allosteric

1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity adipogenesis effects by suppressing obesity-related transcription through a feedback mechanism that regulates the expression of adiponectin, adipoR1, adipoR2, and AMPK. 3. Prunetin and biochanin A are potent reducers of NF-κB and ERK activation, zonula occludens 1 tyrosine phosphorylation, and metalloproteinase-mediated shedding activity, which may account for the barrier-improving ability of these isoflavones. 4. Prunetin significantly suppresses ATP-induced mucin secretion from cultured RTSE cells; Prunetin inhibits the production of MUC5AC mucin protein induced by EGF or PMA from NCI-H292 cells; Prunetin also inhibits the expression of MUC5AC mucin gene induced by EGF or PMA from NCI-H292 cells.

20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo).

Uracil is a common naturally occurring pyrimidine found in RNA, it base pairs with adenine and is replaced by thymine in DNA. Methylation of uracil produces thymine. Uracil's use in the body is to help carry out the synthesis of many enzymes necessary for cell function through bonding with riboses and phosphates. Uracil serves as allosteric regulator and coenzyme for many important biochemical reactions.

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.

6-Methoxyflavanone (6-MeOF) is a positive allosteric modulator of the GABA response in human recombinant GABA A receptors, exhibiting antianxiety and anti-inflammatory properties, and is used to alleviate cisplatin-induced neuropathic pain.

Brevetoxin-3 (PbTx-3) is a potent allosteric activator of voltage-gated Na+ channels, exhibiting a high affinity for site 5 and inhibiting the inactivation of these channels.

24(S)-hydroxy Cholesterol (24S-OHC) is the terminal product of the cholesterol elimination pathway in neural tissues. It is an LXR agonist and a selective positive allosteric modulator of NMDARs. It can serve as a biomarker for NPD, induce cognitive decline in mice, and is useful for studying neurological diseases.

Wogonoside (Wogonin 7-O-glucuronide) acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor.

Norstictic acid is a potent, selective allosteric transcriptional regulator that exhibits anticancer, antioxidant, and antimicrobial activities.

(2S)-6-Prenylnaringenin (6-Prenylnaringenin) is an isomer of the potent phytoestrogen, 8-prenylnaringenin. (2S)-6-Prenylnaringenin is the most potent compound in the forebrain and acts as a positive allosteric modulator of GABAA at the α+β binding site.

Milbemectin is composed of 30% milbemycin A3 and 70% milbemycin A4, exhibiting acaricidal and nematocidal properties effective against adult spider mites, their eggs, and C. elegans, with IC50 values of 5.3, 41.1, and 9.5 µg/ml, respectively. It functions as an allosteric agonist of the Drosophila RDL GABA receptor, and demonstrates efficacy against the pinewood nematode, B. xylophilus, with an LC20 of 0.0781 mg/liter.