Andreu Rodríguez, José Manuel

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First Name
José Manuel
Last Name
Andreu Rodríguez
Universidad Complutense de Madrid
Faculty / Institute
Personalidad, Evaluación y Psicología Clínica
Personalidad, Evaluación y Tratamiento Psicológico
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  • Publication
    Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery
    (ACS Publications, 2021-04-28) Huecas , Sonia; Araújo Bazán , Lidia; Rúiz, Federico M.; Ruiz Ávila, , Laura B.; Martínez, R.Fernando; Escobar Peña, Ana Andrea; Artola, Marta; Vázquez Villa, María Del Henar; Martín-Fontecha Corrales, María Del Mar; Fernández Tornero, Carlos; López Rodríguez, María L.; Andreu Rodríguez, José Manuel
    Bacterial resistance to antibiotics makes previously manageable infections again disabling and lethal, highlighting the need for new antibacterial strategies. In this regard, inhibition of the bacterial division process by targeting key protein FtsZ has been recognized as an attractive approach for discovering new antibiotics. Binding of small molecules to the cleft between the N-terminal guanosine triphosphate (GTP)-binding and the C-terminal subdomains allosterically impairs the FtsZ function, eventually inhibiting bacterial division. Nonetheless, the lack of appropriate chemical tools to develop a binding screen against this site has hampered the discovery of FtsZ antibacterial inhibitors. Herein, we describe the first competitive binding assay to identify FtsZ allosteric ligands interacting with the interdomain cleft, based on the use of specific high-affinity fluorescent probes. This novel assay, together with phenotypic profiling and X-ray crystallographic insights, enables the identification and characterization of FtsZ inhibitors of bacterial division aiming at the discovery of more effective antibacterials.