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Upregulation of receptors, on the other hand, can result in super-sensitized cells, especially after repeated exposure to an antagonistic drug or prolonged absence of the ligand. Some receptor agonists may cause downregulation of their respective receptors, while most receptor antagonists temporarily upregulate their respective receptors.
Up-regulation is a process which occurs within a cell triggered by a signal (originating internal or external to the cell), which results in increased expression of one or more genes and as a result the proteins encoded by those genes. Conversely, down-regulation is a process resulting in decreased gene and corresponding protein expression.
Receptors of a particular type are linked to specific cellular biochemical pathways that correspond to the signal. While numerous receptors are found in most cells, each receptor will only bind with ligands of a particular structure. This has been analogously compared to how locks will only accept specifically shaped keys. When a ligand binds ...
Receptor mediated endocytosis is common way of turning receptors "off". Endocytic down regulation is regarded as a means for reducing receptor signaling. [41] The process involves the binding of a ligand to the receptor, which then triggers the formation of coated pits, the coated pits transform to coated vesicles and are transported to the ...
Use of nasal decongestants (e.g., oxymetazoline) for more than three days leads to tachyphylaxis of response and rebound congestion, caused by alpha-adrenergic receptor downregulation and desensitization. The mechanism may specifically include receptor internalisation and resistance to endogenous vasoconstrictors causing worsening in symptoms ...
Upregulation refers to the increase in the number of receptor sites on the membrane. Estrogen and FSH upregulate LHCGR sites in preparation for ovulation . After ovulation, the luteinized ovary maintains LHCGR s that allow activation in case there is an implantation.
The P2X 4 receptor has been linked to neuropathic pain mediated by microglia in vitro and in vivo. [30] [31] P2X 4 receptors are upregulated following injury. [32] This upregulation allows for increased activation of p38 mitogen-activated protein kinases, thereby increasing the release of brain-derived neurotrophic factor from microglia. [33]
upregulation, activation, or promotion – increase the rate of gene transcription downregulation , repression , or suppression – decrease the rate of gene transcription coactivator – a protein (or a small molecule) that works with transcription factors to increase the rate of gene transcription