of a novel series of 6,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c3b86aa42123689c0f8547589986f3f
https://doi.org/10.1016/j.bmcl.2015.11.098
https://doi.org/10.1016/j.bmcl.2015.11.098
Autor:
José Manuel Bartolomé-Nebreda, Thomas Steckler, Susana Conde-Ceide, Colleen M. Niswender, Chrysa Malosh, María Piedrafita, Meredith J. Noetzel, Claire Mackie, Paige N. Vinson, Jerri M. Rook, Gregor James Macdonald, M. Rosa Sánchez-Casado, P. Jeffrey Conn, Shaun R. Stauffer, Carlos M. Martínez-Viturro, Hilde Lavreysen, J. Scott Daniels, Carrie K. Jones, Mark Turlington, Thomas M. Bridges, Craig W. Lindsley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5115-5120
We report the optimization of a series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from an acyl dihydropyrazolo[1,5-a]pyrimidinone class. Investigation of exocyclic amide transpositions with this unique 5,6-bicy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b8088322559a22014da4ba8a0d907b9
https://doi.org/10.1016/j.bmcl.2015.10.009
https://doi.org/10.1016/j.bmcl.2015.10.009
Autor:
Susana Conde-Ceide, Craig W. Lindsley, P. Jeffrey Conn, Gregor James Macdonald, Colleen M. Niswender, J. Scott Daniels, Claire Mackie, Ya Zhou, José Manuel Bartolomé-Nebreda, Thomas Steckler, Chrysa Malosh, Carlos M. Martínez-Viturro, Jesús Alcázar, Thomas M. Bridges, Hilde Lavreysen, Shaun R. Stauffer, Carrie K. Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3515-3519
This Letter describes the progress and challenges in the continued optimization of the mGlu5 positive allosteric modulator (PAM) clinical candidate VU0490551/JNJ-46778212. While many analogs addressed key areas for improvement, no one compound posses
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7441129eb76aa61e9831657c5e991b6
https://doi.org/10.1016/j.bmcl.2015.06.096
https://doi.org/10.1016/j.bmcl.2015.06.096
Autor:
Carlos M. Martínez-Viturro, Colleen M. Niswender, Han Min Tong, Meredith J. Noetzel, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, P. Jeffrey Conn, Shaun R. Stauffer, Craig W. Lindsley, María Luz Martín-Martín, Thomas M. Bridges, J. Scott Daniels, Hilde Lavreysen, Silvia López, Sergio A. Alonso de Diego
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1310-1317
We report the discovery and SAR of two novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs). Exploration of several structural features in the western
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4a364a4c4741589a3db21524a2a658a
https://doi.org/10.1016/j.bmcl.2015.01.038
https://doi.org/10.1016/j.bmcl.2015.01.038
Autor:
A. Ahnaou, Xavier Langlois, Wilhelmus Drinkenburg, José Manuel Bartolomé-Nebreda, Thomas Steckler
Publikováno v:
Psychopharmacology. 232:1107-1122
Evidence is emerging that positive and negative modulation of the metabotropic glutamate (mGluR5) receptors has the potential for treating cognitive deficits and neuroprotection associated with psychiatric and neurodegenerative diseases, respectively
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72c07c598116ae311253621cb4b138c6
https://doi.org/10.1007/s00213-014-3746-4
https://doi.org/10.1007/s00213-014-3746-4
Autor:
Shaun R. Stauffer, Thomas M. Bridges, J. Scott Daniels, Meredith J. Noetzel, Hilde Lavreysen, Colleen M. Niswender, Craig W. Lindsley, P. Jeffrey Conn, Han Min Tong, Susana Conde-Ceide, José Manuel Bartolomé-Nebreda, Thomas Steckler, Carrie K. Jones, Paige N. Vinson, Gregor James Macdonald, Claire Mackie, Mark Turlington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3641-3646
We report the optimization of a series of novel metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from a 5,6-bicyclic class of dihydropyrazolo[1,5-a]pyridin-4(5H)-ones containing a phenoxymethyl linker. Studies focused o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::570caf0830a9486752156fe572e3bde1
https://doi.org/10.1016/j.bmcl.2014.04.087
https://doi.org/10.1016/j.bmcl.2014.04.087
Autor:
Jason Manka, Hilde Lavreysen, Colleen M. Niswender, Jon Jacobs, M. Luz Martín-Martín, P. Jeffrey Conn, Meredith J. Noetzel, Han Min Tong, Elizabeth J. Herman, C. David Weaver, Chrysa Malosh, J. Scott Daniels, Susana Conde-Ceide, Paige N. Vinson, Shaun R. Stauffer, Gregor James Macdonald, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, Silvia López, Craig W. Lindsley, Carrie K. Jones, Satyawan Jadhav, Mark Turlington
Publikováno v:
Journal of Medicinal Chemistry. 57:5620-5637
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu5) represent a promising therapeutic strategy for the treatment of schizophrenia. Starting from an acetylene-based lead from high throughput screening, an evolved bicycli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec9e09891e97fb3e6b29c5a56f045fdf
https://doi.org/10.1021/jm500259z
https://doi.org/10.1021/jm500259z