Web14 mrt. 2024 · The introduction of the furan substituent at the seven positions of hexahydroimidazo(1,2a) pyridine scaffold led to п-п T-shaped interactions with the condensed ring of Trp143 and п-alkyl interactions with side-chain alkyl of Leu112. These hydrophobic interactions play key roles in the binding of neonicotinoids to the Ls-AChBP … Web13 mrt. 2008 · Neonicotinoid insecticides, which act on nicotinic acetylcholine receptors (nAChRs) in a variety of ways, have extremely low mammalian toxicity, yet the molecular basis of such actions is poorly understood. To elucidate the molecular basis for nAChR–neonicotinoid interactions, a surrogate protein, acetylcholine binding protein …
Synthesis of full-length homodimer αD-VxXXB that targets human …
Web12 jun. 2005 · Binding of α-conotoxins to AChBPs. Because AChBP from Lymnaea stagnalis (Ls-AChBP) resembles the α 7-nAChR in its sensitivity to α-bungarotoxin, we first tested α 7-selective α-Ctx ImI and ... Web11 apr. 2014 · We therefore elucidated X-ray crystal structures of the Lymnaea stagnalis acetylcholine binding protein (Ls-AChBP) and its Gln55Arg mutant, more closely resembling insect nAChRs, in complex with a nitromethylene imidacloprid analog (CH-IMI) and desnitro-imidacloprid metabolite (DN-IMI) as well as commercial neonicotinoids, imidacloprid, … clint ingle
From crystal structure of α-conotoxin GIC in complex with Ac-AChBP …
Web1 okt. 2015 · Confirmed by mutational studies, our structures suggest a unique ligand-specific role of residue H142 on the α 4 subunit. In the cocrystal structure of the mutated Ls -AChBP with the high-efficacy ligand NS3920, the corresponding histidine forms an intersubunit bridge that reinforces the ligand-mediated interactions between subunits. Web1 nov. 2024 · Acetylcholine binding proteins (AChBPs) are homologs of extracellular domains of nicotinic acetylcholine receptors (nAChRs) and serve as models for studies on nAChRs. Particularly, studies on invertebrate nAChRs that are limited due to difficulties in their heterologous expression have benefitted from the discovery of AChBPs. WebBackground: Molecular features governing α4β2 nAChRs efficacy have remained elusive.Results: Binding studies, electrophysiology, and structural data from co-crystallization with Ls-AChBP are reported for a series of α4β2 agonists.Conclusion: Direct halogen bonds and an invariant Loop-C suggest that intersubunit bridge formation … clint info