Zobrazeno 1 - 10
of 94
pro vyhledávání: '"Maikel Wijtmans"'
Publikováno v:
Pharmaceuticals, Vol 17, Iss 4, p 536 (2024)
The modulation of biological processes with light-sensitive chemical probes promises precise temporal and spatial control. Yet, the design and synthesis of suitable probes is a challenge for medicinal chemists. This article introduces a photocaging s
Externí odkaz:
https://doaj.org/article/1bdbc8b0bfa74bf9a416cfbd3237ec62
Autor:
Reggie Bosma, Nicola C. Dijon, Yang Zheng, Hannes Schihada, Niels J. Hauwert, Shuang Shi, Marta Arimont, Rick Riemens, Hans Custers, Andrea van de Stolpe, Henry F. Vischer, Maikel Wijtmans, Nicholas D. Holliday, Diederik W.D. Kuster, Rob Leurs
Publikováno v:
iScience, Vol 25, Iss 9, Pp 104882- (2022)
Summary: In this study, we synthesized and evaluated new photoswitchable ligands for the beta-adrenergic receptors β1-AR and β2-AR, applying an azologization strategy to the first-generation beta-blocker propranolol. The resulting compounds (Opto-p
Externí odkaz:
https://doaj.org/article/febb6a52402644b994ea390ddeafdfc7
Autor:
Zhiyong Wang, Reggie Bosma, Sebastiaan Kuhne, Jelle van den Bor, Wrej Garabitian, Henry F. Vischer, Maikel Wijtmans, Rob Leurs, Iwan J.P. de Esch
Publikováno v:
ACS Omega, Vol 6, Iss 19, Pp 12755-12768 (2021)
Externí odkaz:
https://doaj.org/article/1addc20d56fc415fb4173c268128d1b4
Autor:
Tom Dekker, Jaap W. Harteveld, Gábor Wágner, Max C. M. de Vries, Hans Custers, Andrea C. van de Stolpe, Iwan J. P. de Esch, Maikel Wijtmans
Publikováno v:
Molecules, Vol 28, Iss 4, p 1777 (2023)
Biomass-derived molecules can provide a basis for sustainable drug discovery. However, their full exploration is hampered by the dominance of millions of old-fashioned screening compounds in classical high-throughput screening (HTS) libraries frequen
Externí odkaz:
https://doaj.org/article/a7b2204081fc4a6b81b95b83d44cc530
Autor:
Xavier Gómez-Santacana, Sabrina M. de Munnik, Tamara A. M. Mocking, Niels J. Hauwert, Shanliang Sun, Prashanna Vijayachandran, Iwan J. P. de Esch, Henry F. Vischer, Maikel Wijtmans, Rob Leurs
Publikováno v:
Beilstein Journal of Organic Chemistry, Vol 15, Iss 1, Pp 2509-2523 (2019)
We report a detailed structure–activity relationship for the scaffold of VUF16216, a compound we have previously communicated as a small-molecule efficacy photoswitch for the peptidergic chemokine GPCR CXCR3. A series of photoswitchable azobenzene
Externí odkaz:
https://doaj.org/article/191d27a959cf464cbd751133e1acc2e9
Autor:
David J. Hamilton, Péter Ábrányi-Balogh, Aaron Keeley, László Petri, Martina Hrast, Tímea Imre, Maikel Wijtmans, Stanislav Gobec, Iwan J. P. de Esch, György Miklós Keserű
Publikováno v:
Pharmaceuticals, Vol 13, Iss 11, p 362 (2020)
Drug discovery programs against the antibacterial target UDP-N-acetylglucosamine enolpyruvyl transferase (MurA) have already resulted in covalent inhibitors having small three- and five-membered heterocyclic rings. In the current study, the reactivit
Externí odkaz:
https://doaj.org/article/6dd80a358b834ae49f8f35767510ca13
Autor:
Sylvia Ganghammer, Julia Gutjahr, Evelyn Hutterer, Peter W. Krenn, Susanne Pucher, Claudia Zelle-Rieser, Karin Jöhrer, Maikel Wijtmans, Rob Leurs, Martine J. Smit, Valter Gattei, Richard Greil, Tanja N. Hartmann
Publikováno v:
Haematologica, Vol 101, Iss 3 (2016)
Externí odkaz:
https://doaj.org/article/9e5f0d31e59c49cb8c797b828b9ca32d
Publikováno v:
Journal of Lipid Research, Vol 46, Iss 2, Pp 307-319 (2005)
Phospholipids reside in the surface layer of LDLs and constitute ∼20–25% of the particle by weight. We report a study of the primary products generated from the most abundant molecular species of phosphatidylcholines present in LDL during in vitr
Externí odkaz:
https://doaj.org/article/29cb8b34d8c6407898f51e971585ba0a
Autor:
Tom Dekker, Mathilde A. C. H. Janssen, Christina Sutherland, Rene W. M. Aben, Hans W. Scheeren, Daniel Blanco-Ania, Floris P. J. T. Rutjes, Maikel Wijtmans, Iwan J. P. de Esch
Publikováno v:
ACS Medicinal Chemistry Letters, 14, 583-590
Dekker, T, Janssen, M A C H, Sutherland, C, Aben, R W M, Scheeren, H W, Blanco-Ania, D, Rutjes, F P J T, Wijtmans, M & de Esch, I J P 2023, ' An Automated, Open-Source Workflow for the Generation of (3D) Fragment Libraries ', ACS medicinal chemistry letters, vol. 14, no. 5, pp. 583-590 . https://doi.org/10.1021/acsmedchemlett.2c00503
ACS Medicinal Chemistry Letters, 14, 5, pp. 583-590
Dekker, T, Janssen, M A C H, Sutherland, C, Aben, R W M, Scheeren, H W, Blanco-Ania, D, Rutjes, F P J T, Wijtmans, M & de Esch, I J P 2023, ' An Automated, Open-Source Workflow for the Generation of (3D) Fragment Libraries ', ACS medicinal chemistry letters, vol. 14, no. 5, pp. 583-590 . https://doi.org/10.1021/acsmedchemlett.2c00503
ACS Medicinal Chemistry Letters, 14, 5, pp. 583-590
The recent success of fragment-based drug discovery (FBDD) is inextricably linked to adequate library design. To guide the design of our fragment libraries, we have constructed an automated workflow in the open-source KNIME software. The workflow con
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f290b95a10c644f2244897f62175c70
https://doi.org/10.1021/acsmedchemlett.2c00503
https://doi.org/10.1021/acsmedchemlett.2c00503
Publikováno v:
Wijtmans, M, Josimovic, I, Vischer, H F & Leurs, R 2022, ' Optical control of Class A G protein-coupled receptors with photoswitchable ligands ', Current Opinion in Pharmacology, vol. 63, 102192, pp. 1-19 . https://doi.org/10.1016/j.coph.2022.102192
Curr Opin Pharmacol.
Curr Opin Pharmacol.
The field of photopharmacology of Class A GPCR ligands has recently attracted attention. In this review we analyze 31 papers on currently available photoswitchable ligands for Class A GPCRs. Using the six most recurring terms of all combined paper ab
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4416383a55aed139a9635d3eecb82ef3
https://doi.org/10.1016/j.coph.2022.102192
https://doi.org/10.1016/j.coph.2022.102192