OCA at 07:15, 11 March 2020

OCA — Wed, 11 Mar 2020 07:15:01 GMT

←Older revision		Revision as of 07:15, 11 March 2020
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-	'''Unreleased structure'''

-	~~The entry~~ 6kgh is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Crystal structure of Penicillin binding protein 3 (PBP3) from Mycobacterium tuerculosis (apo-form)==
		+	<StructureSection load='6kgh' size='340' side='right'caption='[[6kgh]], [[Resolution\|resolution]] 2.11Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6kgh]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6KGH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6KGH FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6kgh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6kgh OCA], [http://pdbe.org/6kgh PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6kgh RCSB], [http://www.ebi.ac.uk/pdbsum/6kgh PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6kgh ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/PBPB_MYCTU PBPB_MYCTU]] Synthesis of cross-linked peptidoglycan from the lipid intermediates.<ref>PMID:19496931</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Because of beta-lactamase-mediated resistance, beta-lactam antibiotics were long considered ineffective drugs for tuberculosis (TB) treatment. However, some beta-lactams, including meropenem and faropenem, are being re-evaluated in patients infected with TB. Penicillin-binding protein (PBP) 3, or ftsI, is an essential transpeptidase in Mycobacterium tuberculosis (Mtb) required for cell division, and thus it is an important drug target. Structures of apo MtbPBP3 and of complexes with five beta-lactams, including meropenem and faropenem, reveal how they cause inactivation via formation of hydrolytically stable acyl-enzyme complexes. The structures reveal unique features of the antibiotic interactions, both in terms of differences in their binding to MtbPBP3 and in comparison with structures of other PBPs and serine beta-lactamases, including the tautomerization status of the carbapenem-derived acyl-enzyme complexes. The results suggest that rather than hoping PBP inhibitors developed for other infections will work against TB, work should focus on developing PBP inhibitors specialized for treating TB. SIGNIFICANCE STATEMENT: The structures of Mycobacterium tuberculosis penicillin-binding protein 3, an essential protein in M. tuberculosis, in complex with a number of widely used beta-lactam antibiotics (e.g., meropenem, aztreonam, and amoxicillin) were solved. These data provide new insights for next-generation rational approaches to design tuberculosis (TB)-specific beta-lactam or nonlactam antibiotics. This manuscript is a seminal article in the field of anti-TB drug discovery and suitable for the broad readership.

-	~~Authors~~:	+	Structures of Mycobacterium tuberculosis Penicillin-Binding Protein 3 in Complex with Five beta-Lactam Antibiotics Reveal Mechanism of Inactivation.,Lu Z, Wang H, Zhang A, Liu X, Zhou W, Yang C, Guddat L, Yang H, Schofield CJ, Rao Z Mol Pharmacol. 2020 Apr;97(4):287-294. doi: 10.1124/mol.119.118042. Epub 2020 Feb, 21. PMID:32086254<ref>PMID:32086254</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 6kgh" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Guddat, L]]
		+	[[Category: Liu, X]]
		+	[[Category: Lu, Z K]]
		+	[[Category: Rao, Z H]]
		+	[[Category: Yang, H T]]
		+	[[Category: Zhang, A L]]
		+	[[Category: Mycobacterium tuberculosis]]
		+	[[Category: Native form]]
		+	[[Category: Penicillin-binding protein]]
		+	[[Category: Transferase]]

OCA at 07:15, 30 October 2019

OCA — Wed, 30 Oct 2019 07:15:25 GMT

←Older revision		Revision as of 07:15, 30 October 2019
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6kgh is ON HOLD	+	The entry 6kgh is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "6kgh" [edit=sysop:move=sysop]

OCA — Wed, 17 Jul 2019 08:47:17 GMT

Protected "6kgh" [edit=sysop:move=sysop]

←Older revision

Revision as of 08:47, 17 July 2019

OCA: New page: '''Unreleased structure''' The entry 6kgh is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 17 Jul 2019 08:47:16 GMT

New page: '''Unreleased structure''' The entry 6kgh is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 6kgh is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]

6kgh - Revision history

OCA at 07:15, 11 March 2020

OCA at 07:15, 30 October 2019

OCA: Protected "6kgh" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 6kgh is ON HOLD Authors: Description: Category: Unreleased Structures