Results 21 to 30 of about 36,012 (161)

Filamentation modulates allosteric regulation of PRPS

eLife, 2022
Phosphoribosyl pyrophosphate (PRPP) is a key intermediate in the biosynthesis of purine and pyrimidine nucleotides, histidine, tryptophan, and cofactors NAD and NADP. Abnormal regulation of PRPP synthase (PRPS) is associated with human disorders, including Arts syndrome, retinal dystrophy, and gouty arthritis.
Chia-Chun Chang, Guang-Ming Lu, Huan-Huan Hu, Yilan Li, Jiale Zhong, Chen-Jun Guo, Xian Zhou, Boqi Yin, Tianyi Zhang, Ji-Long Liu   +9 more
openaire   +3 more sources

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

Allosteric Modulator Leads Hiding in Plain Site: Developing Peptide and Peptidomimetics as GPCR Allosteric Modulators [PDF]

Frontiers in Chemistry, 2021
Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug targets because they can produce fewer on-target side effects, improved selectivity, and better biological specificity (e.g., biased signaling or probe dependence) than orthosteric drugs.
Keith M. Olson, John R. Traynor, John R. Traynor, Andrew Alt, Andrew Alt   +4 more
openaire   +3 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

Current Advances in Allosteric Modulation of Muscarinic Receptors

Biomolecules, 2020
Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated from the orthosteric binding site for the endogenous neurotransmitter.
Jan Jakubik, Esam E. El-Fakahany
doaj   +1 more source

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 crosstalk in modular proteins: Function fine-tuning and drug design

Computational and Structural Biotechnology Journal, 2023
Modular proteins are regulatory proteins that carry out more than one function. These proteins upregulate or downregulate a biochemical cascade to establish homeostasis in cells.
Suman Abhishek, Waghela Deeksha, Krishnapura Ranganatha Nethravathi, Mehdi D. Davari, Eerappa Rajakumara   +4 more
doaj   +1 more source

Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

eLife, 2020
Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams, Cedric Govaerts, Kumiko Kambara, Kerry L Price, Radovan Spurny, Anant Gharpure, Els Pardon, Genevieve L Evans, Daniel Bertrand, Sarah CR Lummis, Ryan E Hibbs, Jan Steyaert, Chris Ulens   +12 more
doaj   +1 more source

Allosteric modulation of glycine receptors

British journal 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 ...
Yévenes, G E, Zeilhofer, Hanns Ulrich
openaire   +3 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