Results 41 to 50 of about 833,545 (343)

Cannabinoid receptor interacting protein suppresses agonist-driven CB1 receptor internalization and regulates receptor replenishment in an agonist-biased manner [PDF]

open access: yes, 2016
Cannabinoid receptor interacting protein 1a (CRIP1a) is a CB1 receptor (CB1R) distal C-terminus-associated protein that modulates CB1R signaling via G proteins, and CB1R down-regulation but not desensitization (Blume et al.
Bass, Caroline E.   +8 more
core   +2 more sources

Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors

open access: yesBeilstein Journal of Organic Chemistry, 2017
Continuous-flow microfluidics has shown increased applications in radiochemistry over the last decade, particularly for both pre-clinical and clinical production of fluorine-18 labeled radiotracers.
Thomas Lee Collier   +4 more
doaj   +1 more source

Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives

open access: yesFrontiers in Chemistry, 2019
Among the other members of the adhesion molecules' family, α4β1 integrin, a heterodimeric receptor, plays a crucial role in inflammatory diseases, cancer development, metastasis and stem cell mobilization or retention.
Monica Baiula   +3 more
doaj   +1 more source

Deoxyguanosine is a TLR7 agonist [PDF]

open access: yesEuropean Journal of Immunology, 2019
AbstractToll‐like receptor 7 (TLR7) is an innate immune sensor for single‐strand RNA (ssRNA). Recent structural analysis revealed that TLR7 has an additional binding site for nucleosides such as guanosine, and is activated when both guanosine and ssRNA bind.
Jan Rehwinkel   +4 more
openaire   +2 more sources

Conjecturing about Small-Molecule Agonists and Antagonists of α4β1 Integrin: From Mechanistic Insight to Potential Therapeutic Applications

open access: yesBiomedicines
Integrins are heterodimeric cell-surface receptors that regulate cell–cell adhesion and cellular functions through bidirectional signaling. On the other hand, anomalous trafficking of integrins is also implicated in severe pathologies as cancer ...
Tingting He   +4 more
doaj   +1 more source

Adenosine A1 Receptor Agonist 2-chloro-N6-cyclopentyladenosine and Hippocampal Excitability During Brain Development in Rats

open access: yesFrontiers in Pharmacology, 2019
Objective: The adenosinergic system may influence excitability in the brain. Endogenous and exogenous adenosine has anticonvulsant activity presumably by activating A1 receptors.
Petr Fabera   +11 more
doaj   +1 more source

Licraside as novel potent FXR agonist for relieving cholestasis: structure-based drug discovery and biological evaluation studies

open access: yesFrontiers in Pharmacology, 2023
Cholestasis is a common clinical disease caused by a disorder in bile acids (BAs) homeostasis, which promotes its development. The Farnesoid X receptor (FXR) plays a critical role in regulating BAs homeostasis, making it an essential target for ...
Lili Xi   +5 more
doaj   +1 more source

A covalently bound photoisomerizable agonist. Comparison with reversibly bound agonists at electrophorus electroplaques [PDF]

open access: yes, 1980
After disulphide bonds are reduced with dithiothreitol, trans-3-(alpha-bromomethyl)-3’-[alpha-(trimethylammonium)methyl]azobenzene (trans-QBr) alkylates a sulfhydryl group on receptors.
Erlanger, Bernard F.   +4 more
core   +2 more sources

Agonist binding, agonist affinity and agonist efficacy at G protein‐coupled receptors [PDF]

open access: yesBritish Journal of Pharmacology, 2008
Measurements of affinity and efficacy are fundamental for work on agonists both in drug discovery and in basic studies on receptors. In this review I wish to consider methods for measuring affinity and efficacy at G protein coupled receptors (GPCRs).
openaire   +3 more sources

Activation Pathways of Agonists, Partial Agonists and Inverse Agonist in Beta1 and Beta2 Adrenergic Receptors [PDF]

open access: yesBiophysical Journal, 2010
Modulation of cell signaling by ligands of different efficacies via G-protein coupled receptors (GPCRs), depends intrinsically on the effect of the ligand on the dynamics between the multiple conformational states of these proteins. Ligands with different efficacies can remodel the energy landscape of the receptors, thereby perturbing this ...
Supriyo Bhattacharya, Nagarajan Vaidehi
openaire   +2 more sources

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