3ttz

Crystal structure of a topoisomerase ATPase inhibitorCrystal structure of a topoisomerase ATPase inhibitor

Structural highlights

3ttz is a 2 chain structure with sequence from "micrococcus_aureus"_(rosenbach_1884)_zopf_1885 "micrococcus aureus" (rosenbach 1884) zopf 1885. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Related:	3u2d, 3u2k
Gene:	gyrB ("Micrococcus aureus" (Rosenbach 1884) Zopf 1885)
Activity:	DNA topoisomerase (ATP-hydrolyzing), with EC number 5.99.1.3
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[GYRB_STAAU] DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.[HAMAP-Rule:MF_01898]

Publication Abstract from PubMed

The pyrrolamides are a new class of antibacterial agents targeting DNA gyrase, an essential enzyme across bacterial species and inhibition results in the disruption of DNA synthesis and subsequently, cell death. The optimization of biochemical activity and other drug-like properties through substitutions to the pyrrole, piperidine, and heterocycle portions of the molecule resulted in pyrrolamides with improved cellular activity and in vivo efficacy.

Pyrrolamide DNA gyrase inhibitors: Optimization of antibacterial activity and efficacy.,Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT 3rd, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, Degrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE Bioorg Med Chem Lett. 2011 Oct 12. PMID:22041057^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT 3rd, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, Degrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE. Pyrrolamide DNA gyrase inhibitors: Optimization of antibacterial activity and efficacy. Bioorg Med Chem Lett. 2011 Oct 12. PMID:22041057 doi:10.1016/j.bmcl.2011.10.010

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OCA

[1] Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT 3rd, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, Degrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE. Pyrrolamide DNA gyrase inhibitors: Optimization of antibacterial activity and efficacy. Bioorg Med Chem Lett. 2011 Oct 12. PMID:22041057 doi:10.1016/j.bmcl.2011.10.010

[1]