Phosphopantetheinyl transferase binding and inhibition by amidino-urea and hydroxypyrimidinethione compounds

Autor: Coralie Carivenc, Laurent Maveyraud, Claire Blanger, Stéphanie Ballereau, Coralie Roy-Camille, Minh Chau Nguyen, Yves Génisson, Christophe Guilhot, Christian Chalut, Jean-Denis Pedelacq, Lionel Mourey

Publikováno v: Scientific Reports, Vol 11, Iss 1, Pp 1-10 (2021)

Abstract Owing to their role in activating enzymes essential for bacterial viability and pathogenicity, phosphopantetheinyl transferases represent novel and attractive drug targets. In this work, we examined the inhibitory effect of the aminido-urea

Externí odkaz: https://doaj.org/article/f57ec08b40274ca4ab42e00bdf4c4481

Fragment-Based Ligand Discovery Applied to the Mycolic Acid Methyltransferase Hma (MmaA4) from Mycobacterium tuberculosis: A Crystallographic and Molecular Modelling Study

Autor: Romain Galy, Stéphanie Ballereau, Yves Génisson, Lionel Mourey, Jean-Christophe Plaquevent, Laurent Maveyraud

Publikováno v: Pharmaceuticals, Vol 14, Iss 12, p 1282 (2021)

The mycolic acid biosynthetic pathway represents a promising source of pharmacological targets in the fight against tuberculosis. In Mycobacterium tuberculosis, mycolic acids are subject to specific chemical modifications introduced by a set of eight

Externí odkaz: https://doaj.org/article/869c4c95e0134e7ba56dcb8fa892eb3e

Second-Generation Pharmacological Chaperones: Beyond Inhibitors

Autor: My Lan Tran, Yves Génisson, Stéphanie Ballereau, Cécile Dehoux

Publikováno v: Molecules, Vol 25, Iss 14, p 3145 (2020)

Protein misfolding induced by missense mutations is the source of hundreds of conformational diseases. The cell quality control may eliminate nascent misfolded proteins, such as enzymes, and a pathological loss-of-function may result from their early

Externí odkaz: https://doaj.org/article/c89e87576c754021a793fd79bcf48677

SDR enzymes oxidize specific lipidic alkynylcarbinols into cytotoxic protein-reactive species

Autor: Julien Marcoux, Etienne Joly, Pascal Demange, Patrick RA Zanon, Dymytrii Listunov, Pauline Rullière, Cécile Barthes, Céline Noirot, Jean-Baptiste Izquierdo, Alexandrine Rozié, Karen Pradines, Romain Hee, Maria Vieira de Brito, Marlène Marcellin, Remy-Felix Serre, Olivier Bouchez, Odile Burlet-Schiltz, Maria Conceição Ferreira Oliveira, Stéphanie Ballereau, Vania Bernardes-Génisson, Valérie Maraval, Patrick Calsou, Stephan M Hacker, Yves Génisson, Remi Chauvin, Sébastien Britton

Publikováno v: eLife, 11:e73913
eLife
eLife, 2022, 11, pp.e73913. ⟨10.7554/eLife.73913⟩

© 2022, Demange et al.; International audience; Hundreds of cytotoxic natural or synthetic lipidic compounds contain chiral alkynylcarbinol motifs, but the mechanism of action of those potential therapeutic agents remains unknown. Using a genetic sc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3c4c8a09bfd51db863a599d852d19b7
http://hdl.handle.net/1887/3453355

( R )‐BINOL‐6,6’‐bistriflone: Shortened Synthesis, Characterization, and Enantioselective Catalytic Applications

Autor: Omar Mouhtady, Isabelle Fabing, Christiane André-Barrès, Hafida Gaspard, Yves Génisson, Heinz Gornitzka, Nathalie Saffon-Merceron, Tessa Castellan

Publikováno v: European Journal of Organic Chemistry
European Journal of Organic Chemistry, 2021, 2021 (48), pp.6674-6681. ⟨10.1002/ejoc.202101137⟩
European Journal of Organic Chemistry, Wiley-VCH Verlag, 2021, 2021 (48), pp.6674-6681. ⟨10.1002/ejoc.202101137⟩

International audience; The title compound, characterized by X-ray crystallography, was accessed in 4 steps with 92 % ee. and 25 % yield from an O-protected (R)-BINOL precursor. This revised synthetic route relied on a chlorosulfonylation reaction, a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ea61374902952d234e39cf8b30ddf30
https://hal.science/hal-03511667