Results 11 to 20 of about 512,073 (249)

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

Structural Probing and Molecular Modeling of the A3 Adenosine Receptor: A Focus on Agonist Binding

Molecules, 2017
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

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

Frontiers 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, Axi Shi, Tiantian Shen, Guoxu Wang, Yuhui Wei, Jingjing Guo   +5 more
doaj   +1 more source

Immune Checkpoints as Therapeutic Targets in Autoimmunity

Frontiers in Immunology, 2018
Antibodies that block the immune checkpoint receptors PD1 and CTLA4 have revolutionized the treatment of melanoma and several other cancers, but in the process, a new class of drug side effect has emerged—immune related adverse events.
Christopher Paluch, Christopher Paluch, Ana Mafalda Santos, Ana Mafalda Santos, Consuelo Anzilotti, Consuelo Anzilotti, Richard J. Cornall, Richard J. Cornall, Simon J. Davis, Simon J. Davis   +9 more
doaj   +1 more source

Reconciling intrinsic properties of activating TNF receptors by native ligands versus synthetic agonists

Frontiers in Immunology, 2023
The extracellular domain of tumor necrosis factor receptors (TNFR) generally require assembly into a homotrimeric quaternary structure as a prerequisite for initiation of signaling via the cytoplasmic domains.
George Fromm, Suresh de Silva, Taylor H. Schreiber   +2 more
doaj   +1 more source

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

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