A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation
Alexandra Pastor
Arnaud Machelart
Xue Li
Nicolas Willand
Alain Baulard
Priscille Brodin
Ruxandra Gref
Didier Desmaële
Arnaud Machelart
Machelart Arnaud
ORCID: 0000-0002-4444-0011
Identification of immune effectors essential to the control of primary and secondary intranasal infection with brucella melitensis in mice
10.4049/jimmunol.1502265
In situ characterization of splenic brucella melitensis reservoir cells during the chronic phase of infection in susceptible mice
10.1371/journal.pone.0137835
Brucella melitensis invades murine erythrocytes during infection.
10.1128/iai.01779-14
In situ microscopy analysis reveals local innate immune response developed around Brucella infected cells in resistant and susceptible mice
10.1371/journal.ppat.1002575
Host-directed therapies offer novel opportunities for the fight against tuberculosis
10.1016/j.drudis.2017.05.005
Erythritol availability in bovine, murine and human models highlights a potential role for the host aldose reductase during Brucella infection
10.3389/fmicb.2017.01088
Combination therapy for tuberculosis treatment: Pulmonary administration of ethionamide and booster co-loaded nanoparticles
10.1038/s41598-017-05453-3
Chronic Brucella infection induces selective and persistent IFN-γ-dependent alterations of marginal zone macrophages in the spleen.
10.1128/iai.00115-17
Proteomics of Mycobacterium infection: Moving towards a better understanding of pathogen-driven immunomodulation
10.3389/fimmu.2018.00086
Publisher Correction: Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles.
10.1038/s41598-018-25177-2
Allergic asthma favors Brucella growth in the lungs of infected mice
10.3389/fimmu.2018.01856
Intrinsic antibacterial activity of nanoparticles made of β-cyclodextrins potentiates their effect as drug nanocarriers against tuberculosis
10.1021/acsnano.8b07902
A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation
10.1039/C9OB00680J
Route of Infection Strongly Impacts the Host-Pathogen Relationship
10.3389/fimmu.2019.01589
IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection
10.1101/761551
Occurrence and repair of alkylating stress in the intracellular pathogen Brucella abortus
10.1038/s41467-019-12516-8
Fragment-based optimized EthR inhibitors with in vivo ethionamide boosting activity
10.1021/acsinfecdis.9b00277
Convergent evolution of zoonoticBrucellaspecies toward the selective use of the pentose phosphate pathway
10.1073/pnas.2008939117
Paradoxical Roles of the MAL/Tirap Adaptor in Pathologies
10.3389/fimmu.2020.569127
SARS-CoV-2 infection in nonhuman primates alters the composition and functional activity of the gut microbiota
10.1080/19490976.2021.1893113
Trypanosoma infection favors Brucella elimination via IL-12/IFNγ-dependent pathways
10.3389/fimmu.2017.00903
Large scale screening discovers clofoctol as an inhibitor of SARS-CoV-2 replication that reduces COVID-19-like pathology
10.1101/2021.06.30.450483
High-Content Analysis Monitoring Intracellular Trafficking and Replication of Mycobacterium tuberculosis Inside Host Cells
10.1007/978-1-0716-1460-0_29
Alain Baulard
Baulard Alain
/ Alain Robert Baulard
ORCID: 0000-0002-0150-5241
Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2
10.1016/j.bbrc.2017.04.074
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton
10.15252/embr.201744371
Mercury resistance as a selective marker for recombinant mycobacteria
10.1099/13500872-141-4-1045
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton
10.15252/embr.201744371
10.15252/embr.201744371.
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles
10.1038/s41598-017-05453-3
10.1038/s41598-017-05453-3.
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs
10.1016/j.ijpharm.2017.05.030
10.1016/j.ijpharm.2017.05.030. Epub 2017 May 15.
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays
10.1021/acschembio.7b00091
10.1021/acschembio.7b00091. Epub 2017 Apr 5.
New active leads for tuberculosis booster drugs by structure-based drug discovery
10.1039/c7ob00910k
10.1039/c7ob00910k.
Phenotypic assays for Mycobacterium tuberculosis infection
10.1002/cyto.a.23129
10.1002/cyto.a.23129.
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420
10.1126/science.aag1006
10.1126/science.aag1006. Epub 2017 Mar 16.
Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2
10.1016/j.bbrc.2017.04.074
10.1016/j.bbrc.2017.04.074. Epub 2017 Apr 14.
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters
10.1039/c5ob02630j
10.1039/c5ob02630j. Epub 2016 Jan 25.
Effects of Lipid-Lowering Drugs on Vancomycin Susceptibility of Mycobacteria
10.1128/AAC.00872-16
10.1128/AAC.00872-16. Print 2016 Oct.
STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection
10.1038/srep29297
10.1038/srep29297.
Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG
10.1016/j.chembiol.2015.05.016
10.1016/j.chembiol.2015.05.016. Epub 2015 Jun 18.
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches
10.1021/jm500422b
10.1021/jm500422b. Epub 2014 May 28.
The Mycobacterium tuberculosis transcriptional repressor EthR is negatively regulated by Serine/Threonine phosphorylation
10.1016/j.bbrc.2014.03.074
10.1016/j.bbrc.2014.03.074. Epub 2014 Mar 22.
Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands
10.1016/j.ab.2014.02.011
10.1016/j.ab.2014.02.011. Epub 2014 Feb 20.
Mechanism of competence activation by the ComRS signalling system in streptococci
10.1111/mmi.12157
10.1111/mmi.12157. Epub 2013 Feb 4.
Structural and docking studies of potent ethionamide boosters
10.1107/S0108270113028126
10.1107/S0108270113028126. Epub 2013 Oct 24.
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis
10.1021/jm300377g
10.1021/jm300377g. Epub 2012 Jul 17.
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors
10.1021/jm200825u
10.1021/jm200825u. Epub 2011 Dec 6.
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands
10.1093/nar/gkr1113
10.1093/nar/gkr1113. Epub 2011 Dec 9.
Tuberculosis: the drug development pipeline at a glance
10.1016/j.ejmech.2012.02.033
10.1016/j.ejmech.2012.02.033. Epub 2012 Feb 25.
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors
10.1021/jm200076a
10.1021/jm200076a. Epub 2011 Apr 1.
MALDI imaging techniques dedicated to drug-distribution studies
10.4155/bio.11.88
10.4155/bio.11.88.
Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator
10.1021/cb100177g
10.1021/cb100177g.
Molecular genetics of para-aminosalicylic acid resistance in clinical isolates and spontaneous mutants of Mycobacterium tuberculosis
10.1128/AAC.01197-08
10.1128/AAC.01197-08. Epub 2009 Feb 23.
Molecular mapping of lipoarabinomannans on mycobacteria
10.1021/la900302a
10.1021/la900302a.
Synthetic EthR inhibitors boost antituberculous activity of ethionamide
10.1038/nm.1950
10.1038/nm.1950. Epub 2009 May 3.
Organization of the mycobacterial cell wall: a nanoscale view
10.1007/s00424-007-0386-0
Antibody response in pulmonary tuberculosis against recombinant 27kDa (MPT51, Rv3803c) protein of Mycobacterium tuberculosis
10.1080/00365540701402954
Chemical force microscopy of single live cells
10.1021/nl071476k
Direct measurement of hydrophobic forces on cell surfaces using AFM
10.1021/la702765c
Effects of mechanical wounding on Carica papaya cysteine endopeptidases accumulation and activity
10.1016/j.ijbiomac.2006.02.021
Ethambutol-induced alterations in Mycobacterium bovis BCG imaged by atomic force microscopy
10.1111/j.1574-6968.2006.00443.x
Insights into mechanisms of induction and ligands recognition in the transcriptional repressor EthR from Mycobacterium tuberculosis
10.1016/j.tube.2005.07.005
Selective intracellular accumulation of the major metabolite issued from the activation of the prodrug ethionamide in mycobacteria
10.1093/jac/dkl332
Monitoring of the ethionamide pro-drug activation in mycobacteria by (1)H high resolution magic angle spinning NMR
10.1016/j.bbrc.2005.03.197
[Doping in the peloton of antituberculosis drugs]
10.1051/medsci/2005214351
Cloning, expression, and purification of the 27 kDa (MPT51, Rv3803c) protein of Mycobacterium tuberculosis
10.1016/j.pep.2004.01.016
Identification of a novel class of omega,E,E-farnesyl diphosphate synthase from Mycobacterium tuberculosis
10.1194/jlr.M400047-JLR200
Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis
10.1016/j.molcel.2004.09.020
In vivo interaction between the polyprenol phosphate mannose synthase Ppm1 and the integral membrane protein Ppm2 from Mycobacterium smegmatis revealed by a bacterial two-hybrid system
10.1074/jbc.M207922200
Inhibition of InhA activity, but not KasA activity, induces formation of a KasA-containing complex in mycobacteria
10.1074/jbc.M302435200
Unique mechanism of action of the thiourea drug isoxyl on Mycobacterium tuberculosis
10.1074/jbc.M311209200
Ppm1, a novel polyprenol monophosphomannose synthase from Mycobacterium tuberculosis
10.1042/BJ20020107
Activation of the pro-drug ethionamide is regulated in mycobacteria
10.1074/jbc.M003744200
Thiolactomycin and related analogues as novel anti-mycobacterial agents targeting KasA and KasB condensing enzymes in Mycobacterium tuberculosis
10.1074/jbc.M000569200
A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation
10.1039/C9OB00680J
Priscille Brodin
Brodin Priscille
ORCID: 0000-0003-0991-7344
Email: priscille.brodin@inserm.fr
How can nanoparticles contribute to antituberculosis therapy?
10.1016/j.drudis.2017.01.011
Host-directed therapies offer novel opportunities for the fight against tuberculosis
10.1016/j.drudis.2017.05.005
A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone
10.3390/toxins9070227
A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone
10.3390/toxins9070227
10.3390/toxins9070227.
Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections
10.2217/nnm-2016-0364
Cyclodextrin-based nanocarriers containing a synergic drug combination: a potential formulation for pulmonary administration of antitubercular drugs
10.1016/j.ijpharm.2017.05.030
10.1016/j.ijpharm.2017.05.030.
Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism
10.1007/s00401-016-1652-z
Host-directed therapies offer novel opportunities for the fight against tuberculosis
10.1016/j.drudis.2017.05.005
10.1016/j.drudis.2017.05.005.
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria
10.1111/mmi.13535
Impact of pe_ pgrs33 Gene Polymorphisms on Mycobacterium tuberculosis Infection and Pathogenesis
10.3389/fcimb.2017.00137
LppM impact on the colonization of macrophages by Mycobacterium tuberculosis
10.1111/cmi.12619
Phenotypic assays for Mycobacterium tuberculosis infection
10.1002/cyto.a.23129
10.1002/cyto.a.23129.
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420
10.1126/science.aag1006
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters
10.1039/c5ob02630j
Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro
10.1007/s00705-016-2771-5
Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization
10.1016/j.str.2016.07.009
Mycolactone The amazing analgesic mycobacterial toxin
10.1051/medsci/20163202007
STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection
10.1038/srep29297
2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1
10.1021/cb5007163
Cytosolic Access of Mycobacterium tuberculosis: Critical Impact of Phagosomal Acidification Control and Demonstration of Occurrence In Vivo
10.1371/journal.ppat.1004650
High content screening in chemical biology: overview and main challenges
10.1051/medsci/20153102016
High-Content Screening Technology Combined with a Human Granuloma Model as a New Approach To Evaluate the Activities of Drugs against Mycobacterium tuberculosis
10.1128/aac.03705-14
Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system
10.1016/j.vaccine.2015.03.083
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro
10.3389/fmicb.2015.00438
Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action
10.1128/jvi.01473-15
Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays
10.1007/978-1-4939-2450-9_24
A Microscopic Phenotypic Assay for the Quantification of Intracellular Mycobacteria Adapted for High-throughput/High-content Screening
10.3791/51114
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches
10.1021/jm500422b
Mycobacterial Toxin Induces Analgesia in Buruli Ulcer by Targeting the Angiotensin Pathways
10.1016/j.cell.2014.04.040
Potent antiviral activity of Solanum rantonnetii and the isolated compounds against hepatitis C virus in vitro
10.1016/j.jff.2014.09.022
A novel specific edge effect correction method for RNA interference screenings
10.1093/bioinformatics/btr648
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis
10.1021/jm3003779
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors
10.1021/jm200825u
The Balance of Apoptotic and Necrotic Cell Death in Mycobacterium tuberculosis Infected Macrophages Is Not Dependent on Bacterial Virulence
10.1371/journal.pone.0047573
Analogous Mechanisms of Resistance to Benzothiazinones and Dinitrobenzamides in Mycobacterium smegmatis
10.1371/journal.pone.0026675
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors
10.1021/jm200076a
High-content screening in infectious diseases
10.1016/j.cbpa.2011.05.023
Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ
10.1099/mic.0.038133-0
High Content Phenotypic Cell-Based Visual Screen Identifies Mycobacterium tuberculosis Acyltrehalose-Containing Glycolipids Involved in Phagosome Remodeling
10.1371/journal.ppat.1001100
High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery
10.4155/fmc.10.223
Long-circulating DNA lipid nanocapsules as new vector for passive tumor targeting
10.1016/j.biomaterials.2009.09.044
Automated High-Throughput siRNA Transfection in Raw 264.7 Macrophages: A Case Study for Optimization Procedure
10.1177/1087057108328762
Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis
10.1126/science.1171583
High Content Screening Identifies Decaprenyl-Phosphoribose 2 ' Epimerase as a Target for Intracellular Antimycobacterial Inhibitors
10.1371/journal.ppat.1000645
Systematic Genetic Nomenclature for Type VII Secretion Systems
10.1371/journal.ppat.1000507
Control of M-tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP
10.1371/journal.ppat.0040033
Aquatic insects and transmission of Mycobacterium ulcerans
10.1051/medsci/20072367572
ESAT-6 from Mycobacterium tuberculosis dissociates from its putative chaperone CFP-10 under acidic conditions and exhibits membrane-lysing activity
10.1128/jb.00469-07
Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis
10.1371/journal.ppat.0030062
Protection against mycobacterium ulcerans lesion development by exposure to aquatic insect saliva
10.1371/journal.pmed.0040064
Support vector machines for automatic detection of tuberculosis bacteria in confocal microscopy images
10.1109/isbi.2007.356794
Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues
10.1016/j.bmc.2006.12.009
An increase in antimycobacterial Th1-cell responses by prime-boost protocols of immunization does not enhance protection against tuberculosis
10.1128/iai.74.4.2128-2137.2006
Benzofuro 3,2-f 1 benzopyrans: A new class of antitubercular agents
10.1016/j.bmc.2006.03.033
Dissection of ESAT-6 system 1 of Mycobacterium tuberculosis and impact on immunogenicity and virulence
10.1128/iai.74.1.88-98.2006
High frequency of CD4(+) T cells specific for the TB10.4 protein correlates with protection against Mycobacterium tuberculosis infection
10.1128/iai.02086-05
Inactivation of Rv2525c, a substrate of the twin arginine translocation (Tat) system of Mycobacterium tuberculosis, increases beta-lactam susceptibility and virulence
10.1128/jb.00631-06
Evaluation of vaccines in the EU TB vaccine cluster using a guinea pig aerosol infection model of tuberculosis
10.1016/j.tube.2004.09.009
Functional analysis of early secreted antigenic target-6, the dominant T-cell antigen of Mycobacterium tuberculosis, reveals key residues involved in secretion, complex formation, virulence, and immunogenicity
10.1074/jbc.M503515200
Immunogenic membrane-associated proteins of Mycobacterium tuberculosis revealed by proteomics
10.1099/mic.0.27799-0
Proteomic identification of M. tuberculosis protein kinase substrates: PknB recruits GarA, a FHA domain-containing protein, through activation loop-mediated interactions
10.1016/j.jmb.2005.05.049
Tuberculosis: from genome to vaccine
10.1586/14760584.4.4.541
Cell envelope protein PPE68 contributes to Mycobacterium tuberculosis RDI immunogenicity independently of a 10-kilodalton culture filtrate protein and ESAT-6
10.1128/iai.72.4.2170-2176.2004
Enhanced protection against tuberculosis by vaccination with recombinant Mycobacterium microti vaccine that induces T cell immunity against region of difference 1 antigens
10.1086/421468
ESAT-6 proteins: protective antigens and virulence factors?
10.1016/j.tim.2004.09.007
Macro-array and bioinformatic analyses reveal mycobacterial 'core' genes, variation in the ESAT-6 gene family and new phylogenetic markers for the Mycobacterium tuberculosis complex
10.1099/mic.0.26662-0
CD8(+)-T-cell responses of mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family
10.1128/iai.71.12.7173-7177.2003
Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis
10.1038/nm859
A new evolutionary scenario for the Mycobacterium tuberculosis complex
10.1073/pnas.052548299
Bacterial artificial chromosome-based comparative genomic analysis identifies Mycobacterium microti as a natural ESAT-6 deletion mutant
10.1128/iai.70.10.5568-5578.2002
Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides
10.1021/bi015732y
Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti
10.1046/j.1365-2958.2002.03237.x
6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro
10.1081/ncn-100002322
Determinants of Mg2+-dependent activities of recombinant human immunodeficiency virus type 1 integrase
10.1021/bi000398b
Inhibition of the human immunodeficiency virus type 1 DNA integration by modified oligonucleotides
10.1023/a:1026631910681
Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase
10.1016/s0014-5793(99)01350-2
Inhibition of HIV-1 integration by mono- & bi-functionalized triple helix forming oligonucleotides
10.1080/07328319908044831
Optimization of alternate-strand triple helix formation at the 5 '-TpA-3 ' and 5 '-ApT-3 ' junctions
10.1093/nar/27.15.3029
A truncated HIV-1 Tat protein basic domain rapidly translocates through the plasma membrane and accumulates in the cell nucleus
10.1074/jbc.272.25.16010
Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids
10.1073/pnas.1707840114
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton
10.15252/embr.201744371
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton
10.15252/embr.201744371
10.15252/embr.201744371.
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles
10.1038/s41598-017-05453-3
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis
10.1038/s41598-017-11843-4
10.1038/s41598-017-11843-4.
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays
10.1021/acschembio.7b00091
Host-pathogen systems for early drug discovery against tuberculosis
10.1016/j.mib.2017.11.017
10.1016/j.mib.2017.11.017.
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages
10.1016/j.chom.2017.07.020
10.1016/j.chom.2017.07.020. Epub 2017 Aug 31.
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling
10.1016/j.celrep.2017.08.101
10.1016/j.celrep.2017.08.101.
Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids
10.1073/pnas.1707840114
10.1073/pnas.1707840114.
Identification of Piperazinylbenzenesulfonamides as New Inhibitors of Claudin-1 Trafficking and Hepatitis C Virus Entry
10.1128/jvi.01982-17
Multiplexed Quantitation of Intraphagocyte Mycobacterium tuberculosis Secreted Protein Effectors
10.1016/j.celrep.2018.03.125
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis
10.1016/j.bioorg.2018.08.025
Proteomics of Mycobacterium infection: Moving towards a Better Understanding of Pathogen-Driven immunomodulation
10.3389/fimmu.2018.00086
Synergy between circular bacteriocin AS-48 and ethambutol against Mycobacterium tuberculosis
10.1128/aac.00359-18
The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase
10.1016/j.tube.2018.08.004
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis
10.1038/s41598-017-11843-4
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs
10.1016/j.ijpharm.2017.05.030
Host-pathogen systems for early drug discovery against tuberculosis
10.1016/j.mib.2017.11.017
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages
10.1016/j.chom.2017.07.020
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling
10.1016/j.celrep.2017.08.101
Phenotypic assays for Mycobacterium tuberculosis infection
10.1002/cyto.a.23129
A fast, fully automated cell segmentation algorithm for high-throughput and high-content screening
10.1002/cyto.a.20627
Compartmentalized Encapsulation of Two Antibiotics in Porous Nanoparticles: an Efficient Strategy to Treat Intracellular Infections
10.1002/ppsc.201800360
Spatiotemporal Changes of the Phagosomal Proteome in Dendritic Cells in Response to LPS Stimulation
10.1074/mcp.RA119.001316
Mycolactone as Analgesic: Subcutaneous Bioavailability Parameters
10.3389/fphar.2019.00378
Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis
10.1021/acsnano.8b07902
Mitochondrial Dynamics and Activity in Legionella-Infected Cells
10.1007/978-1-4939-9048-1_13
Heparin-Binding Hemagglutinin Adhesin (HBHA) Is Involved in Intracytosolic Lipid Inclusions Formation in Mycobacteria
10.3389/fmicb.2018.02258
Dehydrojuncusol, a Natural Phenanthrene Compound Extracted from Juncus maritimus, Is a New Inhibitor of Hepatitis C Virus RNA Replication
10.1128/jvi.02009-18
A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation
10.1039/C9OB00680J
Could Mycolactone Inspire New Potent Analgesics? Perspectives and Pitfalls
10.3390/toxins11090516
Paradoxical Roles of the MAL/Tirap Adaptor in Pathologies.
10.3389/fimmu.2020.569127
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity.
10.1021/acsinfecdis.9b00277
Intracellular and in vivo evaluation of imidazo[2,1-b]thiazole-5-carboxamide anti-tuberculosis compounds.
10.1371/journal.pone.0227224
Preclinical assessment of a new live attenuated Mycobacterium tuberculosis Beijing-based vaccine for tuberculosis.
10.1016/j.vaccine.2019.11.085
IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection
10.1101/761551
Worms' Antimicrobial Peptides.
10.3390/md17090512
T(oo)bAd.
10.1038/s41589-019-0347-x
Theaflavins, polyphenols of black tea, inhibit entry of hepatitis C virus in cell culture.
10.1371/journal.pone.0198226
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro.
10.3389/fmicb.2015.00488
Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis.
10.1038/nm.3262
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis.
10.1021/jm300377g
Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease.
10.1186/1753-6561-5-s1-p38
Automated HTS/HCS for antivirals using visual HIV full replication assays.
10.1186/1742-4690-6-s2-p82
Influence of ESAT-6 secretion system 1 (RD1) of Mycobacterium tuberculosis on the interaction between mycobacteria and the host immune system.
10.4049/jimmunol.174.6.3570
Cell microbiology interview
10.1111/cmi.13288
Pathogenomic analyses of Mycobacterium microti, an ESX-1-deleted member of the Mycobacterium tuberculosis complex causing disease in various hosts
10.1099/mgen.0.000505
willand nicolas
nicolas willand
ORCID: 0000-0002-0784-0462
Neuraminidase inhibitors and risk of H5 N1 influenza,Les inhibiteurs de neuraminidase face au risque de grippe aviaire
10.1016/s0003-4509(07)90016-4
Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands
10.1016/j.ab.2014.02.011
Water-based conditions for the microscale parallel synthesis of bicyclic lactams
10.1016/j.tetlet.2012.11.082
Exploring drug target flexibility using in situ click chemistry: Application to a mycobacterial transcriptional regulator
10.1021/cb100177g
Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann-Finkelstein tandem reaction
10.1016/j.tetlet.2005.12.022
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery
10.1016/j.tetlet.2015.05.035
Efficient, two-step synthesis of N-substituted nortropinone derivatives
10.1016/j.tetlet.2007.05.110
Natural compounds: Leads or ideas? Bioinspired molecules for drug discovery
10.1111/j.1747-0285.2008.00673.x
MALDI imaging techniques dedicated to drug-distribution studies
10.4155/bio.11.88
Solid and solution phase syntheses of the 2-cyanopyrrolidide DPP-IV inhibitor NVP-DPP728
10.1016/S0040-4020(02)00536-7
Original loading and Suzuki conditions for the solid-phase synthesis of biphenyltetrazoles. Application to the first solid-phase synthesis of irbesartan
10.1016/j.tetlet.2008.02.147
Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation
10.1016/j.ejmech.2011.05.056
A simple reaction to produce small structurally complex and diverse molecules
10.1016/j.tetlet.2004.05.008
Efficient, protection-free Suzuki-Miyaura synthesis of ortho- biphenyltetrazoles
10.1016/j.tetlet.2005.07.082
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands
10.1093/nar/gkr1113
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space
10.1016/j.tetlet.2016.05.065
Ethionamide boosters: Synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors
10.1021/jm200076a
Carbohydrate-protein interactions at interfaces: Synthesis of thiolactosyl glycolipids and design of a working model for surface plasmon resonance
10.1039/b210672h
Structural and docking studies of potent ethionamide boosters
10.1107/S0108270113028126
A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues
10.1016/j.tetlet.2006.12.050
UFU ('Ullmann-Finkelstein-Ullmann'): a new multicomponent reaction
10.1016/j.tetlet.2006.04.041
Palladium-free Sonogashira-type cross-coupling reaction of bromoisoxazolines or N-alkoxyimidoyl bromides and alkynes
10.1016/j.tetlet.2016.01.070
Tuberculosis: The drug development pipeline at a glance
10.1016/j.ejmech.2012.02.033
Synthesis and structural studies of a novel scaffold for drug discovery: A 4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4′-piperidine]
10.1016/j.tetlet.2003.11.079
Synthetic EthR inhibitors boost antituberculous activity of ethionamide
10.1038/nm.1950
A facile and rapid synthesis of N-benzyl-2-substituted piperazines
10.1016/j.tetlet.2011.02.011
Ligand efficiency driven design of new inhibitors of mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches
10.1021/jm500422b
Discovery of novel N -phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis
10.1021/jm300377g
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors
10.1021/jm200825u
A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR
10.1016/j.bbapap.2018.12.003
A novel codrug made of the combination of ethionamide and its potentiating booster: Synthesis, self-assembly into nanoparticles and antimycobacterial evaluation
10.1039/c9ob00680j
Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2
10.1016/j.bbrc.2017.04.074
Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance
10.1016/bs.armc.2019.06.003
New active leads for tuberculosis booster drugs by structure-based drug discovery
10.1039/c7ob00910k
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420
10.1126/science.aag1006
Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis
10.1016/j.ejmech.2018.09.038
Intrinsic antibacterial activity of nanoparticles made of β-cyclodextrins potentiates their effect as drug nanocarriers against tuberculosis
10.1021/acsnano.8b07902
Combination therapy for tuberculosis treatment: Pulmonary administration of ethionamide and booster co-loaded nanoparticles
10.1038/s41598-017-05453-3
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity
10.1021/acsinfecdis.9b00277
Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening
10.1016/j.ejmech.2020.112440
Microwave-Assisted Suzuki-Miyaura Cross Coupling using Nickel as Catalyst to Rapidly Access to 3-Arylazetidine
10.1002/slct.201702101
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs
10.1016/j.ijpharm.2017.05.030
A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2
10.1016/j.ejmech.2019.02.023
Didier Desmaele
Desmaele Didier
ORCID: 0000-0003-4013-4655
Nanotechnologies for the treatment of colon cancer: From old drugs to new hope
10.1016/j.ijpharm.2016.06.005
A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation
10.1039/C9OB00680J
Design of Rhenium Compounds in Targeted Anticancer Therapeutics
10.2174/1381612825666190902161400
Highly Porous Hybrid Metal–Organic Nanoparticles Loaded with Gemcitabine Monophosphate: a Multimodal Approach to Improve Chemo‐ and Radiotherapy
10.1002/cmdc.201900596
Front Cover: Highly Porous Hybrid Metal–Organic Nanoparticles Loaded with Gemcitabine Monophosphate: a Multimodal Approach to Improve Chemo‐ and Radiotherapy (ChemMedChem 3/2020)
10.1002/cmdc.202000030
A Self-Assembling NHC-Pd-Loaded Calixarene as a Potent Catalyst for the Suzuki-Miyaura Cross-Coupling Reaction in Water
10.3390/molecules25061459
Combinatorial Nanomedicine Made of Squalenoyl-Gemcitabine and Edelfosine for the Treatment of Osteosarcoma
10.3390/cancers12071895
