1lwl
From Proteopedia
(New page: 200px<br /><applet load="1lwl" size="450" color="white" frame="true" align="right" spinBox="true" caption="1lwl, resolution 2.2Å" /> '''Crystal Structure of ...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1lwl.jpg|left|200px]]<br /><applet load="1lwl" size=" | + | [[Image:1lwl.jpg|left|200px]]<br /><applet load="1lwl" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1lwl, resolution 2.2Å" /> | caption="1lwl, resolution 2.2Å" /> | ||
'''Crystal Structure of Cytochrome P450-cam with a Fluorescent Probe D-8-Ad (Adamantane-1-carboxylic acid-5-dimethylamino-naphthalene-1-sulfonylamino-octyl-amide)'''<br /> | '''Crystal Structure of Cytochrome P450-cam with a Fluorescent Probe D-8-Ad (Adamantane-1-carboxylic acid-5-dimethylamino-naphthalene-1-sulfonylamino-octyl-amide)'''<br /> | ||
| + | |||
| + | ==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== | ==About this Structure== | ||
| - | 1LWL is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Pseudomonas_putida Pseudomonas putida] with HEM and DSO as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Camphor_5-monooxygenase Camphor 5-monooxygenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.15.1 1.14.15.1] Full crystallographic information is available from [http:// | + | 1LWL is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Pseudomonas_putida Pseudomonas putida] with <scene name='pdbligand=HEM:'>HEM</scene> and <scene name='pdbligand=DSO:'>DSO</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Camphor_5-monooxygenase Camphor 5-monooxygenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.15.1 1.14.15.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1LWL OCA]. |
==Reference== | ==Reference== | ||
| Line 12: | Line 15: | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Chiu, R.]] | [[Category: Chiu, R.]] | ||
| - | [[Category: Dunn, A | + | [[Category: Dunn, A R.]] |
| - | [[Category: Goodin, D | + | [[Category: Goodin, D B.]] |
| - | [[Category: Gray, H | + | [[Category: Gray, H B.]] |
| - | [[Category: Hays, A | + | [[Category: Hays, A M.]] |
| - | [[Category: Stout, C | + | [[Category: Stout, C D.]] |
| - | [[Category: Winkler, J | + | [[Category: Winkler, J R.]] |
[[Category: DSO]] | [[Category: DSO]] | ||
[[Category: HEM]] | [[Category: HEM]] | ||
| Line 29: | Line 32: | ||
[[Category: substrate-binding]] | [[Category: substrate-binding]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:49:11 2008'' |
Revision as of 11:49, 21 February 2008
|
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 with and as ligands. Active as Camphor 5-monooxygenase, with EC number 1.14.15.1 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[[Category: adamantane-1-carboxylic acid [4-(5-dimethylamino-naphthalene-1-sulfonylamino)-octyl]-amide]]
Page seeded by OCA on Thu Feb 21 13:49:11 2008
