Structural highlights
Function
3SIM1_DENAN Shows a non-competitive interaction with adrenergic and muscarinic receptors. Binds to alpha-2b (ADRA2B) (IC(50)=2.3 nM), alpha-1a (ADRA1A), alpha-1b (ADRA1B), and alpha-2c (ADRA2C) adrenergic receptors. Reversibly binds to M1 (CHRM1) muscarinic acetylcholine receptors, probably by interacting with the orthosteric site (PubMed:7778123, PubMed:12488533, PubMed:24793485). Also reveals a slightly weaker effect at M3 (CHRM3) and M4 (CHRM4) receptors (PubMed:7778123, PubMed:12488533, PubMed:24793485). The order of potency is ADRA2B>>CHRM1>ADRA1A>ADRA1B>ADRA2C/CHRM4 (PubMed:24793485).[1] [2] [3] [4]
References
- ↑ Mourier G, Dutertre S, Fruchart-Gaillard C, Menez A, Servent D. Chemical synthesis of MT1 and MT7 muscarinic toxins: critical role of Arg-34 in their interaction with M1 muscarinic receptor. Mol Pharmacol. 2003 Jan;63(1):26-35. PMID:12488533
- ↑ Nareoja K, Kukkonen JP, Rondinelli S, Toivola DM, Meriluoto J, Nasman J. Adrenoceptor activity of muscarinic toxins identified from mamba venoms. Br J Pharmacol. 2011 Sep;164(2b):538-50. doi: 10.1111/j.1476-5381.2011.01468.x. PMID:21557730 doi:https://dx.doi.org/10.1111/j.1476-5381.2011.01468.x
- ↑ Blanchet G, Collet G, Mourier G, Gilles N, Fruchart-Gaillard C, Marcon E, Servent D. Polypharmacology profiles and phylogenetic analysis of three-finger toxins from mamba venom: case of aminergic toxins. Biochimie. 2014 Aug;103:109-17. doi: 10.1016/j.biochi.2014.04.009. Epub 2014 May , 1. PMID:24793485 doi:https://dx.doi.org/10.1016/j.biochi.2014.04.009
- ↑ Kornisiuk E, Jerusalinsky D, Cervenansky C, Harvey AL. Binding of muscarinic toxins MTx1 and MTx2 from the venom of the green mamba Dendroaspis angusticeps to cloned human muscarinic cholinoceptors. Toxicon. 1995 Jan;33(1):11-8. PMID:7778123
