Results 31 to 40 of about 1,200,697 (382)

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

Functional GLP-1R antibodies identified from a synthetic GPCR-focused library demonstrate potent blood glucose control

mAbs, 2021
G protein-coupled receptors (GPCRs) are a group of seven-transmembrane receptor proteins that have proven to be successful drug targets. Antibodies are becoming an increasingly promising modality to target these receptors due to their unique properties ...
Qiang Liu, Pankaj Garg, Burcu Hasdemir, Linya Wang, Emily Tuscano, Emily Sever, Erica Keane, Ana G Lujan Hernandez, Tom Z. Yuan, Eric Kwan, Joyce Lai, Greg Szot, Sreenivasan Paruthiyil, Fumiko Axelrod, Aaron K. Sato   +14 more
doaj   +1 more source

A–C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions [PDF]

, 2018
Estrogen receptor-beta (ERβ) is a drug target for memory consolidation in postmenopausal women. Herein is reported a series of potent and selective ERβ agonists (SERBAs) with in vivo efficacy that are A–C estrogens, lacking the B and D estrogen rings ...
Donaldson, William A., Frick, Karyn M., Hanson, Alicia M., Imhoff, Andrea, Kim, Jaekyoon, Lu, Xingyun, Mackinnon, Alexander Craig, Pandey, Rajesh K., Perera, K. L. Iresha Sampathi, Sem, Daniel S., Sweeney, Noreena, Van Hart, Rochelle M., Wargolet, Adam J.   +12 more
core   +4 more sources

Impact of dextroamphetamine substitution on the use of illicit amphetamines in adults with amphetamine dependence: a study protocol for the multicentre double blind randomised controlled trial ATLAS4Dependence

BMJ Open
Introduction There is limited evidence on how to effectively treat individuals from marginalised populations with dependence on amphetamine and/or methamphetamine (collectively referred to hereafter as amphetamine dependence).
, Jörg Assmus, Kjell Arne Johansson, Nicholas Lintzeris, Fatemeh Chalabianloo, Anne Halmøy, Lars T Fadnes, Nadine Ezard, Brendan Clifford, John Fredrik Askjer, Olav Spigset, Torgeir Gilje Lid, Jon Mordal, Else-Marie Løberg, Christina Dahl Andersen, Jan Tore Daltveit, Aleksander H Erga, Kristin K Solli, Minna A K Hansen, Christian Ohldieck, Christer F Aas, Trond Aamo, Tine B Edvardsdal, Siv-Elin L Carlsen, Prayash Chaudhary, Marianne Cook Pierron, Gry I Dale, Silvana De Pirro, Karl Trygve Druckrey-Fiskaan, Zhanna Gaulen, Beate H Trettenes, Minna AK Hansen, Mette H Nordbotn, Line Holtan, Arild Knutsen, Kristin K Solli, Heidi F Kristiansen, Svanhild Mellingen, Maria K Olsvold, Solveig IS Reinertsen, Kristin Sannerud, Krista Siefried, Bente Sikveland, Morten Sommerbakk, Herman Steffensen, Jørn H Vold   +45 more
doaj   +1 more source

Targeting GLP-1 receptor trafficking to improve agonist efficacy

Nature Communications, 2018
Glucagon-like peptide-1 receptor (GLP-1R) activation promotes insulin secretion from pancreatic beta cells, causes weight loss, and is an important pharmacological target in type 2 diabetes (T2D).
B. Jones, Teresa Buenaventura, N. Kanda, Pauline Chabosseau, B. Owen, R. Scott, R. Goldin, N. Angkathunyakul, Ivan R. Corrêa Jr, D. Bosco, Paul R Johnson, L. Piemonti, P. Marchetti, A. Shapiro, B. Cochran, Aylin C. Hanyaloglu, A. Inoue, T. Tan, Guy A. Rutter, Alejandra Tomas, Stephen R. Bloom   +20 more
semanticscholar   +1 more source

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

, 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.
Choi, Sun, Hyeon, Changbong, Lee, Yoonji
core   +3 more sources

Namodenoson at the Crossroad of Metabolic Dysfunction-Associated Steatohepatitis and Hepatocellular Carcinoma

Biomedicines
Namodenoson (CF102) is a small, orally available, anti-inflammatory, and anti-cancer drug candidate currently in phase 2B trial for the treatment of metabolic dysfunction-associated steatohepatitis (MASH; formerly known as non-alcoholic steatohepatitis ...
Ohad Etzion, Avital Bareket-Samish, David Yardeni, Pnina Fishman   +3 more
doaj   +1 more source