Results 101 to 110 of about 1,168,781 (390)

Identification and Semi-Synthesis of 3-O-Protocatechuoylceanothic Acid, a Novel and Natural GPR120 Agonist †

Molecules, 2019
The identification and three step synthesis of 3-O-protocatechuoylceanothic acid, a novel and natural GPR120 agonist, is described. This ceanothane-type triterpenoid was identified from the components of Ziziphus jujuba roots and was found to be a new ...
Changjin Lim, Jung Gyu Park, Kyo Bin Kang, Young-Ger Suh   +3 more
doaj   +1 more source

Rates and Equilibria for a Photoisomerizable Antagonist at the Acetylcholine Receptor of Electrophorus Electroplaques [PDF]

, 1985
Voltage-jump and light-flash experiments have been performed on isolated Electrophorus electroplaques exposed simultaneously to nicotinic agonists and to the photoisomerizable compound 2,2'-bis-[α-(trimethylammonium)methyl]-azobenzene (2BQ).
Erlanger, Bernard F., Krouse, Mauri E., Lester, Henry A., Wassermann, Norbert H.   +3 more
core   +1 more source

The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]

, 2013
G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D., Milligan, Graeme, Ulven, Trond   +2 more
core   +1 more source

Endocytic Programming via Porous Silicon Nanoparticles Enhances TLR4 Nanoagonist Potency for Macrophage‐Mediated Immunotherapy

Advanced Functional Materials, EarlyView.
Porous silicon nanoparticles (PSiNPs) reprogram macrophage endocytosis of manganese@albumin‐based TLR4 nanoagonists, driving TRIF‐biased TLR4 signaling, eliciting robust proinflammatory responses, and potentiating macrophage‐mediated immunotherapeutic effects against NSCLC.
Xiaomei Zhang, Huiying Li, Shuodan Huang, Linxuan Zhang, Yan Gao, Ruoran Wang, Xiaoyu Wang, Hélder A. Santos, Zhenyu Yin, Bing Xia   +9 more
wiley   +1 more source

cGAS–STING, an important signaling pathway in diseases and their therapy

MedComm
Since cyclic guanosine monophosphate‐adenosine monophosphate synthase (cGAS)–stimulator of interferon genes (STING) signaling pathway was discovered in 2013, great progress has been made to elucidate the origin, function, and regulating mechanism of cGAS–
Qijie Li, Ping Wu, Qiujing Du, Ullah Hanif, Hongbo Hu, Ka Li   +5 more
doaj   +1 more source

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Nature, 2011
Adenosine receptors and β-adrenoceptors are G-protein-coupled receptors (GPCRs) that activate intracellular G proteins on binding the agonists adenosine or noradrenaline, respectively.
G. Lebon, Tony Warne, P. Edwards, K. Bennett, C. Langmead, A. Leslie, C. Tate   +6 more
semanticscholar   +1 more source

Cholesterol in mRNA‐Lipid Nanoparticles can be Replaced with the Synthetic Mycobacterial Monomycoloyl Glycerol Analogue MMG‐1

Advanced Functional Materials, EarlyView.
This study demonstrates that cholesterol in messenger RNA‐lipid nanoparticles (mRNA‐LNPs) can be completely replaced with an immunopotentiating lipid, i.e., a synthetic analogue of the C‐type lectin receptor agonist monomycoloyl glycerol (MMG‐1), without compromising physicochemical properties, in vivo transfection efficiency, and immunogenicity of the
Abhijeet G. Lokras, Saahil S. Baghel, Rune F. Jensen, Aneesh Thakur, Henrik Franzyk, Oskar Thofte, Marco Herrera‐Barrera, Madeleine Landry, Melike Ongun, Ahmad Tami, Marlene P. Thanthrige, Eva Callens, Corinne Beinat, Thomas Rades, Søren R. Paludan, Kristian Riesbeck, Ida Rosenkrands, Dennis Christensen, Gabriel K. Pedersen, Camilla Foged   +19 more
wiley   +1 more source

Ligand-Specific Regulation of the Endogenous Mu-Opioid Receptor by Chronic Treatment with Mu-Opioid Peptide Agonist [PDF]

, 2013
Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles.
Birkás, Erika, Bozó, Beáta, Cinar, Resat, Dochnal, Roberta Beatrix, Fábián, Gabriella, Kicsi, Emese Gabriella, Kékesi, Orsolya, Murányi, Marianna, Mácsai, Mónika, Szabó, Gyula, Szűcs, Mária, Tóth, Géza, Zentai, András   +12 more
core   +3 more sources

Biomaterial Strategies for Targeted Intracellular Delivery to Phagocytes

Advanced Functional Materials, EarlyView.
Phagocytes are essential to a functional immune system, and their behavior defines disease outcomes. Engineered particles offer a strategic opportunity to target phagocytes, harnessing inflammatory modulation in disease. By tuning features like size, shape, and surface, these systems can modulate immune responses and improve targeted treatment for a ...
Kaitlyn E. Woodworth, Neal I. Callaghan, Locke Davenport Huyer   +2 more
wiley   +1 more source

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source