Identification of inhibitors targeting the energy-coupling factor (ECF) transporters

Autor: Eleonora Diamanti, Paulo C. T. Souza, Inda Setyawati, Spyridon Bousis, Leticia Monjas, Lotteke J.Y.M. Swier, Atanaz Shams, Aleksei Tsarenko, Weronika K. Stanek, Manuel Jäger, Siewert J. Marrink, Dirk J. Slotboom, Anna K. H. Hirsch

Publikováno v: Communications Biology, Vol 6, Iss 1, Pp 1-8 (2023)

Abstract The energy-coupling factor (ECF) transporters are a family of transmembrane proteins involved in the uptake of vitamins in a wide range of bacteria. Inhibition of the activity of these proteins could reduce the viability of pathogens that de

Externí odkaz: https://doaj.org/article/cb7fa63baaae402daad67c5aaefc6bbd

Exploration of Novel Urolithin C Derivatives as Non-Competitive Inhibitors of Liver Pyruvate Kinase

Autor: Umberto Maria Battisti, Leticia Monjas, Fady Akladios, Josipa Matic, Eric Andresen, Carolin H. Nagel, Malin Hagkvist, Liliana Håversen, Woonghee Kim, Mathias Uhlen, Jan Borén, Adil Mardinoğlu, Morten Grøtli

Publikováno v: Pharmaceuticals, Vol 16, Iss 5, p 668 (2023)

The inhibition of liver pyruvate kinase could be beneficial to halt or reverse non-alcoholic fatty liver disease (NAFLD), a progressive accumulation of fat in the liver that can lead eventually to cirrhosis. Recently, urolithin C has been reported as

Externí odkaz: https://doaj.org/article/030b7f82a2c046bcb5af2aeb60b25820

Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase

Autor: Amalyn Nain-Perez, Anders Foller Füchtbauer, Liliana Håversen, Aleksei Lulla, Chunxia Gao, Josipa Matic, Leticia Monjas, Alexandra Rodríguez, Paul Brear, Woonghee Kim, Marko Hyvönen, Jan Borén, Adil Mardinoglu, Mathias Uhlen, Morten Grøtli

Publikováno v: Nain-Perez, A, Foller Füchtbauer, A, Håversen, L, Lulla, A, Gao, C, Matic, J, Monjas, L, Rodríguez, A, Brear, P, Kim, W, Hyvönen, M, Borén, J, Mardinoglu, A, Uhlen, M & Grøtli, M 2022, ' Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase ', EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 234, 114270 . https://doi.org/10.1016/j.ejmech.2022.114270

Liver pyruvate kinase (PKL) is a major regulator of metabolic flux and ATP production during liver cell glycolysis and is considered a potential drug target for the treatment of non-alcoholic fatty liver disease (NAFLD). In this study, we report the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59629082bdb8f96a61b22bdcd8add453
https://pubmed.ncbi.nlm.nih.gov/35290845

Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents

Autor: Carlo Cassani, Maja Genheden, Peter Fodran, Johanna Kollback, Carl-Johan Wallentin, Thomas Olsson, D. G. Joakim Larsson, Leticia Monjas

Publikováno v: Beilstein Journal of Organic Chemistry
Beilstein Journal of Organic Chemistry, Vol 15, Iss 1, Pp 1468-1474 (2019)

The synthesis and antibacterial activity of two new highly truncated derivatives of the natural product abyssomicin C are reported. This work outlines the limits of structural truncation of the natural product and consequently provides insights for f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb97a4a8e205090e0875963f79ef6307
http://europepmc.org/articles/PMC6633193

Dynamic Combinatorial Chemistry to Identify Binders of ThiT, an S-Component of the Energy-Coupling Factor Transporter for Thiamine

Autor: Lotteke J Y M Swier, Anna K. H. Hirsch, Dirk Jan Slotboom, Leticia Monjas, Inda Setyawati

Publikováno v: Chemmedchem
ChemMedChem, 12(20), 1693-1696. WILEY-V C H VERLAG GMBH

We applied dynamic combinatorial chemistry (DCC) to identify ligands of ThiT, the S‐component of the energy‐coupling factor (ECF) transporter for thiamine in Lactococcus lactis. We used a pre‐equilibrated dynamic combinatorial library (DCL) and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25b9e406cfc92a1a979a5079fcadb571