2rcu

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(New page: 200px<br /><applet load="2rcu" size="350" color="white" frame="true" align="right" spinBox="true" caption="2rcu, resolution 1.78&Aring;" /> '''Crystal structure of...)
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==Overview==
==Overview==
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The mitochondrial membrane-associated carnitine palmitoyltransferase, system is a validated target for the treatment of type 2 diabetes, mellitus. To further facilitate structure-based drug discovery, we, determined the crystal structure of rat CPT-2 (rCPT-2) in complex with the, substrate analogue palmitoyl-aminocarnitine at 1.8A resolution., Biochemical analyses revealed a strong effect of this compound on rCPT-2, activity and stability. Using a computational approach we examined the, membrane association of rCPT-2. The protein interacts with the membrane as, a functional monomer and the calculations confirm the presence of a, membrane association domain that consists of layers of hydrophobic and, positively charged residues.
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The mitochondrial membrane-associated carnitine palmitoyltransferase system is a validated target for the treatment of type 2 diabetes mellitus. To further facilitate structure-based drug discovery, we determined the crystal structure of rat CPT-2 (rCPT-2) in complex with the substrate analogue palmitoyl-aminocarnitine at 1.8A resolution. Biochemical analyses revealed a strong effect of this compound on rCPT-2 activity and stability. Using a computational approach we examined the membrane association of rCPT-2. The protein interacts with the membrane as a functional monomer and the calculations confirm the presence of a membrane association domain that consists of layers of hydrophobic and positively charged residues.
==About this Structure==
==About this Structure==
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[[Category: Chomienne, O.]]
[[Category: Chomienne, O.]]
[[Category: Hennig, M.]]
[[Category: Hennig, M.]]
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[[Category: Rufer, A.C.]]
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[[Category: Rufer, A C.]]
[[Category: Thoma, R.]]
[[Category: Thoma, R.]]
[[Category: BOG]]
[[Category: BOG]]
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[[Category: transport]]
[[Category: transport]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:54:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:46:15 2008''

Revision as of 16:46, 21 February 2008


2rcu, resolution 1.78Å

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Crystal structure of rat carnitine palmitoyltransferase 2 in complex with r-3-(hexadecanoylamino)-4-(trimethylazaniumyl)butanoate

Overview

The mitochondrial membrane-associated carnitine palmitoyltransferase system is a validated target for the treatment of type 2 diabetes mellitus. To further facilitate structure-based drug discovery, we determined the crystal structure of rat CPT-2 (rCPT-2) in complex with the substrate analogue palmitoyl-aminocarnitine at 1.8A resolution. Biochemical analyses revealed a strong effect of this compound on rCPT-2 activity and stability. Using a computational approach we examined the membrane association of rCPT-2. The protein interacts with the membrane as a functional monomer and the calculations confirm the presence of a membrane association domain that consists of layers of hydrophobic and positively charged residues.

About this Structure

2RCU is a Single protein structure of sequence from Rattus norvegicus with and as ligands. Active as Carnitine O-palmitoyltransferase, with EC number 2.3.1.21 Full crystallographic information is available from OCA.

Reference

Carnitine palmitoyltransferase 2: analysis of membrane association and complex structure with a substrate analog., Rufer AC, Lomize A, Benz J, Chomienne O, Thoma R, Hennig M, FEBS Lett. 2007 Jul 10;581(17):3247-52. Epub 2007 Jun 8. PMID:17585909

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