Results 11 to 20 of about 131,252 (300)
Profiling Allosteric Modulators of CB1R with an Allosteric Fluoroprobe [PDF]
Angewandte ChemieAllosteric modulation of cannabinoid receptor type 1 (CB1R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs).
Carreira, E. +25 more
core +6 more sources
Development of allosteric modulators of GPCRs for treatment of CNS disorders [PDF]
Neurobiology of Disease, 2014 The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols +1 more
doaj +2 more sources
Allosteric Modulators of Sigma-1 Receptor: A Review [PDF]
Frontiers in Pharmacology, 2019 Allosteric modulators of sigma-1 receptor (Sig1R) are described as compounds that can increase the activity of some Sig1R ligands that compete with (+)-pentazocine, one of the classic prototypical ligands that binds to the orthosteric Sig1R binding site.
Edijs Vavers +3 more
doaj +2 more sources
Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation. The identification and development of PTH1R non-peptide allosteric modulators have obtained widespread attention.
Mengrong Li +5 more
openaire +3 more sources
Discovery of Potential GSK-3β Allosteric Modulators for Alzheimer’s Disease [PDF]
, 2023 Glycogen Synthase Kinase-3 beta (GSK-3β) is a validated target-enzyme associated with Alzheimer’s Disease (AD). Usage of allosteric inhibitors of this enzyme represents a valid and promising therapeutic strategy due to their selective and subtle ...
Alexander, Tropsha +6 more
core +2 more sources
Allosteric Modulation of Chemoattractant Receptors [PDF]
Frontiers in Immunology, 2016 Chemoattractants control selective leukocyte homing via interactions with a dedicated family of related G protein-coupled receptor (GPCR). Emerging evidence indicates that the signaling activity of these receptors, as for other GPCR, is influenced by allosteric modulators, which interact with the receptor in a binding site distinct from the binding ...
Maria Candida Cesta +3 more
openaire +3 more sources
Computational and Structural Biotechnology Journal, 2021 The rational search for allosteric modulators and the allosteric mechanisms of these modulators in the presence of mutations is a relatively unexplored field.
Olivier Sheik Amamuddy +4 more
doaj +1 more source
Frontiers in Pharmacology, 2022 Adenosine receptors (ARs) have been identified as promising therapeutic targets for countless pathological conditions, spanning from inflammatory diseases to central nervous system disorders, from cancer to metabolic diseases, from cardiovascular ...
Silvia Pasquini +5 more
doaj +1 more source
Allosteric modulation of G protein-coupled receptor signaling
Frontiers in Endocrinology, 2023 G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins, regulate a wide array of physiological processes in response to extracellular signals. Although these receptors have proven to be the most successful class of drug targets,
Siyuan Shen +6 more
doaj +1 more source
Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]
, 2013 Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter +3 more
core +2 more sources