Results 41 to 50 of about 13,362 (255)

Molecular Modeling of the M3 Acetylcholine Muscarinic Receptor and Its Binding Site [PDF]

Journal of Biomedicine and Biotechnology, 2012
The present study reports the results of a combined computational and site mutagenesis study designed to provide new insights into the orthosteric binding site of the human M3 muscarinic acetylcholine receptor. For this purpose a three-dimensional structure of the receptor at atomic resolution was built by homology modeling, using the crystallographic ...
Arnau Cordomí, Arnau Cordomí, Marlet Martinez-Archundia, Juan J. Perez, Pere Garriga   +4 more
openaire   +3 more sources

Selective M3 Muscarinic Receptor Antagonist Inhibits Small-Cell Lung Carcinoma Growth in a Mouse Orthotopic Xenograft Model

Journal of Pharmacological Sciences, 2011
.: In small cell lung carcinoma (SCLC), acetylcholine (ACh) is synthesized and secreted, and it acts as an autocrine growth factor through activation of its receptors, muscarinic receptor (mAChR) and nicotinic receptor (nAChR). Alteration of tumor growth
Nozomi Ami, Kazumi Koga, Hiroshi Fushiki, Yoko Ueno, Yoshio Ogino, Hisashi Ohta   +5 more
doaj   +1 more source

Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]

, 2016
Pulmonary hypertension (PH) is a complex disease comprising a pathologic remodeling and thickening of the pulmonary vessels causing an after load on the right heart ventricle that can result in ventricular failure. Triggered by oxidative stress, episodes
Ahmed, Mohamed, Al-Abed, Yousef, Coleman, Thomas, Lakshminrusimha, Satyanarayana, Patel, Hardik, VanPatten, Sonya   +5 more
core   +2 more sources

Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists [PDF]

Proceedings of the National Academy of Sciences, 2018
Significance The development of selective antagonists for muscarinic acetylcholine receptors is challenging due to high homology in orthosteric binding sites among subtypes. Starting from a single amino acid difference in the orthosteric pockets in M2 muscarinic acetylcholine receptor (M2R) and M3R, we developed an M3R-selective antagonist ...
Inbar Fish, Amelie L. Bartuschat, Jonas Kaindl, Mary J. Clark, Sandra G. Vincent, Brian K. Shoichet, Josefa Hofmann, Xiangyu Liu, Hongtao Liu, Harald Hübner, Markus R. Heinrich, Hannelore Rampp, Roger K. Sunahara, Katrin Eitel, Brian K. Kobilka, Brian K. Kobilka, Kunio Hirata, Ashutosh Banerjee, John T. Fisher, Peter Gmeiner, Benjamin Schaake   +20 more
openaire   +5 more sources

The Cholinergic Pathways in Inflammation: A Potential Pharmacotherapeutic Target for COPD

Frontiers in Pharmacology, 2018
In COPD, the activity of the cholinergic system is increased, which is one of the reasons for the airflow limitation caused by the contraction of airway smooth muscles.
Mitsuhiro Yamada, Masakazu Ichinose
doaj   +1 more source

M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]

, 2017
Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity.
Alvarez-Curto, Elisa, Lopez-Gimenez, Juan, Milligan, Graeme   +2 more
core   +1 more source

Allosteric interactions at the M3 muscarinic acetylcholine receptor

, 2023
The extracellular loops of muscarinic acetylcholine receptors are predicted to play a role in the binding and regulation of allosteric modulators. Furthermore, the sequence of the five subtypes of muscarinic receptors shows a large degree of diversity in this region.
openaire   +4 more sources

Mir-34a-5p Mediates Cross-Talk between M2 Muscarinic Receptors and Notch-1/EGFR Pathways in U87MG Glioblastoma Cells: Implication in Cell Proliferation [PDF]

, 2018
Glioblastoma (GBM) is the most aggressive human brain tumor. The high growth potential and decreased susceptibility to apoptosis of the glioma cells is mainly dependent on genetic amplifications or mutations of oncogenic or pro-apoptotic genes ...
Bevilacqua, Valeria, Caffarelli, Elisa, De Jaco, Antonella, Di Bari, Maria, Laneve, Pietro, Piovesana, Roberta, Talora, Claudio, Tata, Ada Maria, Trobiani, Laura   +8 more
core   +2 more sources

Cholinergic receptor alterations in the cerebral cortex of spinal cord injured rat

Biochemistry and Biophysics Reports, 2017
Many areas of the cerebral cortex process sensory information or coordinate motor output necessary for control of movement. Disturbances in cortical cholinergic system can affect locomotor coordination.
R. Chinthu, T.R. Anju, C.S. Paulose
doaj   +1 more source

Review article: pathogenesis and clinical manifestations of gastrointestinal involvement in systemic sclerosis. [PDF]

, 2017
BACKGROUND: Gastrointestinal tract (GIT) involvement is a common cause of debilitating symptoms in patients with systemic sclerosis (SSc). There are no disease modifying therapies for this condition and the treatment remains symptomatic, largely owing to
Abraham, Assandri, Assassi, Auluck, Bacher, Baron, Baron, Bodukam, Cavazzana, Chizzolini, Chizzolini, Ciechomska, Clark, Cohen, Colina, Crowell, Denton, Denton, Derk, Derynck, Emmanuel, Frech, Fynne, Gabrielli, Goldblatt, Gregersen, Gu, Hartleb, Heyt, Hinz, Hu, Hudson, Hung, Ingraham, Jimenez, Johnson, Jung, Kaburaki, Kaneko, Khanna, Khanna, Koh, Krause, Kumar, Luciano, Malandrini, Manetti, Manetti, Manetti, Marie, Marie, Marie, Marie, Marie, Matucci-Cerinic, Maurer, Miao, Milette, Murray-Lyon, Nagaraja, O'Reilly, O'Reilly, Omair, Parker, Parodi, Pattanaik, Peng, Piasecki, Poelman, Radic, Raja, Raja, Raja, Rajapakse, Reynolds, Richard, Richardson, Rigamonti, Riviere, Roulis, Russell, Sakkas, Savarino, Savarino, Shawis, Singh, Singh, Sjogren, Skare, Solis-Herruzo, Spiegel, Steen, Stern, Stumpf, Thonhofer, Thoua, Trezza, Trojanowska, Valenzuela, Varga, Veale, Vischio, Watson, Wipff, Wynn, Zheng   +105 more
core   +2 more sources