Results 21 to 30 of about 7,559,498 (434)
Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties
Journal of Chemistry, 2022 Lead optimization represents the tedious process of fine-tuning lead compounds from biologically active hits to suitable drug candidates for clinical trials.
Kato Bredael +4 more
doaj +1 more source
An Introduction to Receptors and Receptor Disorders
Experimental Biology and Medicine, 1979 SummaryIn the last decade reliable methods have been introduced to quantitate and characterize receptors for hormones and other biologically interesting ligands. Applied initially to hormone receptors on malignant cells and to androgen-resistant and insulin-resistant states, these methods have led to the identification of many disease processes where ...
J. Roth +8 more
openaire +4 more sources
Scientific Reports, 2017 The glucocorticoid receptor (GR) is a transcription factor of which the underlying gene regulatory mechanisms are complex and incompletely understood. The non-steroidal anti-inflammatory Compound A (CpdA), a selective GR modulating compound in various ...
S. J. Desmet +9 more
doaj +1 more source
Structural insights into the peptide selectivity and activation of human neuromedin U receptors
Nature Communications, 2022 Neuromedin U receptors (NMURs) are potential drug targets for obesity and inflammatory disorders. Here, the authors report structural basis for neuromedin recognition and activation mechanism of NMURs.
Chongzhao You +6 more
doaj +1 more source
Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs [PDF]
, 2016 Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands is unknown.
Godin, Antoine G. +4 more
core +1 more source
Chimeric antigen receptor T cells for sustained remissions in leukemia.
New England Journal of Medicine, 2014 BACKGROUND Relapsed acute lymphoblastic leukemia (ALL) is difficult to treat despite the availability of aggressive therapies. Chimeric antigen receptor-modified T cells targeting CD19 may overcome many limitations of conventional therapies and induce ...
S. Maude +18 more
semanticscholar +1 more source
Scientific Reports, 2017 The transcriptional activity of the glucocorticoid receptor (GR) is co-determined by its ability to recruit a vast and varying number of cofactors. We here identify Striatin-3 (STRN3) as a novel interaction partner of GR that interferes with GR’s ligand ...
Ioanna Petta +12 more
doaj +1 more source
Direct imaging of lateral movements of AMPA receptors inside synapses [PDF]
EMBO J 22, 18 (15/09/2003) 4656-65, 2007 Trafficking of AMPA receptors in and out of synapses is crucial for synaptic plasticity. Previous studies have focused on the role of endo/exocytosis processes or that of lateral diffusion of extra-synaptic receptors. We have now directly imaged AMPAR movements inside and outside synapses of live neurons using single-molecule fluorescence microscopy ...
arxiv +1 more source
Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function [PDF]
, 2006 Following inducible expression in HEK293 cells, the human orexin-1 receptor was targeted to the cell surface but became internalized following exposure to the peptide agonist orexin A.
Canals Buj, M. +4 more
core +1 more source
Cold Spring Harbor Perspectives in Biology, 2010 Of the established Ca2+-mobilizing messengers, NAADP is arguably the most tantalizing. It is the most potent, often efficacious at low nanomolar concentrations, and its receptors undergo dramatic desensitization. Recent studies have identified a new class of calcium-release channel, the two-pore channels (TPCs), as the likely targets for NAADP ...
openaire +5 more sources