Identification of novel inhibitors of bacterial surface enzyme Staphylococcus aureus Sortase A

Chenna, Balachandra; Shinkre, Bidhan A.; King, Jason R.; Lucius, Aaron L.; Narayana, S.V.L.; Velu, Sadanandan E.

doi:10.1016/j.bmcl.2007.10.051

Cited by 46 publications

(40 citation statements)

References 35 publications

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“…55 Preliminary structureactivity studies on the lead compound resulted in the development of compounds with improved activity, such as 5 (Fig. 4), which had an IC 50 value of 58 mM.…”

Section: Synthetic Small Molecule Srta Inhibitorsmentioning

confidence: 99%

Recent progress in the development of sortase A inhibitors as novel anti-bacterial virulence agents

Guo

Cai

et al. 2015

RSC Adv.

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Sortase A (SrtA) is a membrane-associated enzyme responsible for the covalent anchoring of many virulent factors of Gram-positive bacteria onto the cell wall. It has been shown that SrtA plays a pivotal role in the pathogenic processes of bacterial infection. Additionally, SrtA is not essential for microbial growth and viability, and its inhibition does not therefore place pressure on bacteria to develop drug-resistant mechanism. As an extracellular membrane enzyme, it can more readily be targeted by drugs relevant to intracellular enzymes. SrtA is thus an excellent target for the design and development of novel anti-virulence drugs against the drug-resistant Gram-positive bacteria that have become a major worldwide health problem. A number of SrtA inhibitors have so far been identified by techniques such as the rational design of substrate mimetic inhibitors based on the structure of the enzyme and enzyme substrates, identification of novel inhibitors among natural products, the discovery and development of SrtA inhibitors via high-throughput, and in silico screening of small molecule libraries followed by structural optimization. The present article reviews the progress made recently in the development of SrtA inhibitors as new antibacterial agents using similar techniques.

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“…55 Preliminary structureactivity studies on the lead compound resulted in the development of compounds with improved activity, such as 5 (Fig. 4), which had an IC 50 value of 58 mM.…”

Section: Synthetic Small Molecule Srta Inhibitorsmentioning

confidence: 99%

Recent progress in the development of sortase A inhibitors as novel anti-bacterial virulence agents

Guo

Cai

et al. 2015

RSC Adv.

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show abstract

“…For their study, Chenna et al selected the high resolution structure of recombinant S. aureus SrtA D59 [36], and using flexible docking (FLEX software package) they fit approximately 150,000 small molecules into the enzyme active site [37]. The top scoring compounds were screened against S. aureus SrtA D59 in order to confirm the reliability of the model used and 7.4% (8 of 108 molecules) of the identified leads exhibited SrtA inhibition in vitro with IC 50 [38].…”

Section: Virtual Screeningmentioning

confidence: 99%

Sortase A: An ideal target for anti-virulence drug development

Cascioferro¹,

Totsika²,

Schillaci³

2014

Microbial Pathogenesis

160

142

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“…A dataset of 149 compounds collected from the literature [15,16,23,24]. Every compound in the data set underwent the same cell growth suppression analysis, which makes the results uniform.…”

Section: Ligand Preparationmentioning

confidence: 99%

Designing of potential inhibitors against Staphylococcus aureus sortase A: Combined analogue and structure based approach with in vitro validation

Raj

Kumar

Madhuri

et al. 2015

Journal of Molecular Graphics and Modelling

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Identification of novel inhibitors of bacterial surface enzyme Staphylococcus aureus Sortase A

Cited by 46 publications

References 35 publications

Recent progress in the development of sortase A inhibitors as novel anti-bacterial virulence agents

Recent progress in the development of sortase A inhibitors as novel anti-bacterial virulence agents

Sortase A: An ideal target for anti-virulence drug development

Designing of potential inhibitors against Staphylococcus aureus sortase A: Combined analogue and structure based approach with in vitro validation

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