Rob Leurs
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Explore the profile of Rob Leurs including associated specialties, affiliations and a list of published articles.
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277
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4712
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Recent Articles
1.
Berenger S, Adamska J, Deflorian F, de Graaf C, Palmer C, Szpakowska M, et al.
ACS Omega
. 2025 Mar;
10(8):8675-8686.
PMID: 40060784
Photopharmacology offers the promise of optical modulation of cellular signaling in a spatially and temporally controlled fashion with light-sensitive molecules. This study presents the first small-molecule photoswitchable agonist for an...
2.
Kuhne S, Bosma R, Kooistra A, Riemens R, Stroet M, Vischer H, et al.
J Med Chem
. 2024 Dec;
68(1):448-464.
PMID: 39723903
Analysis of structure-kinetic relationships (SKR) can contribute to an improved understanding of receptor-ligand interactions. Here, fragment (4-(2-benzylphenoxy)-1-methylpiperidine) was used in different fragment growing approaches to mimic the putative binding mode...
3.
Gomez-Gonzalez P, Gupta A, Drought L, Patel A, Okombo J, van der Watt M, et al.
Sci Adv
. 2024 Dec;
10(49):eadq1383.
PMID: 39642214
Cyclic nucleotide-dependent phosphodiesterases (PDEs) play essential roles in regulating the malaria parasite life cycle, suggesting that they may be promising antimalarial drug targets. PDE inhibitors are used safely to treat...
4.
Denecke S, Malfara M, Hodges K, Holmes N, Williams A, Gallagher-Teske J, et al.
mSphere
. 2024 Sep;
9(10):e0061724.
PMID: 39315810
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 their single flagellum...
5.
Blaazer A, Singh A, Zara L, Boronat P, Bautista L, Irving S, et al.
ChemMedChem
. 2024 Aug;
19(22):e202400417.
PMID: 39193819
In search of new opportunities to develop Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitors that have selectivity over the off-target human PDE4 (hPDE4), different stages of a fragment-growing campaign were studied...
6.
McNaught-Flores D, Chen Y, Arias-Montano J, Panula P, Leurs R
Eur J Pharmacol
. 2024 Aug;
981:176870.
PMID: 39117262
The zebrafish, Danio rerio, is a widely adopted in vivo model that conserves organs such as the liver, kidney, stomach, and brain, being, therefore, suitable for studying human diseases, drug...
7.
Gao M, Ooms J, Leurs R, Vischer H
Biomolecules
. 2024 Jul;
14(7).
PMID: 39062475
Alternative splicing significantly enhances the diversity of the G protein-coupled receptor (GPCR) family, including the histamine H receptor (HR). This post-transcriptional modification generates multiple HR isoforms with potentially distinct pharmacological...
8.
Otun O, Aljamous C, Del Nero E, Arimont-Segura M, Bosma R, Zarzycka B, et al.
Proc Natl Acad Sci U S A
. 2024 Jul;
121(30):e2404000121.
PMID: 39008676
Atypical Chemokine Receptor 3 (ACKR3) belongs to the G protein-coupled receptor family but it does not signal through G proteins. The structural properties that govern the functional selectivity and the...
9.
Shi S, Zheng Y, Goulding J, Marri S, Lucarini L, Konecny B, et al.
Biochem Pharmacol
. 2024 Jun;
226:116396.
PMID: 38942089
This study introduces (S)-Opto-prop-2, a second-generation photoswitchable ligand designed for precise modulation of β-adrenoceptor (βAR). Synthesised by incorporating an azobenzene moiety with propranolol, (S)-Opto-prop-2 exhibited a high PSS (photostationary state...
10.
Adamska J, Leftheriotis S, Bosma R, Vischer H, Leurs R
Int J Mol Sci
. 2024 May;
25(9).
PMID: 38732237
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,...