Results 11 to 20 of about 37,458 (256)
A Structure-Based Allosteric Modulator Design Paradigm
Health Data Science, 2023 Importance: Allosteric drugs bound to topologically distal allosteric sites hold a substantial promise in modulating therapeutic targets deemed undruggable at their orthosteric sites. Traditionally, allosteric modulator discovery has predominantly relied
Mingyu Li +3 more
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Disorder driven allosteric control of protein activity
Current Research in Structural Biology, 2020 Studies of protein allostery increasingly reveal an involvement of the back and forth order-disorder transitions in this mechanism of protein activity regulation.
Wei-Ven Tee +2 more
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Pharmaceutics, 2022 The acquisition of penicillin-binding protein (PBP) 2a in resistant strains of Staphylococcus aureus allows for the continuous production of cell walls even after the inactivation of intrinsic PBPs. Thus, the discovery of novel therapeutics with enhanced
Jamiu Olaseni Aribisala, Saheed Sabiu
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Allosteric modulation of adenosine receptors [PDF]
Purinergic Signalling, 2008 Allosteric ligands for G protein-coupled receptors (GPCRs) may alter receptor conformations induced by an orthosteric ligand. These modulators can thus fine-tune classical pharmacological responses. In this review we will describe efforts to synthesize and characterize allosteric modulators for one particular GPCR subfamily, the adenosine receptors ...
Göblyös, Anikó, IJzerman, Ad P.
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Mechanism of Allosteric Modulation of the Cys-loop Receptors
Pharmaceuticals, 2010 The cys-loop receptor family is a major family of neurotransmitter-operated ion channels. They play important roles in fast synaptic transmission, controlling neuronal excitability, and brain function.
Paul Whiteaker +2 more
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Allosteric Modulators for mGlu Receptors [PDF]
Current Neuropharmacology, 2007 The metabotropic glutamate receptor family comprises eight subtypes (mGlu1-8) of G-protein coupled receptors. mGlu receptors have a large extracellular domain which acts as recognition domain for the natural agonist glutamate. In contrast to the ionotropic glutamate receptors which mediate the fast excitatory neurotransmission, mGlu receptors have been
Gasparini, F, Spooren, W
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Induced effects of sodium ions on dopaminergic G-protein coupled receptors. [PDF]
PLoS Computational Biology, 2010 G-protein coupled receptors, the largest family of proteins in the human genome, are involved in many complex signal transduction pathways, typically activated by orthosteric ligand binding and subject to allosteric modulation.
Jana Selent +3 more
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Allosteric modulation of the activity of thrombin [PDF]
Biochemical Journal, 1997 Substrates containing a P3 aspartic residue are in general cleaved poorly by thrombin. This may be partly due to an unfavourable interaction between the P3 aspartate and Glu192 in the active site of thrombin. In Protein C activation and perhaps also thrombin receptor cleavage, binding of ligands at the anion-binding exosite of thrombin seems to improve
DUFFY, Edward J. +3 more
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Modulation of Allosteric Control and Evolution of Hemoglobin
Biomolecules, 2023 Allostery arises when a ligand-induced change in shape of a binding site of a protein is coupled to a tertiary/quaternary conformational change with a consequent modulation of functional properties. The two-state allosteric model of Monod, Wyman and Changeux [J. Mol. Biol.
Maurizio Brunori, Adriana Erica Miele
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Allosteric modulation of adenosine A1 and cannabinoid 1 receptor signaling by G‐peptides
Pharmacology Research & Perspectives, 2020 While allosteric modulation of GPCR signaling has gained prominence to address the need for receptor specificity, efforts have mainly focused on allosteric sites adjacent to the orthosteric ligand‐binding pocket and lipophilic molecules that target ...
Anja M. Touma +3 more
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