Results 31 to 40 of about 1,182,206 (391)

The β-blocker Nebivolol Is a GRK/β-arrestin Biased Agonist [PDF]

, 2013
Nebivolol, a third generation β-adrenoceptor (β-AR) antagonist (β-blocker), causes vasodilation by inducing nitric oxide (NO) production. The mechanism via which nebivolol induces NO production remains unknown, resulting in the genesis of much of the ...
Andresen, Bradley T., Bastepe, Murat, Blessing, Christopher P., Erickson, Catherine E., Gul, Rukhsana, Holowka, David, Jackson, Edwin K., Liu, Tammy, Nguyen, Jenny, Pulakat, Lakshmi   +9 more
core   +3 more sources

In Vitro and In Silico Characterization of G-Protein Coupled Receptor (GPCR) Targets of Phlorofucofuroeckol-A and Dieckol

Marine Drugs, 2021
Phlorotannins are polyphenolic compounds in marine alga, especially the brown algae. Among numerous phlorotannins, dieckol and phlorofucofuroeckol-A (PFF-A) are the major ones and despite a wider biological activity profile, knowledge of the G protein ...
Pradeep Paudel, Su Hui Seong, Se Eun Park, Jong Hoon Ryu, Hyun Ah Jung, Jae Sue Choi   +5 more
doaj   +1 more source

Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening Model

Molecules, 2014
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, Hong Chen, Xuelan He, Jingyi Xu, Bingbing Xu, Biyun Huang, Xue Liang, Mu Yuan   +7 more
doaj   +1 more source

An Enantiomer of an Oral Small Molecule TSH Receptor Agonist Exhibits Improved Pharmacologic Properties

Frontiers in Endocrinology, 2016
We are developing an orally available small molecule, allosteric TSH receptor (TSHR) agonist for follow up diagnostics of patients with thyroid cancer.
Susanne Neumann, Umesh Padia, Mary Jane Cullen, Elena Eliseeva, Eshel A Nir, Robert F Place, Sarah J Morgan, Marvin C Gershengorn   +7 more
doaj   +1 more source

Nikotinski acetilholinski receptor kot farmakološka tarča pri pljučnem raku

Acta Biologica Slovenica, 2022
Rak pljuč je zelo razširjena oblika raka z nizko stopnjo preživetja. Kajenje tobaka predstavlja glavni dejavnik tveganja za razvoj raka pljuč, saj v tobačnem dimu najdemo veliko rakotvornih snovi.
Veno Kononenko, Tadeja Bele, Sara Novak, Igor Križaj, Damjana Drobne, Tom Turk   +5 more
doaj   +1 more source

A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias [PDF]

, 2017
Free Fatty Acid Receptor 2 is a GPCR activated by short chain fatty acids produced in high levels in the lower gut by microbial fermentation of non-digestible carbohydrates.
Aoki, Junken, Bolognini, Daniele, Hansen, Anders Højgaard, Hudson, Brian D., Inoue, Asuka, Kawakami, Kouki, Kishi, Takayuki, Milligan, Graeme, Sergeev, Eugenia, Ulven, Trond   +9 more
core   +2 more sources

Beta-Adrenergic Agonists [PDF]

Pharmaceuticals, 2010
Inhaled β2-adrenoceptor (β2-AR) agonists are considered essential bronchodilator drugs in the treatment of bronchial asthma, both as symptoms-relievers and, in combination with inhaled corticosteroids, as disease-controllers. In this article, we first review the basic mechanisms by which the β2-adrenergic system contributes to the control of airway ...
Giovanni Barisione, BAROFFIO, MICHELE, CRIMI, EMANUELE, BRUSASCO, VITO   +3 more
openaire   +3 more sources

6-Bromohypaphorine from Marine Nudibranch Mollusk Hermissenda crassicornis is an Agonist of Human α7 Nicotinic Acetylcholine Receptor

Marine Drugs, 2015
6-Bromohypaphorine (6-BHP) has been isolated from the marine sponges Pachymatisma johnstoni, Aplysina sp., and the tunicate Aplidium conicum, but data on its biological activity were not available.
Igor E. Kasheverov, Irina V. Shelukhina, Denis S. Kudryavtsev, Tatyana N. Makarieva, Ekaterina N. Spirova, Alla G. Guzii, Valentin A. Stonik, Victor I. Tsetlin   +7 more
doaj   +1 more source

A simple open source bioinformatic methodology for initial exploration of GPCR ligands’ agonistic/antagonistic properties

Pharmacology Research & Perspectives, 2020
Drug development is an arduous procedure, necessitating testing the interaction of a large number of potential candidates with potential interacting (macro)molecules.
Athanasios A. Panagiotopoulos, Christina Papachristofi, Konstantina Kalyvianaki, Panagiotis Malamos, Panayiotis A. Theodoropoulos, George Notas, Theodora Calogeropoulou, Elias Castanas, Marilena Kampa   +8 more
doaj   +1 more source

A meta-analysis and systematic review of randomized controlled trials with degarelix versus gonadotropin-releasing hormone agonists for advanced prostate cancer [PDF]

, 2016
Our aim was to systematically evaluate the benefits of degarelix as antagonist versus agonists of gonadotropin-releasing hormones (GnRH) for the treatment of advanced prostate cancer (PC).
CATTARINO, SUSANNA, CIARDI, Antonio, Fasulo, Andrea, GENTILE, Vincenzo, GENTILUCCI, ALESSANDRO, INNOCENZI, MICHELE, Maggi, Martina, PETRANGELI, Elisa, PIERELLA, FEDERICO, SALCICCIA, STEFANO, SCIARRA, Alessandro   +10 more
core   +1 more source