Zobrazeno 1 - 10
of 371
pro vyhledávání: '"A J, Bojarski"'
Autor:
Anna Stankiewicz, Katarzyna Kaczorowska, Ryszard Bugno, Aneta Kozioł, Maria H. Paluchowska, Grzegorz Burnat, Barbara Chruścicka, Paulina Chorobik, Piotr Brański, Joanna M. Wierońska, Beata Duszyńska, Andrzej Pilc, Andrzej J. Bojarski
Publikováno v:
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 211-225 (2022)
Considering the allosteric regulation of mGlu receptors for potential therapeutic applications, we developed a group of 1,2,4-oxadiazole derivatives that displayed mGlu4 receptor positive allosteric modulatory activity (EC50 = 282–656 nM). Selectiv
Externí odkaz:
https://doaj.org/article/986c7044b75f497b83b535e2846fde7c
Publikováno v:
Journal of Cheminformatics, Vol 13, Iss 1, Pp 1-8 (2021)
Abstract Depicting a ligand-receptor complex via Interaction Fingerprints has been shown to be both a viable data visualization and an analysis tool. The spectrum of its applications ranges from simple visualization of the binding site through analys
Externí odkaz:
https://doaj.org/article/b9e01b0333ff4fe3b62f6ff41fd5c169
Autor:
Dávid Bajusz, Warren S. Wade, Grzegorz Satała, Andrzej J. Bojarski, Janez Ilaš, Jessica Ebner, Florian Grebien, Henrietta Papp, Ferenc Jakab, Alice Douangamath, Daren Fearon, Frank von Delft, Marion Schuller, Ivan Ahel, Amanda Wakefield, Sándor Vajda, János Gerencsér, Péter Pallai, György M. Keserű
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-10 (2021)
Fragment-based drug discovery employs screening of small polar compounds typically exhibiting low affinity towards protein targets. Here, the authors combine the use of protein-based binding pharmacophores with the theory of protein hotspots to devel
Externí odkaz:
https://doaj.org/article/95bb508cd6554e5ea43dd584b6c41ad1
Autor:
Katarzyna Grychowska, Wojciech Pietruś, Ludmiła Kulawik, Ophélie Bento, Grzegorz Satała, Xavier Bantreil, Frédéric Lamaty, Andrzej J. Bojarski, Joanna Gołębiowska, Agnieszka Nikiforuk, Philippe Marin, Séverine Chaumont-Dubel, Rafał Kurczab, Paweł Zajdel
Publikováno v:
Molecules, Vol 28, Iss 3, p 1096 (2023)
Salt bridge (SB, double-charge-assisted hydrogen bonds) formation is one of the strongest molecular non-covalent interactions in biological systems, including ligand–receptor complexes. In the case of G-protein-coupled receptors, such an interactio
Externí odkaz:
https://doaj.org/article/813c1b8b56594a4e9a7cc04e5eb520b2
Publikováno v:
Molecules, Vol 28, Iss 2, p 490 (2023)
Currently, G protein-coupled receptors (GPCRs) constitute a significant group of membrane-bound receptors representing more than 30% of therapeutic targets. Fluorine is commonly used in designing highly active biological compounds, as evidenced by th
Externí odkaz:
https://doaj.org/article/559e0679c117414196be797e1f236ff9
Autor:
Vittorio Canale, Wojciech Trybała, Séverine Chaumont-Dubel, Paulina Koczurkiewicz-Adamczyk, Grzegorz Satała, Ophélie Bento, Klaudia Blicharz-Futera, Xavier Bantreil, Elżbieta Pękala, Andrzej J. Bojarski, Frédéric Lamaty, Philippe Marin, Paweł Zajdel
Publikováno v:
Biomolecules, Vol 13, Iss 1, p 12 (2022)
In addition to the canonical Gs adenylyl cyclase pathway, the serotonin type 6 receptor (5-HT6R) recruits additional signaling pathways that control cognitive function, brain development, and synaptic plasticity in an agonist-dependent and independen
Externí odkaz:
https://doaj.org/article/359b495a9fb64b6395f525a0ff337ced
Autor:
Jolanta Dyniewicz, Stefan Mordalski, Piotr F. J. Lipiński, Andrzej J. Bojarski, Piotr Kosson, Joanna Matalińska, Aleksandra Misicka
Publikováno v:
Pharmacological Reports. 75:465-473
Background G protein-coupled receptors (GPCRs) transduce external stimuli into the cell by G proteins via an allosteric mechanism. Agonist binding to the receptor stimulates GDP/GTP exchange within the heterotrimeric G protein complex, whereas recent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8d99e1280c0f243fb7220d618a72ccb
https://doi.org/10.1007/s43440-023-00457-5
https://doi.org/10.1007/s43440-023-00457-5
Publikováno v:
Molecules, Vol 27, Iss 3, p 1005 (2022)
Fluorine is a common substituent in medicinal chemistry and is found in up to 50% of the most profitable drugs. In this study, a statistical analysis of the nature, geometry, and frequency of hydrogen bonds (HBs) formed between the aromatic and aliph
Externí odkaz:
https://doaj.org/article/22010f55c5ec4f809b592f104bacb84b
Autor:
Krzysztof Marciniec, Rafał Kurczab, Maria Książek, Ewa Bębenek, Elwira Chrobak, Grzegorz Satała, Andrzej J. Bojarski, Joachim Kusz, Paweł Zajdel
Publikováno v:
Chemistry Central Journal, Vol 12, Iss 1, Pp 1-12 (2018)
Abstract A series of azinesulfonamide derivatives of long-chain arylpiperazines with variable-length alkylene spacers between sulfonamide and 4-arylpiperazine moiety is designed, synthesized, and biologically evaluated. In vitro methods are used to d
Externí odkaz:
https://doaj.org/article/15d0490c26fd4615adc6c75587e8b1be
Autor:
Lucja Kudla, Ryszard Bugno, Sabina Podlewska, Lukasz Szumiec, Lucja Wiktorowska, Andrzej J. Bojarski, Ryszard Przewlocki
Publikováno v:
Pharmaceutics, Vol 14, Iss 1, p 55 (2021)
Among different approaches to the search for novel—safer and less addictive—opioid analgesics, biased agonism has received the most attention in recent years. Some μ-opioid receptor agonists with G protein bias, including SR compounds, were prop
Externí odkaz:
https://doaj.org/article/bb245714fddc472f878e903337a1c137