Definitions
from Wiktionary, Creative Commons Attribution/Share-Alike License.
- adjective biochemistry Describing the
primary ,unmodulated binding site (on areceptor ) of aligand
Etymologies
from Wiktionary, Creative Commons Attribution/Share-Alike License
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Examples
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"orthosteric" drugs and the body's natural activators (i.e. endogenous ligands), glutamate in this case.
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"orthosteric" drugs and the body's natural activators (i.e. endogenous ligands), glutamate in this case.
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"orthosteric" drugs and the body's natural activators (i.e. endogenous ligands), glutamate in this case.
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Under the agreement, Addex will regain rights to intellectual property and know-how and can pursue the program independently. www.addexpharma.com discovers and develops an emerging class of small molecule drugs, called allosteric modulators, which have the potential to be more specific and confer significant therapeutic advantages over conventional "orthosteric" small molecule or biological drugs.
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Much like flipping a light switch on, endogenous ligands or orthosteric agonists, effectively turn receptors on, sending a message to the cell to perform a specific function.
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Separately, a related orthosteric mGluR2 / 3 agonist has been shown to have efficacy in Phase II trials in patients with generalized anxiety disorder.
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Furthermore, Addex believes it can find specific drug-like allosteric modulators with more success than others have had with orthosteric drug discovery.
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Much like flipping a light switch on, endogenous ligands or orthosteric agonists, effectively turn receptors on, sending a message to the cell to perform a specific function.
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Although no drug specifically targeting mGluR2 is marketed, a Phase II clinical study published in Nature Medicine in 2007 showed that an orthosteric mGluR2 / 3 agonist improved symptoms of schizophrenia with efficacy similar to a leading marketed drug for schizophrenia.
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Allosteric molecules afford modulation of receptors that is different than orthosteric drugs.
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