Results 11 to 20 of about 4,842,588 (336)
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
Bioengineering, 2021 Extracellular nano vesicles and exosomes hold compelling evidence in intercellular communication. Exosomal intracellular signal transduction is mediated by the transfer of cargo proteins, lipids, micro (mi)RNAs, long noncoding (lnc)RNAs, small ...
Priyanka Saha +5 more
doaj +1 more source
Spatial intensity distribution analysis quantifies the extent and regulation of homodimerization of the secretin receptor [PDF]
, 2017 Previous studies have indicated that the G protein-coupled secretin receptor is present as a homo-dimer, organized through symmetrical contacts in transmembrane domain IV, and that receptor dimerization is critical for high potency signalling by secretin.
Harikumar, Kaleeckal G. +4 more
core +2 more sources
Nature Communications, 2023 The class Frizzled of G protein-coupled receptors (GPCRs), consisting of ten Frizzled (FZD1-10) paralogs and Smoothened, remains one of the most enigmatic GPCR families.
Lukas Grätz +8 more
doaj +1 more source
Structural insights into the activation of human calcium-sensing receptor
eLife, 2021 Human calcium-sensing receptor (CaSR) is a G-protein-coupled receptor that maintains Ca2+ homeostasis in serum. Here, we present the cryo-electron microscopy structures of the CaSR in the inactive and agonist+PAM bound states.
Xiaochen Chen +13 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
The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]
, 2013 The calcitonin gene-related peptide (CGRP) receptor is a complex of a calcitonin receptor-like receptor (CLR), which is a family B G-protein-coupled receptor (GPCR) and receptor activity modifying protein 1.
Alex C. Conner +13 more
core +2 more sources
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
IL-1α and TNF-α Down-Regulate CRH Receptor-2 mRNA Expression in the Mouse Heart [PDF]
, 2001 Two receptors (CRH receptor type 1 and CRH receptor type 2) have been identified for the stress-induced neuropeptide, CRH and related peptides, urocortin, and urocortin II.
Coste, Sarah C. +4 more
core +2 more sources