2ntv

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[[Image:2ntv.gif|left|200px]]
[[Image:2ntv.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2ntv |SIZE=350|CAPTION= <scene name='initialview01'>2ntv</scene>, resolution 2.100&Aring;
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The line below this paragraph, containing "STRUCTURE_2ntv", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=P1H:{(2R,3S,4R,5R)-5-[(4S)-3-(AMINOCARBONYL)-4-(2-PROPYLISONICOTINOYL)PYRIDIN-1(4H)-YL]-3,4-DIHYDROXYTETRAHYDROFURAN-2-YL}METHYL+[(2R,3S,4R,5R)-5-(6-AMINO-9H-PURIN-9-YL)-3,4-DIHYDROXYTETRAHYDROFURAN-2-YL]METHYL+DIHYDROGEN+DIPHOSPHATE'>P1H</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= inhA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=1769 Mycobacterium leprae])
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-->
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|DOMAIN=
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{{STRUCTURE_2ntv| PDB=2ntv | SCENE= }}
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|RELATEDENTRY=[[2h9i|2H9I]], [[2ntj|2NTJ]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ntv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ntv OCA], [http://www.ebi.ac.uk/pdbsum/2ntv PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ntv RCSB]</span>
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}}
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'''Mycobacterium leprae InhA bound with PTH-NAD adduct'''
'''Mycobacterium leprae InhA bound with PTH-NAD adduct'''
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[[Category: Sacchettini, J C.]]
[[Category: Sacchettini, J C.]]
[[Category: Wang, F.]]
[[Category: Wang, F.]]
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[[Category: inha]]
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[[Category: Inha]]
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[[Category: leprosy]]
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[[Category: Leprosy]]
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[[Category: prothionamide]]
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[[Category: Prothionamide]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 09:54:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:08:19 2008''
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Revision as of 06:54, 4 May 2008

Image:2ntv.gif

Template:STRUCTURE 2ntv

Mycobacterium leprae InhA bound with PTH-NAD adduct


Overview

Thioamide drugs, ethionamide (ETH) and prothionamide (PTH), are clinically effective in the treatment of Mycobacterium tuberculosis, M. leprae, and M. avium complex infections. Although generally considered second-line drugs for tuberculosis, their use has increased considerably as the number of multidrug resistant and extensively drug resistant tuberculosis cases continues to rise. Despite the widespread use of thioamide drugs to treat tuberculosis and leprosy, their precise mechanisms of action remain unknown. Using a cell-based activation method, we now have definitive evidence that both thioamides form covalent adducts with nicotinamide adenine dinucleotide (NAD) and that these adducts are tight-binding inhibitors of M. tuberculosis and M. leprae InhA. The crystal structures of the inhibited M. leprae and M. tuberculosis InhA complexes provide the molecular details of target-drug interactions. The purified ETH-NAD and PTH-NAD adducts both showed nanomolar Kis against M. tuberculosis and M. leprae InhA. Knowledge of the precise structures and mechanisms of action of these drugs provides insights into designing new drugs that can overcome drug resistance.

About this Structure

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

Reference

Mechanism of thioamide drug action against tuberculosis and leprosy., Wang F, Langley R, Gulten G, Dover LG, Besra GS, Jacobs WR Jr, Sacchettini JC, J Exp Med. 2007 Jan 22;204(1):73-8. Epub 2007 Jan 16. PMID:17227913 Page seeded by OCA on Sun May 4 09:54:19 2008

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