Results 11 to 20 of about 61,419 (246)

Regulation of CXCR4 function by S1P1 through heteromerization [PDF]

Cell Communication and Signaling
Background The trafficking of immune cells between lymphoid organs and circulation depends on gradients of CXCL12 and sphingosine-1-phosphate (S1P), mediated through their cognate receptors C-X-C chemokine receptor type 4 (CXCR4) and S1P receptor type 1 (
Hyun-Tae Kim, Jae-Yeon Jeong, Won-Ki Huh
doaj   +2 more sources

Exploiting the Unique Properties of Lanthanide Complexes as FRET Probes: from Quantitation to Protein Dynamics

Analysis &Sensing, Volume 3, Issue 1, January 2023., 2023
Lanthanide complexes are ideal donors for FRET (Förster resonance energy transfer) assays with a variety of applications from easy‐to‐use quantitation of proteins to sophisticated experiments giving real‐time information on the movement of proteins. This Review article introduces the principles of using such assays before surveying the full scope of ...
Simon Wheeler, Stephen J. Butler
wiley   +1 more source

SAR exploration of the non‐imidazole histamine H3 receptor ligand ZEL‐H16 reveals potent inverse agonism

Archiv der Pharmazie, Volume 356, Issue 1, January 2023., 2023
ZEL‐H16 (1) has been disclosed to be a high‐affinity non‐imidazole H3R (partial) agonist. However, it was found that 1 acts as an inverse agonist for Gαi in various assays. Concise structure–activity relationship studies, molecular pharmacology, and docking were used to shed more light on the properties of 1.
Gábor Wágner, Tamara A. M. Mocking, Xiaoyuan Ma, Inna Slynko, Daniel Da Costa Pereira, Robin Breeuwer, Niek J. N. Rood, Cas van der Horst, Henry F. Vischer, Chris de Graaf, Iwan J. P. de Esch, Maikel Wijtmans, Rob Leurs   +12 more
wiley   +1 more source

The Chemerin Receptor CMKLR1 Requires Full‐Length Chemerin for High Affinity in Contrast to GPR1 as Demonstrated by a New Nanoluciferase‐Based Binding Assay

ChemMedChem, Volume 17, Issue 23, December 5, 2022., 2022
The adipokine chemerin and the short peptide agonist chemerin‐9 activate two GPCRs: CMKLR1 and GPR1. Here, we established a nanoluciferase based binding assay to analyze differences in ligand binding. For GPR1, both ligands show high affinity and comparable binding.
Anne Sophie Czerniak, Kevin Kretschmer, Tina Weiß, Annette G. Beck‐Sickinger   +3 more
wiley   +1 more source

ACE2 interaction with cytoplasmic PDZ protein enhances SARS-CoV-2 invasion

iScience, 2021
Summary: SARS-CoV-2 is responsible for the global COVID-19 pandemic. Angiotensin converting enzyme 2 (ACE2) is the membrane-delimited receptor for SARS-CoV-2.
Qiangmin Zhang, Julia Gefter, W. Bruce Sneddon, Tatyana Mamonova, Peter A. Friedman   +4 more
doaj  

Precision-engineered Peptide and Protein Analogs: Establishing a New Discovery Platform for Potent GPCR Modulators

CHIMIA, 2021
Numerous members of the human G protein-coupled receptor (GPCR) superfamily are receptors of therapeutic interest. GPCRs are considered to be highly tractable for drug discovery, representing the targets of approximately one-third of currently licensed ...
Kalyan Bharati Akondi, Marianne Paolini-Bertrand, Oliver Hartley   +2 more
doaj   +1 more source

Role of eIF4A1 in triple‐negative breast cancer stem‐like cell‐mediated drug resistance

Cancer Reports, Volume 5, Issue 12, December 2022., 2022
Abstract In cap‐dependent translation, the eukaryotic translation initiation factor 4A (eIF4A1) is an mRNA helicase is involved in unwinding of the secondary structure, such as the stem‐loops, at the 5′‐leader regions of the key oncogenic mRNAs. This facilitates ribosomal scanning and translation of the oncogenic mRNAs.
Dayanidhi Raman, Amit K. Tiwari
wiley   +1 more source

Structure and evolution of neuronal wiring receptors and ligands

Developmental Dynamics, Volume 252, Issue 1, Page 27-60, January 2023., 2023
Abstract One of the fundamental properties of a neuronal circuit is the map of its connections. The cellular and developmental processes that allow for the growth of axons and dendrites, selection of synaptic targets, and formation of functional synapses use neuronal surface receptors and their interactions with other surface receptors, secreted ...
Elena Cortés, Joseph S. Pak, Engin Özkan   +2 more
wiley   +1 more source

Contribution to the Discovery of a Novel Medicine for a Neuromuscular Disease and of other Promising Molecules for the Treatment of Neurodevelopmental and Neurodegenerative Diseases

CHIMIA, 2021
Nervous system disorders affect millions of people around the world, through a very broad range of diseases. Here we describe our contribution to find a treatment for patients suffering from three of those diseases.
Hasane Ratni
doaj   +1 more source

Functional consequences of brain exposure to saturated fatty acids: From energy metabolism and insulin resistance to neuronal damage

Endocrinology, Diabetes &Metabolism, Volume 6, Issue 1, January 2023., 2023
Saturated fatty acids induce insulin resistance in neurons. Neuronal metabolism of palmitic acid alters mitochondrial function. Abstract Introduction Saturated fatty acids (FAs) are the main component of high‐fat diets (HFDs), and high consumption has been associated with the development of insulin resistance, endoplasmic reticulum stress and ...
Karina Sánchez‐Alegría, Clorinda Arias   +1 more
wiley   +1 more source