Exploring the Antitubercular Activity of Anthranilic Acid Derivatives: From MabA (FabG1) Inhibition to Intrabacterial Acidification

Autor: Léo Faïon, Kamel Djaout, Catalin Pintiala, Catherine Piveteau, Florence Leroux, Alexandre Biela, Stéphanie Slupek, Rudy Antoine, Monika Záhorszká, Francois-Xavier Cantrelle, Xavier Hanoulle, Jana Korduláková, Benoit Deprez, Nicolas Willand, Alain R. Baulard, Marion Flipo

Publikováno v: Pharmaceuticals, Vol 16, Iss 3, p 335 (2023)

Mycobacterium tuberculosis, the pathogen that causes tuberculosis, is responsible for the death of 1.5 million people each year and the number of bacteria resistant to the standard regimen is constantly increasing. This highlights the need to discove

Externí odkaz: https://doaj.org/article/8f8af7ff2c8049dca93bfab59dd0da06

Identification of a novel class of ω,E,E-farnesyl diphosphate synthase from Mycobacterium tuberculosis

Autor: Rakesh K. Dhiman, Mark C. Schulbach, Sebabrata Mahapatra, Alain R. Baulard, Varalakshmi Vissa, Patrick J. Brennan, Dean C. Crick

Publikováno v: Journal of Lipid Research, Vol 45, Iss 6, Pp 1140-1147 (2004)

We have identified an ω,E,E-farnesyl diphosphate (ω,E,E-FPP) synthase, encoded by the open reading frame Rv3398c, from Mycobacterium tuberculosis that is unique among reported FPP synthases in that it does not contain the type I (eukaryotic) or the

Externí odkaz: https://doaj.org/article/206f8398d11c41a891f794692d28a480

Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening

Autor: Martin Moune, Florence Leroux, Léo Faïon, Abdalkarim Tanina, Alexandre Biela, Nicolas Willand, Kevin Bourbiaux, Francois-Xavier Cantrelle, Alain R. Baulard, Laurent Kremer, Catalin Pintiala, Benoit Deprez, Kamel Djaout, René Wintjens, Adrien Herledan, Marion Flipo, Mickaël Blaise, Rosangela Frita, Alexandre Vandeputte, Catherine Piveteau, Xavier Hanoulle

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2020, 200, pp.112440. ⟨10.1016/j.ejmech.2020.112440⟩
European Journal of Medicinal Chemistry, 2020, 200, pp.112440. ⟨10.1016/j.ejmech.2020.112440⟩
European journal of medicinal chemistry, 200

Mycobacterium tuberculosis (M.tb), the etiologic agent of tuberculosis, remains the leading cause of death from a single infectious agent worldwide. The emergence of drug-resistant M.tb strains stresses the need for drugs acting on new targets. Mycol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f002ea775c736cf5d49380e21b9b23b6
https://pubmed.ncbi.nlm.nih.gov/32505086

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs

Autor: Giuseppina Salzano, Ilse Manet, Priscille Brodin, Stefano Ottani, Alain R. Baulard, Jitendra Wankar, Nicolas Willand, Ruxandra Gref, Baptiste Villemagne

Publikováno v: International journal of pharmaceutics
(2017). doi:10.1016/j.ijpharm.2017.05.030
info:cnr-pdr/source/autori:Salzano, Giuseppina; Wankar, Jitendra; Ottani, Stefano; Villemagne, Baptiste; Baulard, Alain R; Willand, Nicolas; Brodin, Priscille; Manet, Ilse; Gref, Ruxandra/titolo:Cyclodextrin-based nanocarriers containing a synergic drug combination: a potential formulation for pulmonary administration of antitubercular drugs./doi:10.1016%2Fj.ijpharm.2017.05.030/rivista:International journal of pharmaceutics (Print)/anno:2017/pagina_da:/pagina_a:/intervallo_pagine:/volume

Tuberculosis (TB) remains a major global health problem. The use of ethionamide (ETH), a main second line drug, is associated to severe toxic side-effects due to its low therapeutic index. In this challenging context, "booster" molecules have been sy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9b632e351937dfa6102eae116383294
https://doi.org/10.1016/j.ijpharm.2017.05.030

Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2

Autor: René Wintjens, Jan Steyaert, Martin Moune, Alain R. Baulard, Matthieu Desroses, Alexandre Wohlkonig, Nicolas Willand, Abdalkarim Tanina, Franck Meyer, Han Remaut

Publikováno v: Biochemical and Biophysical Research Communications. 487:403-408

Inhibition of transcriptional regulators of bacterial pathogens with the aim of reprogramming their metabolism to modify their antibiotic susceptibility constitutes a promising therapeutic strategy. One example is the bio-activation of the anti-tuber

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ea1b46cdb6ad5000da6b51bdb24205a
https://doi.org/10.1016/j.bbrc.2017.04.074