Results 251 to 260 of about 702,558 (291)
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Allosteric modulation of neurotransmission
Biochemical PharmacologyThe therapeutic effects of allosteric modulators on neurotransmission are described. The two unique features of allosteric modulators are: (1) separate binding sites on proteins, and (2) the production of altered receptor conformation upon binding.
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Profiling Allosteric Modulators of CB 1 R with an Allosteric Fluoroprobe
Angewandte ChemieAbstract Allosteric modulation of cannabinoid receptor type 1 (CB 1 R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs).
Miroslav Kosar +12 more
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Allosteric Modulation of Dopamine Receptors
Mini-Reviews in Medicinal Chemistry, 2005Allosteric modulators allow for the fine-tuning of receptor responses to endogenous neurotransmitters and exogenous therapeutic agents. Different types of allosteric modulation of dopamine receptors are discussed as well as the significance of such modulation in the control of normal biological processes and in the treatment of disease.
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The concept of allosteric modulation: an overview
Drug Discovery Today: Technologies, 2013A brief historical overview of the concept of allosteric interaction is presented together with the different kinds of allosteric control recognized, in the past decades, with the model system of pentameric ligandgated ion channels. Multiple levels of allosteric modulation are identified that include sites distributed in the extracellular ligand ...
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GPCR Allosteric Modulator Discovery
2019G protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology; about one-third of all marketed drugs target members of this family. GPCR allosteric ligands hold the promise of improved subtype selectivity, spatiotemporal sensitivity, and possible biased property over typical orthosteric ligands.
Yiran, Wu +4 more
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Allosteric Modulation of Intrinsically Disordered Proteins
2019The allosteric property of globular proteins is applauded as their intrinsic ability to regulate distant sites, and this property further plays a critical role in a wide variety of cellular regulatory mechanisms. Recent advancements and studies have revealed the manifestation of allostery in intrinsically disordered proteins or regions as allosteric ...
Ashfaq Ur, Rehman +3 more
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Differential Allosteric Modulation of Cas9 Specificity
Journal of Chemical Theory and ComputationBoth RNA- and protein-based strategies have been developed to mitigate off-target cleavage by CRISPR-Cas9, yielding noncanonical guide RNAs (gRNAs) and Cas9 variants with enhanced gene-editing precision. However, the molecular mechanisms by which such PAM-distal alterations─remote from the nuclease centers─modulate Cas9 activity and specificity remain ...
Yuanhao Li +4 more
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Allosteric modulation of GPCRs: From structural insights to drug discovery
Pharmacology & Therapeutics, 2022Daniel Hilger +2 more
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Allosteric Modulation of Muscarinic Receptors by Cholesterol, Neurosteroids and Neuroactive Steroids
International Journal of Molecular Sciences, 2022Eva Kudova +2 more
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