Receptor activated solely by a synthetic ligand information
Artificial biochemical receptors only responsive to predesigned drugs
"DREADD" redirects here. Not to be confused with dread or dredd.
A receptor activated solely by a synthetic ligand (RASSL) or designer receptor exclusively activated by designer drugs (DREADD), is a class of artificially engineered protein receptors used in the field of chemogenetics which are selectively activated by certain ligands.[1] They are used in biomedical research, in particular in neuroscience to manipulate the activity of neurons.[2]
Originally differentiated by the approach used to engineer them, RASSLs and DREADDs are often used interchangeably now to represent an engineered receptor-ligand system.[3] These systems typically utilize G protein-coupled receptors (GPCR) engineered to respond exclusively to synthetic ligands, like clozapine N-oxide (CNO),[4] and not to endogenous ligands. Several types of these receptors exists, derived from muscarinic or κ-opioid receptors.[1]
^Campbell, Erin J.; Marchant, Nathan J. (April 2018). "The use of chemogenetics in behavioural neuroscience: receptor variants, targeting approaches and caveats". British Journal of Pharmacology. 175 (7): 994–1003. doi:10.1111/bph.14146. ISSN 1476-5381. PMC 5843707. PMID 29338070.
^Armbruster BN, Li X, Pausch MH, Herlitze S, Roth BL (March 2007). "Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand". Proceedings of the National Academy of Sciences of the United States of America. 104 (12): 5163–8. Bibcode:2007PNAS..104.5163A. doi:10.1073/pnas.0700293104. PMC 1829280. PMID 17360345.
and 26 Related for: Receptor activated solely by a synthetic ligand information
Dreadlocks, a hairstyle also known as dreads Anti Dread, Polish punk rock band Dred (disambiguation) Dredd (disambiguation) Receptoractivatedsolelybya synthetic...
in a preclinical model of drug-resistant epilepsy, where seizures arise from a discrete part of the brain. Receptoractivatedsolelybyasynthetic ligand...
SEGRAMs achieve their selectivity by triggering only a subset the glucocorticoid receptor mechanisms of action. Synthetic steroids with SEGRA-like properties...
developing receptorsactivatedsolelybyasyntheticligand (DREADDs), a chemogenetic platform used to direct selective, dose-dependent activation of a specific...
that angiotensin IV interacts with the HGF system through the c-Met receptor. Synthetic small molecule analogues of angiotensin IV with the ability to penetrate...
form concentrating platforms after ligand binding activation for individual receptors. Lipid rafts have been found by researchers to be involved in many...
tazarotene, which is a treatment for psoriasis and acne, and in the preparation of SIB-1508Y, also known as Altinicline, a nicotinic receptor agonist. The alkynylation...
serotonin as the endogenous ligand and of a broad range of pharmaceutical and psychedelic drugs. Except for the 5-HT3 receptor, aligand-gated ion channel, all...
Gabapentinoids, also known as α2δ ligands, are a class of drugs that are derivatives of the inhibitory neurotransmitter gamma-Aminobutyric acid (GABA)...
brain to enter a protective cycle, useful in preventing damage during ischemic shock. Synthetic thyroxine was first successfully produced by Charles Robert...
were based on a general mathematical model that describes the interaction between a polyvalent disordered ligand and a single receptor site It was later...
relatively small quantity can cause overdose. Fentanyl works byactivating μ-opioid receptors. Fentanyl is sold under the brand names Actiq, Duragesic and...
undergo metabolization via phosphorylation to become activated. Antisense oligonucleotides (ASO): synthetic oligonucleotides have been used in the treatment...
Harrison EB, French JA (2015). "Genetic diversity in oxytocin ligands and receptors in New World monkeys". PLOS ONE. 10 (5): e0125775. Bibcode:2015PLoSO...
sialyl-Lewis X, sialyl-Lewis A, and possible unknown ligands to adhesion of human urothelial cancer cells to activated endothelium". Urologia Internationalis...
stimulating receptorligands. aAPCs loaded with cytokines have been found to stimulate T-cells to a higher degree than particles containing solely costimulatory...
Pregabalin is a gabapentinoid and acts by inhibiting certain calcium channels. Specifically it is aligand of the auxiliary α2δ subunit site of certain...
paracetamol exerts an anticonvulsant effect byactivation of the TRPV1 receptors and a decrease in neuronal excitability by hyperpolarization of neurons. The exact...
opioid receptors and their endogenous ligands have been the subject of intensive activity in association studies. These studies test broadly for a number...
estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. It is asynthetic and nonsteroidal estrogen of the stilbestrol...
structures attract ATR and eventually activates the checkpoint pathway. However, activation of Chk1 is not solely dependent on ATR, intermediate proteins...
causing a conformational change that results in its activation through an increase in the flexibility of its reactive site loop. The activated AT then...
and uracil, thiamine (vitamin B1) and alloxan. It is also found in many synthetic compounds such as barbiturates and the HIV drug zidovudine. Although pyrimidine...
Global Information