RT Journal Article
T1 Epigenetic modulator UVI5008 inhibits MRSA by interfering with bacterial gyrase
A1 Franci, Gianluigi
A1 Folliero, Veronica
A1 Cammarota, Marcella
A1 Zannella, Carla
A1 Sarno, Federica
A1 Schiraldi, Chiara
A1 Rodríguez de Lera, Ángel
A1 Altucci, Lucia
A1 Galdiero, Massimiliano
K1 2302 Bioquímica
K1 2390 Química Farmacéutica
K1 2306 Química Orgánica
AB The impact of multi-drug resistant bacterial strains on human health is reaching worrisome levels. Over 2 million people are infected by resistant bacteria, and more than 700,000 people die each year because of the continuous spread of resistant strains. The development of new antibiotics and the prudent use of existing ones to prolong their lifespan require a constant effort by drug industries and healthcare workers. The re-purposing of existing drugs for use as antimicrobial agents would streamline the development of new antibacterial strategies. As part of this effort, we screened a panel of drugs previously characterized to be epigenetic modulators/pro-apoptotic/differentiative drugs. We selected a few compounds that alter Gram-positive growth. Among these, UVI5008, a derivative of the natural compound psammaplin A (Psa_A), was identified. The interaction of Psa_A with the DNA gyrase enzyme has been shown, and here, we hypothesized and confirmed the gyrase-specific activity by biochemical assays. UVI5008 exhibited growth inhibition activity against Staphylococcus aureus via structural modification of the cell wall, which was observed by SEM electron microscopy. Based on our findings, we propose UVI5008 as an alternative antibacterial compound against methicillin-resistant (Met.R) S. aureus strains
PB Scientific Reports
SN 20452322
YR 2018
FD 2018-09-03
LK http://hdl.handle.net/11093/4302
UL http://hdl.handle.net/11093/4302
LA eng
NO Scientific Reports, 8(1): 13117 (2018)
NO Ministerio de Economía | Ref. SAF2016-77620-R-FEDER
DS Investigo
RD 04-oct-2024