| Structural highlights
5d7d 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: | 5cph, 5ctu, 5ctw, 5ctx, 5cty, 5d6p, 5d6q, 5d7c, 5d7r |
| 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
Antibacterials with a novel mechanism of action offer a great opportunity to combat widespread antimicrobial resistance. Bacterial DNA Gyrase is a clinically validated target. Through physiochemical property optimization of a pyrazolopyridone hit, a novel class of GyrB inhibitors were discovered. Guided by structure-based drug design, indazole derivatives with excellent enzymatic and antibacterial activity as well as great animal efficacy were discovered.
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.,Zhang J, Yang Q, Romero JA, Cross J, Wang B, Poutsiaka KM, Epie F, Bevan D, Wu Y, Moy T, Daniel A, Chamberlain B, Carter N, Shotwell J, Arya A, Kumar V, Silverman J, Nguyen K, Metcalf CA 3rd, Ryan D, Lippa B, Dolle RE ACS Med Chem Lett. 2015 Sep 8;6(10):1080-5. doi: 10.1021/acsmedchemlett.5b00266. , eCollection 2015 Oct 8. PMID:26487916[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Zhang J, Yang Q, Romero JA, Cross J, Wang B, Poutsiaka KM, Epie F, Bevan D, Wu Y, Moy T, Daniel A, Chamberlain B, Carter N, Shotwell J, Arya A, Kumar V, Silverman J, Nguyen K, Metcalf CA 3rd, Ryan D, Lippa B, Dolle RE. Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors. ACS Med Chem Lett. 2015 Sep 8;6(10):1080-5. doi: 10.1021/acsmedchemlett.5b00266. , eCollection 2015 Oct 8. PMID:26487916 doi:http://dx.doi.org/10.1021/acsmedchemlett.5b00266
|
