Results 11 to 20 of about 799,914 (365)

Communication over the network of binary switches regulates the activation of A$_{2A}$ adenosine receptor [PDF]

PLoS Comp. Biol. (2015) 11(2): e1004044, 2014
Dynamics and functions of G-protein coupled receptors (GPCRs) are accurately regulated by the type of ligands that bind to the orthosteric or allosteric binding sites. To glean the structural and dynamical origin of ligand-dependent modulation of GPCR activity, we performed total $\sim$ 5 $\mu$sec molecular dynamics simulations of A$_{2A}$ adenosine ...
Choi, Sun, Hyeon, Changbong, Lee, Yoonji
arxiv   +5 more sources

TLRs as a Promise Target Along With Immune Checkpoint Against Gastric Cancer

Frontiers in Cell and Developmental Biology, 2021
Gastric cancer (GC) is one of the most common cancers in the world, and the incidence of gastric cancer in Asia appears to increase in recent years. Although there is a lot of improvement in treatment approaches, the prognosis of GC is poor.
Lin Cui, Xiuqing Wang, Dekai Zhang
doaj   +1 more source

Identification of ligand-specific G protein-coupled receptor states and prediction of downstream efficacy via data-driven modeling

eLife, 2021
Ligand binding stabilizes different G protein-coupled receptor states via a complex allosteric process that is not completely understood. Here, we have derived free energy landscapes describing activation of the β2 adrenergic receptor bound to ligands ...
Oliver Fleetwood, Jens Carlsson, Lucie Delemotte   +2 more
doaj   +1 more source

The relationship between anti-mullerian hormone and ovarian response and fertility outcome in infertile women undergoing assisted reproductive techniques (ART) and IUI [PDF]

Majallah-i Zanān, Māmā̓ī va Nāzā̓ī-i Īrān, 2023
Introduction: Anti-Mullerian Hormone (AMH) is related to woman's age, the number of antral follicles, and the outcome of assisted reproductive techniques.
Fariba Seyedoshohadaei, Masomeh Rezaie, Khaled Rhmani, Fariba Bakhshi   +3 more
doaj   +1 more source

Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT2A and 5-HT2B serotonin receptors

Frontiers in Pharmacology, 2023
Certain 4-substituted analogs of 1-(2,5-dimethoxyphenyl)isopropylamine (2,5-DMA) are psychoactive classical hallucinogens or serotonergic psychedelic agents that function as human 5-HT2A (h5-HT2A) serotonin receptor agonists.
Prithvi Hemanth, Pallavi Nistala, Vy T. Nguyen, Jose M. Eltit, Richard A. Glennon, Małgorzata Dukat   +5 more
doaj   +1 more source

Characterization of TR‐107, a novel chemical activator of the human mitochondrial protease ClpP

Pharmacology Research & Perspectives, 2022
We recently described the identification of a new class of small‐molecule activators of the mitochondrial protease ClpP. These compounds synthesized by Madera Therapeutics showed increased potency of cancer growth inhibition over the related compound ...
Emily M. J. Fennell, Lucas J. Aponte‐Collazo, Joshua D. Wynn, Kristina Drizyte‐Miller, Elisa Leung, Yoshimi Endo Greer, Paul R. Graves, Andrew A. Iwanowicz, Hani Ashamalla, Ekhson Holmuhamedov, Henk Lang, Donald S. Karanewsky, Channing J. Der, Walid A. Houry, Stanley Lipkowitz, Edwin J. Iwanowicz, Lee M. Graves   +16 more
doaj   +1 more source

Conductance increases produced by bath application of cholinergic agonists to Electrophorus electroplaques [PDF]

, 1975
When solutions containing agonists are applied to the innervated face of an Electrophorus electroplaque, the membrane's conductance increases. The agonist-induced conductance is increased at more negative membrane potentials.
Changeux, Jean-Pierre, Lester, Henry A., Sheridan, Robert E.   +2 more
core   +7 more sources

A TNFR2-Specific TNF Fusion Protein With Improved In Vivo Activity

Frontiers in Immunology, 2022
Tumor necrosis factor (TNF) receptor-2 (TNFR2) has attracted considerable interest as a target for immunotherapy. Indeed, using oligomeric fusion proteins of single chain-encoded TNFR2-specific TNF mutants (scTNF80), expansion of regulatory T cells and ...
Juan Gamboa Vargas, Juan Gamboa Vargas, Jennifer Wagner, Haroon Shaikh, Haroon Shaikh, Isabell Lang, Juliane Medler, Mohamed Anany, Mohamed Anany, Tim Steinfatt, Josefina Peña Mosca, Josefina Peña Mosca, Stephanie Haack, Julia Dahlhoff, Maike Büttner-Herold, Carolin Graf, Estibaliz Arellano Viera, Hermann Einsele, Harald Wajant, Andreas Beilhack, Andreas Beilhack   +20 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

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