Discovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand-based drug design

• Main Authors: Joana Magalhães (Author), Nina Franko (Author), Giannamaria Annunziato (Author), Martin Welch (Author), Stephen K. Dolan (Author), Agostino Bruno (Author), Andrea Mozzarelli (Author), Stefano Armao (Author), Aigars Jirgensons (Author), Marco Pieroni (Author), Gabriele Costantino (Author), Barbara Campanini (Author)
• Format: Book
• Published: Taylor & Francis Group, 2018-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Several bacteria rely on the reductive sulphur assimilation pathway, absent in mammals, to synthesise cysteine. Reduction of virulence and decrease in antibiotic resistance have already been associated with mutations on the genes that codify cysteine biosynthetic enzymes. Therefore, inhibition of cy...