2GYD

Complex of equine apoferritin with the H-diaziflurane photolabeling reagent

Summary for 2GYD

• Entry DOI: 10.2210/pdb2gyd/pdb
• Descriptor: ferritin L subunit, CADMIUM ION, 2-(1,1-DIFLUOROETHOXY)-1,1,1-TRIFLUOROETHANE, ... (4 entities in total)
• Functional Keywords: helical bundles, anesthetic, isoflurane, metal binding protein
• Biological source: Equus caballus (horse)
• Total number of polymer chains: 1
• Total formula weight: 20353.89

Authors

Loll, P.J.,Rossi, M.J.,Eckenhoff, R. (deposition date: 2006-05-09, release date: 2006-06-13, Last modification date: 2024-11-13)

Primary citation

Xi, J.,Liu, R.,Rossi, M.J.,Yang, J.,Loll, P.J.,Dailey, W.P.,Eckenhoff, R.G.
Photoactive analogues of the haloether anesthetics provide high-resolution features from low-affinity interactions.
Acs Chem.Biol., 1:377-384, 2006

PubMed Abstract: The difficulty in obtaining binding target and site information for low-affinity drugs, like the inhaled anesthetics, has limited identification of their molecular effectors. Because such information can be provided by photoactive analogues, we designed, synthesized, and characterized a novel diazirnyl haloether that closely mimics isoflurane, the most widely used clinical general anesthetic. This compound, H-diaziflurane, is a nontoxic, potent anesthetic that potentiates GABA-gated ion channels in primary cultures of hippocampal neurons. Calorimetric and structural characterizations show that H-diaziflurane binds a model anesthetic host protein with similar energetics as isoflurane and forms photoadducts with residues lining the isoflurane binding site. H-diaziflurane will be immediately useful for identifying targets and sites important for the molecular pharmacology of the inhaled haloether anesthetics.

PubMed: 17163775
DOI: 10.1021/cb600207d

Experimental method

X-RAY DIFFRACTION (1.72 Å)