1lwl | pdb_00001lwl
Crystal Structure of Cytochrome P450-cam with a Fluorescent Probe D-8-Ad (Adamantane-1-carboxylic acid-5-dimethylamino-naphthalene-1-sulfonylamino-octyl-amide)
Overview
We have synthesized two luminescent probes (D-4-Ad and D-8-Ad) that target cytochrome P450cam. D-4-Ad luminescence is quenched by Forster energy transfer upon binding (Kd = 0.83 muM) but is restored when the probe is displaced from the active site by camphor. In contrast, D-8-Ad (Kd approximately 0.02 muM) is not displaced from the enzyme, even in the presence of a large excess of camphor. The 2.2 A resolution crystal structure of the D-8-Ad:P450cam complex reveals extensive hydrophobic contacts between the probe and the enzyme, which result from the conformational flexibility of the B', F, and G helices. Probes with properties similar to those of D-4-Ad potentially could be useful for screening P450 inhibitors.
About this Structure
1LWL is a Single protein structure of sequence from Pseudomonas putida. Full crystallographic information is available from OCA.
Reference
Fluorescent probes for cytochrome p450 structural characterization and inhibitor screening., Dunn AR, Hays AM, Goodin DB, Stout CD, Chiu R, Winkler JR, Gray HB, J Am Chem Soc. 2002 Sep 4;124(35):10254-5. PMID:12197708 Page seeded by OCA on Sat May 3 00:22:26 2008
