Results 61 to 70 of about 1,298 (145)

Fluorescent ligands for dopamine D2/D3 receptors

Scientific Reports, 2020
Fluorescent ligands are versatile tools for the study of G protein-coupled receptors. Depending on the fluorophore, they can be used for a range of different applications, including fluorescence microscopy and bioluminescence or fluorescence resonance ...
Anni Allikalt, Nirupam Purkayastha, Khajidmaa Flad, Maximilian F. Schmidt, Alina Tabor, Peter Gmeiner, Harald Hübner, Dorothee Weikert   +7 more
doaj   +1 more source

tracerDB: a crowdsourced fluorescent tracer database for target engagement analysis

Nature Communications
Investigating ligand-protein complexes is essential in the areas of chemical biology and drug discovery. However, detailed information on key reagents such as fluorescent tracers and associated data for the development of widely used bioluminescence ...
Johannes Dopfer, James D. Vasta, Susanne Müller, Stefan Knapp, Matthew B. Robers, Martin P. Schwalm   +5 more
doaj   +1 more source

Agonist efficacy at the β2AR is driven by the faster association rate of the Gs protein

Frontiers in Pharmacology
IntroductionThe β2-adrenoceptor (β2AR) is a class A G protein-coupled receptor (GPCR). It is therapeutically relevant in asthma and chronic obstructive pulmonary disease (COPD), where β2AR agonists relieve bronchoconstriction.
Clare R. Harwood, Clare R. Harwood, David A. Sykes, David A. Sykes, David A. Sykes, Theo Redfern-Nichols, Owen Underwood, Colin Nicholson, Colin Nicholson, Armin N. Khoshgrudi, Armin N. Khoshgrudi, Eline J. Koers, Eline J. Koers, Graham Ladds, Graham Ladds, Stephen J. Briddon, Stephen J. Briddon, Dmitry B. Veprintsev, Dmitry B. Veprintsev, Dmitry B. Veprintsev   +19 more
doaj   +1 more source

Virtual screening and experimental validation of a METTL3-targeting peptide with in vitro antiproliferative activity against non-small cell lung cancer cells

Journal of Enzyme Inhibition and Medicinal Chemistry
The METTL3–METTL14 protein–protein interaction (PPI) plays an important role in tumour progression, and disruption of this interaction has been explored as a potential strategy. In this study, four peptides were identified from a peptide database through
Ying Dai, Hanying Wu, Yahui Shen, Fan Yang, Xiaohao Liu, Ting Zhuang   +5 more
doaj   +1 more source

Biased antagonism of a series of bicyclic CXCR2 intracellular allosteric modulators

Frontiers in Pharmacology
Targeting the human chemokine receptor (CXCR2) holds significant potential in treating inflammatory diseases and cancer. In this study, we investigate the biased properties of previously reported CXCR2 antagonists (i.e., the MVH compounds).
Brent Van Bosstraeten, Katrijn Boon, Max Van Hoof, Wim Dehaen, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Steven De Jonghe, Tom Van Loy   +8 more
doaj   +1 more source

Publication Only

HemaSphere, Volume 10, Issue S1, June 2026.
wiley   +1 more source

AI and network biology for rational polypharmacology in signaling drug design: a review

npj Precision Oncology
The complexity of disease-causing signaling networks is indicative of the failure of single-target therapeutics to work, particularly because of feedback, redundancy and activation of compensatory responses.
Xuehao Li, Zhaoqi Wu, Te Fang, Jun Li, Danyang Li, Ximeng Zhang, Ling Liu, Liming Wang   +7 more
doaj   +1 more source

Agonist-specific FPR1 conformational change prevents receptor recycling and promotes targeted protein degradation

Acta Pharmaceutica Sinica B
Recycling of internalized cell surface receptors is critical for membrane transport and receptor-mediated signaling. Formyl peptide receptor 1 (FPR1) plays important roles in host defense and inflammatory tissue injury.
Junlin Wang, Qiwen Liao, Geng Chen, Yixin Chang, Hong Nie, Jiahong Lu, Richard D. Ye   +6 more
doaj   +1 more source

ISEV2026 Abstract Book

Journal of Extracellular Vesicles, Volume 15, Issue S1, June 2026.
wiley   +1 more source

Development of a NanoBRET Screening Assay for Buruli Ulcer Drug Leads with a Novel Mode of Action

, 2022
Mycolactone A/B (MycA/B) is the compound which confers virulence to <em>Mycobacterium ulcerans</em> which causes the neglected tropical disease Buruli ulcer. Simmonds discovered that MycA/B inhibits the protein channel Sec61, which is responsible for the movement of proteins into the endoplasmic reticulum (translocation) for incorporation ...
openaire   +2 more sources