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Some of them, like benzodiazepines or alcohol, function as psychoactive drugs. [1] The site that an allosteric modulator binds to (i.e., an allosteric site) is not the same one to which an endogenous agonist of the receptor would bind (i.e., an orthosteric site). Modulators and agonists can both be called receptor ligands. [2]
Allosteric regulation of an enzyme. In the fields of biochemistry and pharmacology an allosteric regulator (or allosteric modulator) is a substance that binds to a site on an enzyme or receptor distinct from the active site, resulting in a conformational change that alters the protein's activity, either enhancing or inhibiting its function.
As for orthosteric and allosteric modulation, this describes the manner in which the ligand binds to the receptor in question: if it binds directly to the prescribed binding site of a receptor, the ligand is orthosteric in this instance; if the ligand alters the receptor by interacting with it at any place other than a binding site, allosteric ...
Binding of a ligand to a binding site on protein often triggers a change in conformation in the protein and results in altered cellular function. Hence binding site on protein are critical parts of signal transduction pathways. [10] Types of ligands include neurotransmitters, toxins, neuropeptides, and steroid hormones. [11]
Allosteric enzymes are enzymes that change their conformational ensemble upon binding of an effector (allosteric modulator) which results in an apparent change in binding affinity at a different ligand binding site. This "action at a distance" through binding of one ligand affecting the binding of another at a distinctly different site, is the ...
The action of drugs on the human body (or any other organism's body) is called pharmacodynamics, and the body's response to drugs is called pharmacokinetics. The drugs that enter an individual tend to stimulate certain receptors, ion channels, act on enzymes or transport proteins. As a result, they cause the human body to react in a specific ...
The oxytocin receptor, also known as OXTR, is a protein which functions as receptor for the hormone and neurotransmitter oxytocin. [4] [5] In humans, the oxytocin receptor is encoded by the OXTR gene [6] [7] which has been localized to human chromosome 3p25. [8] Evolutionary tree of the oxytocin, vasotocin, mesotocin and isotocin receptors and ...
DNA-binding domain's globular proteins contain eight cysteines and allow for a tetrahedral coordination of two zinc ions. This coordination makes the binding of ER to estrogen response elements possible. [14] The ligand-binding domain is a globular, three-layered structure made of 11 helixes and contains a pocket for the natural or synthetic ...