We apologize for Proteopedia being slow to respond. For the past two years, a new implementation of Proteopedia has been being built. Soon, it will replace this 18-year old system. All existing content will be moved to the new system at a date that will be announced here.

2cig

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:2cig.gif|left|200px]]<br /><applet load="2cig" size="350" color="white" frame="true" align="right" spinBox="true"
+
[[Image:2cig.gif|left|200px]]
-
caption="2cig, resolution 1.90&Aring;" />
+
 
-
'''DIHYDROFOLATE REDUCTASE FROM MYCOBACTERIUM TUBERCULOSIS INHIBITED BY THE ACYCLIC 4R ISOMER OF INH-NADP A DERIVATIVE OF THE PRODRUG ISONIAZID.'''<br />
+
{{Structure
 +
|PDB= 2cig |SIZE=350|CAPTION= <scene name='initialview01'>2cig</scene>, resolution 1.90&Aring;
 +
|SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+A'>AC1</scene>
 +
|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=1DG:(4R)-ISONICOTINIC-ACETYL-NICOTINAMIDE-ADENINE+DINUCLEOTIDE'>1DG</scene> and <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>
 +
|ACTIVITY= [http://en.wikipedia.org/wiki/Dihydrofolate_reductase Dihydrofolate reductase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.5.1.3 1.5.1.3]
 +
|GENE=
 +
}}
 +
 
 +
'''DIHYDROFOLATE REDUCTASE FROM MYCOBACTERIUM TUBERCULOSIS INHIBITED BY THE ACYCLIC 4R ISOMER OF INH-NADP A DERIVATIVE OF THE PRODRUG ISONIAZID.'''
 +
 
==Overview==
==Overview==
Line 7: Line 16:
==About this Structure==
==About this Structure==
-
2CIG is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mycobacterium_tuberculosis Mycobacterium tuberculosis] with <scene name='pdbligand=SO4:'>SO4</scene>, <scene name='pdbligand=1DG:'>1DG</scene> and <scene name='pdbligand=GOL:'>GOL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Dihydrofolate_reductase Dihydrofolate reductase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.5.1.3 1.5.1.3] Known structural/functional Site: <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2CIG OCA].
+
2CIG is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Mycobacterium_tuberculosis Mycobacterium tuberculosis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2CIG OCA].
==Reference==
==Reference==
-
Mycobacterium tuberculosis dihydrofolate reductase is a target for isoniazid., Argyrou A, Vetting MW, Aladegbami B, Blanchard JS, Nat Struct Mol Biol. 2006 May;13(5):408-13. Epub 2006 Apr 30. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16648861 16648861]
+
Mycobacterium tuberculosis dihydrofolate reductase is a target for isoniazid., Argyrou A, Vetting MW, Aladegbami B, Blanchard JS, Nat Struct Mol Biol. 2006 May;13(5):408-13. Epub 2006 Apr 30. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16648861 16648861]
[[Category: Dihydrofolate reductase]]
[[Category: Dihydrofolate reductase]]
[[Category: Mycobacterium tuberculosis]]
[[Category: Mycobacterium tuberculosis]]
Line 30: Line 39:
[[Category: tuberculosis]]
[[Category: tuberculosis]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:49:00 2008''
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:15:50 2008''

Revision as of 14:15, 20 March 2008

Image:2cig.gif


PDB ID 2cig

Drag the structure with the mouse to rotate
, resolution 1.90Å
Sites:
Ligands: , and
Activity: Dihydrofolate reductase, with EC number 1.5.1.3
Coordinates: save as pdb, mmCIF, xml



DIHYDROFOLATE REDUCTASE FROM MYCOBACTERIUM TUBERCULOSIS INHIBITED BY THE ACYCLIC 4R ISOMER OF INH-NADP A DERIVATIVE OF THE PRODRUG ISONIAZID.


Overview

Isoniazid is a key drug used in the treatment of tuberculosis. Isoniazid is a pro-drug, which, after activation by the katG-encoded catalase peroxidase, reacts nonenzymatically with NAD(+) and NADP(+) to generate several isonicotinoyl adducts of these pyridine nucleotides. One of these, the acyclic 4S isomer of isoniazid-NAD, targets the inhA-encoded enoyl-ACP reductase, an enzyme essential for mycolic acid biosynthesis in Mycobacterium tuberculosis. Here we show that the acyclic 4R isomer of isoniazid-NADP inhibits the M. tuberculosis dihydrofolate reductase (DHFR), an enzyme essential for nucleic acid synthesis. This biologically relevant form of the isoniazid adduct is a subnanomolar bisubstrate inhibitor of M. tuberculosis DHFR. Expression of M. tuberculosis DHFR in Mycobacterium smegmatis mc(2)155 protects cells against growth inhibition by isoniazid by sequestering the drug. Thus, M. tuberculosis DHFR is the first new target for isoniazid identified in the last decade.

About this Structure

2CIG is a Single protein structure of sequence from Mycobacterium tuberculosis. Full crystallographic information is available from OCA.

Reference

Mycobacterium tuberculosis dihydrofolate reductase is a target for isoniazid., Argyrou A, Vetting MW, Aladegbami B, Blanchard JS, Nat Struct Mol Biol. 2006 May;13(5):408-13. Epub 2006 Apr 30. PMID:16648861

Page seeded by OCA on Thu Mar 20 16:15:50 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2cig"
Personal tools