Zobrazeno 1 - 10
of 531
pro vyhledávání: '"Rob Leurs"'
Autor:
Shane Denecke, Madeline F. Malfara, Kelly R. Hodges, Nikki A. Holmes, Andre R. Williams, Julia H. Gallagher-Teske, Julia M. Pascarella, Abigail M. Daniels, Geert Jan Sterk, Rob Leurs, Gordon Ruthel, Rachel Hoang, Megan L. Povelones, Michael Povelones
Publikováno v:
mSphere, Vol 9, Iss 10 (2024)
ABSTRACT Trypanosomatids are single-celled parasites responsible for human and animal disease. Typically, colonization of an insect host is required for transmission. Stable attachment of parasites to insect tissues via their single flagellum coincid
Externí odkaz:
https://doaj.org/article/a6014f6cadd84ebdab05a5e7194aaddd
Autor:
Ruixue Xia, Shuang Shi, Zhenmei Xu, Henry F. Vischer, Albert D. Windhorst, Yu Qian, Yaning Duan, Jiale Liang, Kai Chen, Anqi Zhang, Changyou Guo, Rob Leurs, Yuanzheng He
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-13 (2024)
Abstract The histamine H4 receptor (H4R) plays key role in immune cell function and is a highly valued target for treating allergic and inflammatory diseases. However, structural information of H4R remains elusive. Here, we report four cryo-EM struct
Externí odkaz:
https://doaj.org/article/bb329f6ecb7241a28d3a490e5bc87b0e
Publikováno v:
Biomolecules, Vol 14, Iss 7, p 761 (2024)
Alternative splicing significantly enhances the diversity of the G protein-coupled receptor (GPCR) family, including the histamine H3 receptor (H3R). This post-transcriptional modification generates multiple H3R isoforms with potentially distinct pha
Externí odkaz:
https://doaj.org/article/538c618ab9414ac199dcb4a006cfb741
Publikováno v:
International Journal of Molecular Sciences, Vol 25, Iss 9, p 5018 (2024)
NanoLuc-mediated bioluminescence resonance energy transfer (NanoBRET) has gained popularity for its ability to homogenously measure ligand binding to G protein-coupled receptors (GPCRs), including the subfamily of chemokine receptors. These receptors
Externí odkaz:
https://doaj.org/article/1e5af73ed9b3428f8b38e307d087a50a
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:
Georgi K Kanev, Yaran Zhang, Albert J Kooistra, Andreas Bender, Rob Leurs, David Bailey, Thomas Würdinger, Chris de Graaf, Iwan J P de Esch, Bart A Westerman
Publikováno v:
PLoS Computational Biology, Vol 19, Iss 9, p e1011301 (2023)
Many therapies in clinical trials are based on single drug-single target relationships. To further extend this concept to multi-target approaches using multi-targeted drugs, we developed a machine learning pipeline to unravel the target landscape of
Externí odkaz:
https://doaj.org/article/3875d0fdcc1341ac8c4a8184e67a02c7
Autor:
Yang Zheng, Joachim Müller, Stefan Kunz, Marco Siderius, Louis Maes, Guy Caljon, Norbert Müller, Andrew Hemphill, Geert Jan Sterk, Rob Leurs
Publikováno v:
International Journal for Parasitology: Drugs and Drug Resistance, Vol 19, Iss , Pp 47-55 (2022)
As there is a continuous need for novel anti-infectives, the present study aimed to fuse two modes of action into a novel 3-nitroimidazo[1,2-b]pyridazine scaffold to improve antiparasitic efficacy. For this purpose, we combined known structural eleme
Externí odkaz:
https://doaj.org/article/71ceaef05ad240feb9f42da5d282b02b
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
Publikováno v:
Molecules, Vol 28, Iss 13, p 4939 (2023)
Malaria continues to pose a significant health threat, causing thousands of deaths each year. The limited availability of vaccines and medications, combined with the emergence of drug resistance, further complicates the fight against this disease. In
Externí odkaz:
https://doaj.org/article/affb4457868d42f1a3c374913a0413f2
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