Allosteric Modulation of PCSK9-LDLR Interaction: Can Structureless Loops be Drug Targets? [PDF]
, 2022 While most of the drugs available in the market are competitive inhibitors, there is a rapidly growing interest in development of allosteric drugs, particularly to inhibit protein-protein interactions (PPI) with large interaction surface area.
Suman, Chakrabarty +4 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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Allosteric Modulation of Beta1 Integrin Function Induces Lung Tissue Repair [PDF]
, 2012 The cellular cytoskeleton, adhesion receptors, extracellular matrix composition, and their spatial distribution are together fundamental in a cell's balanced mechanical sensing of its environment.
Susan McIntyre +13 more
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Computational Studies of Liver Receptor Homolog 1 in the Presence of Small Molecule Agonists: Allosteric Communication and Virtual Screening for New Potential Drug Candidates [PDF]
, 2019 Liver Receptor Homolog 1 (LRH-1) is a nuclear receptor whose dysfunction is affiliated with diseases such as diabetes and cancer. Recent investigations demonstrate that higher levels of activation and modulation of its activity can be achieved through ...
Scott, Bernard
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Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I [PDF]
, 2012 Background: Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphatic leukemia (Ph + ALL) are caused by the t(9;22), which fuses BCR to ABL resulting in deregulated ABL-tyrosine kinase activity.
Ruimi, Nili +18 more
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Mechanism of GPR84 allosteric modulation at a helix 8-proximate site. [PDF]
Sci AdvAllosteric modulators offer opportunities for pathway-selective GPCR signalling, but the structural mechanisms enabling biased allosteric modulation remain unclear.
Zhang X +14 more
europepmc +2 more sources
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
doaj +1 more source
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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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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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 +2 more
doaj +1 more source