Results 21 to 30 of about 37,458 (256)

Allosteric Modulators of Dopamine D₂ Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis

Molecules, 2022
Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in medicinal chemistry. Allosteric modulators, i.e., compounds which bind in a receptor site topologically distinct from orthosteric sites, exhibit a number of ...
Agnieszka A. Kaczor, Tomasz M. Wróbel, Damian Bartuzi   +2 more
doaj   +1 more source

Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]

Proceedings of the National Academy of Sciences, 2013
μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford, Mary J, Clark, Tom S, Wehrman, Samuel W, Gerritz, Martyn, Banks, Jonathan, O'Connell, John R, Traynor, Andrew, Alt   +7 more
openaire   +2 more sources

The Structural Basis of ATP as an Allosteric Modulator [PDF]

PLoS Computational Biology, 2014
Adenosine-5'-triphosphate (ATP) is generally regarded as a substrate for energy currency and protein modification. Recent findings uncovered the allosteric function of ATP in cellular signal transduction but little is understood about this critical behavior of ATP.
Shaoyong Lu, Wenkang Huang, Qi Wang, Qiancheng Shen, Shuai Li, Ruth Nussinov, Jian Zhang 0037   +6 more
openaire   +3 more sources

Aiming for allosterism: Evaluation of allosteric modulators of CB1 in a neuronal model [PDF]

Pharmacological Research, 2015
Cannabinoid pharmacology has proven nettlesome with issues of promiscuity a common theme among both agonists and antagonists. One recourse is to develop allosteric ligands to modulate cannabinoid receptor signaling. Cannabinoids have come late to the allosteric table.
Alex, Straiker, José, Mitjavila, Danielle, Yin, Anne, Gibson, Ken, Mackie   +4 more
openaire   +2 more sources

Membrane Heteroreceptor Complexes as Second-Order Protein Modulators: A Novel Integrative Mechanism through Allosteric Receptor–Receptor Interactions

Membranes
Bioluminescence and fluorescence resonance energy transfer (BRET and FRET) together with the proximity ligation method revealed the existence of G-protein-coupled receptors, Ionotropic and Receptor tyrosine kinase heterocomplexes, e.g., A2AR–D2R, GABAA ...
Marina Mirchandani-Duque, Malak Choucri, Juan C. Hernández-Mondragón, Minerva Crespo-Ramírez, Catalina Pérez-Olives, Luca Ferraro, Rafael Franco, Miguel Pérez de la Mora, Kjell Fuxe, Dasiel O. Borroto-Escuela   +9 more
doaj   +1 more source

Allosteric modulation of glycine receptors.

British Jounral of Pharmacology, 2011
Inhibitory (or strychnine sensitive) glycine receptors (GlyRs) are anion-selective transmitter-gated ion channels of the cys-loop superfamily, which includes among others also the inhibitory γ-aminobutyric acid receptors (GABA(A) receptors). While GABA mediates fast inhibitory neurotransmission throughout the CNS, the action of glycine as a fast ...
Yevenes GE, Zeilhofer HU
openaire   +5 more sources

Correction for Inhibition Leads to an Allosteric Co-Agonist Model for Pentobarbital Modulation and Activation of α1β3γ2L GABAA Receptors. [PDF]

PLoS ONE, 2016
BACKGROUND:Pentobarbital, like propofol and etomidate, produces important general anesthetic effects through GABAA receptors. Photolabeling also indicates that pentobarbital binds to some of the same sites where propofol and etomidate act.
Alexis M Ziemba, Stuart A Forman
doaj   +1 more source

Allosteric modulation by the fatty acid site in the glycosylated SARS-CoV-2 spike. [PDF]

Elife
The spike protein is essential to the SARS-CoV-2 virus life cycle, facilitating virus entry and mediating viral-host membrane fusion. The spike contains a fatty acid (FA) binding site between every two neighbouring receptor-binding domains.
Oliveira ASF, Kearns FL, Rosenfeld MA, Casalino L, Tulli L, Berger I, Schaffitzel C, Davidson AD, Amaro RE, Mulholland AJ.   +9 more
europepmc   +2 more sources

The antipsychotic potential of muscarinic allosteric modulation [PDF]

Drug News & Perspectives, 2010
The cholinergic hypothesis of schizophrenia emerged over 50 years ago based on clinical observations with both anticholinergics and pan-muscarinic agonists. Not until the 1990s did the cholinergic hypothesis of schizophrenia receive renewed enthusiasm based on clinical data with xanomeline, a muscarinic acetylcholine receptor M(1)/M(4)-preferring ...
Thomas M, Bridges, Evan P, LeBois, Corey R, Hopkins, Michael R, Wood, Carrie K, Jones, P Jeffrey, Conn, Craig W, Lindsley   +6 more
openaire   +2 more sources

Review on allosteric modulators of dopamine receptors so far

Health Science Reports
Background Contemporary research is predominantly directed towards allosteric modulators, a class of compounds designed to interact with specific sites distinct from the orthosteric site on G protein‐coupled receptors.
Fentaw Girmaw
doaj   +1 more source