Zobrazeno 1 - 10
of 204
pro vyhledávání: '"Lipophilic efficiency"'
Autor:
Robert Roskoski Jr.
Publikováno v:
Pharmacological Research, Vol 194, Iss , Pp 106847- (2023)
Owing to genetic alterations and overexpression, the dysregulation of protein kinases plays a significant role in the pathogenesis of many autoimmune and neoplastic disorders and protein kinase antagonists have become an important drug target. Althou
Externí odkaz:
https://doaj.org/article/6a816da400b14d8fb6032c3e46c8f1b6
Autor:
Robert Roskoski, Jr.
Publikováno v:
Pharmacological Research, Vol 191, Iss , Pp 106774- (2023)
Because genetic alterations including mutations, overexpression, translocations, and dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this enzyme family is the target of many drug discovery programs in the pharmace
Externí odkaz:
https://doaj.org/article/dc98d3078f1b4bef841fad25cdca6d3c
Akademický článek
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Akademický článek
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Autor:
Yusra Sajid Kiani, Ishrat Jabeen
Publikováno v:
Computation, Vol 7, Iss 2, p 26 (2019)
The cytochrome P450s (CYPs) play a central role in the metabolism of various endogenous and exogenous compounds including drugs. CYPs are vulnerable to inhibition and induction which can lead to adverse drug reactions. Therefore, insights into the un
Externí odkaz:
https://doaj.org/article/df12f12edace469c8a2068b697b5e9dc
Autor:
Richard Tjhen, Noriko Uchiyama, Michiko Tawada, Yohei Kosugi, Satoshi Endo, Huikai Sun, Kei Masuda, Makoto Fushimi, Tatsuki Koike, Weston Lane
Publikováno v:
Journal of Medicinal Chemistry. 64:1103-1115
O-GlcNAcase (OGA) has received increasing attention as an attractive therapeutic target for tau-mediated neurodegenerative disorders; however, its role in these pathologies remains unclear. Therefore, potent chemical tools with favorable pharmacokine
Autor:
Strang Ross Sinclair, Markus Streiff, Daniel J. McKay, Johannes Ottl, Andreas Billich, Claudia Betschart, Stephanie Harlfinger, Eloísa Jiménez-Núñez, Nigel Graham Cooke, Christine Guntermann, Markus Voegtle, Janet Dawson, Samuel Hintermann, Klemens Kaupmann, Rowan Stringer, Christian Beerli, Nathalie Gobeau, Juergen Wagner, Klemens Hoegenauer, Joerg Kallen, Peter Ertl
Publikováno v:
Journal of Medicinal Chemistry. 62:10816-10832
Retinoic acid receptor-related orphan receptor gamma-t (RORγt) is considered to be the master transcription factor for the development of Th17 cells that produce proinflammatory cytokines such as IL-17A. Overproportionate Th17 cell abundance is asso
Autor:
Shawn K. Milano, Qingqiu Huang, Thuy-Tien T. Nguyen, Sekar Ramachandran, Aaron Finke, Irina Kriksunov, David J. Schuller, D. Marian Szebenyi, Elke Arenholz, Lee A. McDermott, N. Sukumar, Richard A. Cerione, William P. Katt
Publikováno v:
The Journal of Biological Chemistry
Cancer cells frequently exhibit uncoupling of the glycolytic pathway from the TCA cycle (i.e., the “Warburg effect”) and as a result, often become dependent on their ability to increase glutamine catabolism. The mitochondrial enzyme Glutaminase C
Publikováno v:
Molecules
Volume 26
Issue 12
Molecules, Vol 26, Iss 3542, p 3542 (2021)
Volume 26
Issue 12
Molecules, Vol 26, Iss 3542, p 3542 (2021)
Curcuminoids are the main bioactive components of the well-known Asian spice and traditional medicine turmeric. Curcuminoids have poor chemical stability and bioavailability
in vivo they are rapidly metabolized to a set of bioreduced derivatives
in vivo they are rapidly metabolized to a set of bioreduced derivatives
Autor:
Thierry Christophe, Nicolas Houvenaghel, Philippe Clément-Lacroix, Reginald Brys, Line Oste, Inge Duys, Emanuelle Wakselman, Bertrand Heckmann, Caroline Joannesse, Alex Jaunet, Adeline Marie Elise Palisse, Brigitte Allart, Laurent Saniere, Mia Jans, Monica Borgonovi, Sandy El Bkassiny, Oscar Mammoliti, Beatrice Coornaert, Christel Jeanne Marie Menet, Kathleen Sonck
Publikováno v:
Journal of medicinal chemistry. 64(9)
Mounting evidence from the literature suggests that blocking S1P2 receptor (S1PR2) signaling could be effective for the treatment of idiopathic pulmonary fibrosis (IPF). However, only a few antagonists have been so far disclosed. A chemical enablemen