Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Nidhal Selmi"'
Autor:
Catherine Bardelle, James M. Smith, Nidhal Selmi, Alice Lanne, Robert J. Sheppard, Daniel Hillebrand O'donovan, Jon Read, Geoffrey A. Holdgate
Publikováno v:
Drug discovery today. 27(4)
Dysregulation of the epigenome is associated with the onset and progression of several diseases, including cancer, autoimmune, cardiovascular, and neurological disorders. Members from the three families of epigenetic proteins (readers, writers, and e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1767602e5f23f8762840780554ff6b00
https://pubmed.ncbi.nlm.nih.gov/34728375
https://pubmed.ncbi.nlm.nih.gov/34728375
Autor:
Kenneth L. Granberg, Zhong-Qing Yuan, Bo Lindmark, Karl Edman, Johan Kajanus, Anders Hogner, Marcus Malmgren, Gavin O’Mahony, Anneli Nordqvist, Jan Lindberg, Stefan Tångefjord, Michael Kossenjans, Christian Löfberg, Jonas Brånalt, Dongmei Liu, Nidhal Selmi, Grigorios Nikitidis, Peter Nordberg, Ahlke Hayen, Anna Aagaard, Eva Hansson, Majlis Hermansson, Ida Ivarsson, Rasmus Jansson-Löfmark, Ulla Karlsson, Ulrika Johansson, Lena William-Olsson, Judith Hartleib-Geschwindner, Krister Bamberg
Publikováno v:
Journal of Medicinal Chemistry. 62:1385-1406
The mechanism-based risk for hyperkalemia has limited the use of mineralocorticoid receptor antagonists (MRAs) like eplerenone in cardio-renal diseases. Here, we describe the structure and property-driven lead generation and optimization, which resul
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0f3415ae30a4bd17f715f083a4fc37e
https://doi.org/10.1021/acs.jmedchem.8b01523
https://doi.org/10.1021/acs.jmedchem.8b01523
Ring systems in pharmaceuticals, agrochemicals and dyes are ubiquitous chemical motifs. Whilst the synthesis of common ring systems is well described, and novel ring systems can be readily computationally enumerated, the synthetic accessibility of un
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c3f81f439fab203928039c0b00f3cf8
Autor:
Tomas Akerud, Hannah de la Motte, Eva Hurt-Camejo, Tim D. J. Perkins, Åsa Månsson, Frank Jansen, Hans-Georg Beisel, Mikael Dahlström, Gabrielle Saarinen, Fabrizio Giordanetto, Robert G. Roth, Marie Ahlqvist, Fredrik Klingegård, Birgitta Rosengren, Laurent Knerr, Kenth Hallberg, Ingemar Starke, Jenny Sandmark, Daniel Pettersen, Nidhal Selmi, Margareta Herslöf, Johan Brengdahl, Tommy Olsson, Mattias Rohman, Peter Nordberg, Johan Broddefalk
Publikováno v:
ACS Medicinal Chemistry Letters. 9:594-599
[Image: see text] In order to assess the potential of sPLA(2)-X as a therapeutic target for atherosclerosis, novel sPLA(2) inhibitors with improved type X selectivity are required. To achieve the objective of identifying such compounds, we embarked o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3062a7d8619a16b010f0164ff18f98cf
https://doi.org/10.1021/acsmedchemlett.7b00505
https://doi.org/10.1021/acsmedchemlett.7b00505
Autor:
Per-Ola Norrby, Lynette A. Smyth, Ola Engkvist, Edward C. Sherer, Nidhal Selmi, Willi Amberg, Yu-hong Lam, Thomas Erhard, Zhengwei Peng
Publikováno v:
Drug Discovery Today. 23:1203-1218
Over the past few decades, various computational methods have become increasingly important for discovering and developing novel drugs. Computational prediction of chemical reactions is a key part of an efficient drug discovery process. In this revie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e6a48fe7cb179b7b40a7f2f9492e237
https://doi.org/10.1016/j.drudis.2018.02.014
https://doi.org/10.1016/j.drudis.2018.02.014
Phenotypic high-throughput screening platform identifies novel chemotypes for necroptosis inhibition
Autor:
Rui Moreira, Natália Aniceto, Ieuan Roberts, Hugo Brito, Rita C. Guedes, Martina Fitzek, Cecília M. P. Rodrigues, Ulf Börjesson, Nidhal Selmi, Dean G. Brown, Marta B. Afonso, David M. Smith, Vanda Marques
Publikováno v:
Cell Death Discovery
Cell Death Discovery, Vol 6, Iss 1, Pp 1-13 (2020)
Cell Death Discovery, Vol 6, Iss 1, Pp 1-13 (2020)
Regulated necrosis or necroptosis, mediated by receptor-interacting kinase 1 (RIPK1), RIPK3 and pseudokinase mixed lineage kinase domain-like protein (MLKL), contributes to the pathogenesis of inflammatory, infectious and degenerative diseases. Recen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34167117284c1506dbe26a6a39eee1b5
https://pubmed.ncbi.nlm.nih.gov/32123582
https://pubmed.ncbi.nlm.nih.gov/32123582
Autor:
Niek Dekker, Fabrizio Giordanetto, Laurent Knerr, Lars-Olof Larsson, Nidhal Selmi, Jenny Sandmark, Ulla Karlsson, Eva Hurt-Camejo, Peter Nordberg, Marie Castaldo, Mikael Dahlström, Birgitta Rosengren, Ingemar Starke, Daniel Pettersen
Publikováno v:
ACS Medicinal Chemistry Letters. 7:884-889
Expedited structure-based optimization of the initial fragment hit 1 led to the design of (R)-7 (AZD2716) a novel, potent secreted phospholipase A2 (sPLA2) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cc1bd66b430756a7150d5201c276dbbd
https://doi.org/10.1021/acsmedchemlett.6b00188
https://doi.org/10.1021/acsmedchemlett.6b00188
Autor:
Thierry Kogej, Ying Zhang, Nidhal Selmi, Robert A. Goodnow, Xia Tian, Matthew Clark, Gregory S. Basarab
Publikováno v:
MedChemComm. 7:1316-1322
The generation of novel chemical leads for clinical development is a constant challenge in the pharmaceutical industry. The synthesis of DNA-encoded libraries has emerged as a powerful method for hit and lead generation. We report the development of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b8021a9e357208f5e112dd4bae914ca1
https://doi.org/10.1039/c6md00088f
https://doi.org/10.1039/c6md00088f
Autor:
Johannes Wikström, Johan Brengdahl, Hanna De La Motte, Hans Georg Beisel, Maria Wågberg, Robert G. Roth, Mikael Dahlström, Nidhal Selmi, Gabrielle Saarinen, Daniel Pettersen, Fabrizio Giordanetto, Eva Hurt-Camejo, Åsa Månsson, Frank Jansen, Mattias Rohman, Laurent Knerr, Fredrik Klingegård, Birgitta Rosengren, Marie Ahlqvist, Tomas Akerud, Jenny Sandmark, Johan Broddefalk, Peter Nordberg
[Image: see text] A lead generation campaign identified indole-based sPLA(2)-X inhibitors with a promising selectivity profile against other sPLA(2) isoforms. Further optimization of sPLA(2) selectivity and metabolic stability resulted in the design
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5426bebf6e544cdf4fd5b3f245895890
https://europepmc.org/articles/PMC6047026/
https://europepmc.org/articles/PMC6047026/
Autor:
Lars Löfgren, Tomas Drmota, Kristina Wallenius, Stefan Hallén, Jianming Liu, Nidhal Selmi, Mattias Rohman, Martin Bauer, Bo Lindmark, Therese Admyre, Judith Hartleib-Geschwindner, Mikael Bjursell, Lena Amrot-Fors, Maria Andersson
Publikováno v:
Chemistry & Biology. 21(11):1486-1496
SummaryInhibition of AMP deaminase (AMPD) holds the potential to elevate intracellular adenosine and AMP levels and, therefore, to augment adenosine signaling and activation of AMP-activated protein kinase (AMPK). To test the latter hypothesis, novel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e52a07f3903cfcb1da19e4209fe17eba