With overexpression in various cancers, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer imaging and therapy. However, the high pancreas uptake of reported GRPR-targeting radioligands limits their clinical application.
Lei Wang+9 more
doaj +1 more source
Recent advances in cancer immunotherapy: Modulation of tumor microenvironment by Toll-like receptor ligands [PDF]
Immunotherapy is considered a promising approach for cancer treatment. An important strategy for cancer immunotherapy is the use of cancer vaccines, which have been widely used for cancer treatment.
Leila Rostamizadeh+6 more
doaj +1 more source
Comparison of antimüllerian hormone levels and antral follicle count as predictor of ovarian response to controlled ovarian stimulation in good-prognosis patients at individual fertility clinics in two multicenter trials [PDF]
Objective To compare antimüllerian hormone (AMH) and antral follicle count (AFC) as predictors of ovarian response to controlled ovarian stimulation at individual fertility clinics.
Arce, Joan-Carles+2 more
core +1 more source
Functioning of the dimeric GABA(B) receptor extracellular domain revealed by glycan wedge scanning [PDF]
The G-protein-coupled receptor (GPCR) activated by the neurotransmitter GABA is made up of two subunits, GABA(B1) and GABA(B2). GABA(B1) binds agonists, whereas GABA(B2) is required for trafficking GABA(B1) to the cell surface, increasing agonist affinity to GABA(B1), and activating associated G proteins.
arxiv +1 more source
Structural Probing and Molecular Modeling of the A3 Adenosine Receptor: A Focus on Agonist Binding
Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, termed A1, A2A, A2B and A3, which belong to the G protein-coupled receptor (GPCR) superfamily.
Antonella Ciancetta, Kenneth A. Jacobson
doaj +1 more source
The effect of adding inhaled corticosteroids to tiotropium and long-acting beta(2)-agonists for chronic obstructive pulmonary disease (Review) [PDF]
BackgroundLong-acting bronchodilators comprising long-acting beta(2)-agonists and the anticholinergic agent tiotropiumare commonly used, either on their own or in combination, for managing persistent symptoms of chronic obstructive pulmonary disease ...
Aaron+32 more
core +1 more source
Differences in the signaling pathways of α1A- and α1B-adrenoceptors are related to different endosomal targeting [PDF]
Aims: To compare the constitutive and agonist-dependent endosomal trafficking of α1A- and α1B-adrenoceptors (ARs) and to establish if the internalization pattern determines the signaling pathways of each subtype.
A Hirasawa+54 more
core +7 more sources
Molecular determinants involved in the allosteric control of agonist affinity in the GABAB receptor by the GABAB2 subunit [PDF]
The gamma-aminobutyric acid type B (GABAB) receptor is an allosteric complex made of two subunits, GABAB1 (GB1) and GABAB2 (GB2). Both subunits are composed of an extracellular Venus flytrap domain (VFT) and a heptahelical domain (HD). GB1 binds GABA, and GB2 plays a major role in G-protein activation as well as in the high agonist affinity state of ...
arxiv +1 more source
Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening Model
α1-Adrenoceptors (ARs; 1A, 1B, and 1D) have been determined to perform different prominent functions in the physiological responses of the sympathetic nervous system.
Fang Xu+7 more
doaj +1 more source
Novel 2-amino-isoflavones exhibit aryl hydrocarbon receptor agonist or antagonist activity in a species/cell-specific context [PDF]
The aryl hydrocarbon receptor (AhR) mediates the induction of a variety of xenobiotic metabolism genes. Activation of the AhR occurs through binding to a group of structurally diverse compounds, most notably dioxins, which are exogenous ligands ...
BALBONI, GIANFRANCO+10 more
core +1 more source