Results 21 to 30 of about 1,168,781 (390)

Analogs of 6-Bromohypaphorine with Increased Agonist Potency for α7 Nicotinic Receptor as Anti-Inflammatory Analgesic Agents

Marine Drugs, 2023
Hypaphorines, tryptophan derivatives, have anti-inflammatory activity, but their mechanism of action was largely unknown. Marine alkaloid L-6-bromohypaphorine with EC50 of 80 μM acts as an agonist of α7 nicotinic acetylcholine receptor (nAChR) involved ...
Igor A. Ivanov, Andrei E. Siniavin, Victor A. Palikov, Dmitry A. Senko, Irina V. Shelukhina, Lyubov A. Epifanova, Lucy O. Ojomoko, Svetlana Y. Belukhina, Nikita A. Prokopev, Mariia A. Landau, Yulia A. Palikova, Vitaly A. Kazakov, Natalia A. Borozdina, Arina V. Bervinova, Igor A. Dyachenko, Igor E. Kasheverov, Victor I. Tsetlin, Denis S. Kudryavtsev   +17 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

⁶⁸Ga-Labeled [Thz¹⁴]Bombesin(7–14) Analogs: Promising GRPR-Targeting Agonist PET Tracers with Low Pancreas Uptake

Molecules, 2023
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, Ivica Jerolim Bratanovic, Zhengxing Zhang, Hsiou-Ting Kuo, Helen Merkens, Jutta Zeisler, Chengcheng Zhang, Ruiyan Tan, François Bénard, Kuo-Shyan Lin   +9 more
doaj   +1 more source

Beta-agonist stimulation ameliorates the phenotype of spinal and bulbar muscular atrophy mice and patient-derived myotubes [PDF]

, 2017
Spinal and bulbar muscular atrophy (SBMA) is a neuromuscular disease characterized by the loss of lower motor neurons. SBMA is caused by expansions of a polyglutamine tract in the gene coding for androgen receptor (AR).
Blaauw, Bert, Borgia, Doriana, Gomes Pereira, Marcelo, Lieberman, Andrew P., Maino, Eleonora, Malena, Adriana, Marchioretti, Caterina, Milioto, Carmelo, Pegoraro, Elena, Pennuto, Maria, Pennuto, Maria, Plebani, Mario, Polanco, Maria J., Sambataro, Fabio, Sambataro, Fabio, Sorar, Gianni, Soraru', Gianni, Venturini, Roberta, Vergani, Lodovica   +18 more
core   +3 more sources

High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist

Molecules, 2021
Relaxin/insulin-like family peptide receptor 3 (RXFP3) belongs to class A G protein-coupled receptor family. RXFP3 and its endogenous ligand relaxin-3 are mainly expressed in the brain with important roles in the regulation of appetite, energy metabolism,
Guangyao Lin, Yang Feng, Xiaoqing Cai, Caihong Zhou, Lijun Shao, Yan Chen, Linhai Chen, Qing Liu, Qingtong Zhou, Ross A.D. Bathgate, Dehua Yang, Ming-Wei Wang   +11 more
doaj   +1 more source

β2 Agonists [PDF]

, 2016
History suggests β agonists, the cognate ligand of the β2 adrenoceptor, have been used as bronchodilators for around 5,000 years, and β agonists remain today the frontline treatment for asthma and chronic obstructive pulmonary disease (COPD). The β agonists used clinically today are the products of significant expenditure and over 100 year's intensive ...
Charlotte K. Billington, Ian P. Hall, Raymond B. Penn   +2 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

Cyclic nucleotide-gated channels: structural basis of ligand efficacy and allosteric modulation [PDF]

, 1997
Most working proteins, including metabolic enzymes, transcription regulators, and membrane receptors, transporters, and ion channels, share the property of allosteric coupling. The term 'allosteric' means that these proteins mediate indirect interactions
Lester, Henry A., Li, Jun, Zagotta, William N.   +2 more
core   +1 more source

Receptor modulators associated with the hypothalamus -pituitary-thyroid axis

Frontiers in Pharmacology, 2023
The hypothalamus-pituitary-thyroid (HPT) axis maintains normal metabolic balance and homeostasis in the human body through positive and negative feedback regulation.
Xianbin Cheng, Xianbin Cheng, Xianbin Cheng, Hong Zhang, Shanshan Guan, Qi Zhao, Yaming Shan, Yaming Shan   +7 more
doaj   +1 more source

Recent advances in cancer immunotherapy: Modulation of tumor microenvironment by Toll-like receptor ligands [PDF]

BioImpacts, 2022
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, Ommoleila Molavi, Mohsen Rashid, Fatemeh Ramazani, Behzad Baradaran, Afsaneh Lavasanaifar, Raymond Lai   +6 more
doaj   +1 more source