Fragment-based optimized EthR inhibitors with in vivo ethionamide boosting activity
Baptiste Villemagne Arnaud Machelart Ngoc Chau Tran Marion Flipo Martin Moune Florence Leroux Catherine Piveteau Alexandre Wohlkönig René Wintjens Xue Li Ruxandra Gref Priscille Brodin Benoit Deprez Alain R Baulard Nicolas Willand
ACS infectious diseases, 2020-3
https://doi.org/10.1021/acsinfecdis.9b00277
Arnaud Machelart
Machelart Arnaud
ORCID: 0000-0002-4444-0011
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Publisher Correction: Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-018-25177-2
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Fragment-based optimized EthR inhibitors with in vivo ethionamide boosting activity 10.1021/acsinfecdis.9b00277
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Chau N. Tran
Tran Chau N. / Ngoc Chau Tran / Trần Ngọc Châu
ORCID: 0000-0002-6959-7066
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Fragment-based optimized EthR inhibitors with in vivo ethionamide boosting activity 10.1021/acsinfecdis.9b00277
Baptiste Villemagne
Villemagne Baptiste
ORCID: 0000-0002-8416-5253
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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/acsinfecdis.9b00277
Priscille Brodin
Brodin Priscille
ORCID: 0000-0003-0991-7344
Email: priscille.brodin@inserm.fr
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willand nicolas
nicolas willand
ORCID: 0000-0002-0784-0462
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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/acsinfecdis.9b00277
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Marion Flipo
Flipo Marion
ORCID: 0000-0003-2863-5721
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Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.1126/science.aag1006
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space 10.1016/j.tetlet.2016.05.065
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery 10.1016/j.tetlet.2015.05.035
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-beta hydrolysis 10.1016/j.ejmech.2014.04.009
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches 10.1021/jm500422b
Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands 10.1016/j.ab.2014.02.011
On the Mechanism of Degradation of Oxytocin and its Analogues in Aqueous Solution 10.1002/bip.22260
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
Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors 10.1021/jm301506h
Tuberculosis: The drug development pipeline at a glance 10.1016/j.ejmech.2012.02.033
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a
Hydroxamates: Relationships between Structure and Plasma Stability 10.1021/jm900648x
A library of novel hydroxamic acids targeting the metallo-protease family: Design, parallel synthesis and screening 10.1016/j.bmc.2006.10.010
Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents 10.1021/jm061169b
Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors 10.1016/S0960-894X(03)00550-X
Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis 10.1021/acsnano.8b07902
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
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
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
florence leroux
leroux florence
ORCID: 0000-0003-0554-873X
Synthetic EthR inhibitors boost antituberculous activity of ethionamide 10.1038/NM.1950
Designing Focused Chemical Libraries Enriched in Protein-Protein Interaction Inhibitors using Machine-Learning Methods 10.1371/JOURNAL.PCBI.1000695
Synthesis of a 200-member library of squaric acid N-hydroxylamide amides (vol 18, pg 4968, 2008) 10.1016/J.BMCL.2008.08.116
New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold 10.1016/J.BMCL.2010.08.108
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/JM200076A
Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds 10.1021/JM201422E
Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds 10.1021/JM1014617
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
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/JM3003779
Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation 10.1039/C2MD00287F
Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors 10.1021/JM301506H
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-beta hydrolysis 10.1016/J.EJMECH.2014.04.009
Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis 10.4155/FMC.14.84
Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737 10.1177/1087057114534070
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group 10.1016/J.EJMECH.2013.08.027
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches 10.1021/JM500422B
Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance 10.1021/ACS.JMEDCHEM.6B01873
Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme 10.1016/J.EJMECH.2014.12.005
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
Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice 10.1038/NCOMMS9250
ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease 10.1016/J.EBIOM.2016.06.002
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/ACSINFECDIS.9B00277
Drug Target Engagement Using Coupled Cellular Thermal Shift Assay-Acoustic Reverse-Phase Protein Array 10.1177/2472555219897256
Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox 10.1021/ACS.JMEDCHEM.7B01444
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
BIN1 recovers tauopathy-induced long-term memory deficits in mice and interacts with Tau through Thr(348) phosphorylation 10.1007/S00401-019-02017-9
Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening 10.1016/J.EJMECH.2019.06.057
HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC DETERMINATION OF CYCLIC 3',5'-AMP WITH FLUORESCENCE DETECTION - VASOACTIVE INTESTINAL PEPTIDE-INDUCED MODIFICATION OF ITS CONCENTRATION IN NEUROBLASTOMA-CELLS 10.1016/0378-4347(94)80086-3
A NEW VASOACTIVE-INTESTINAL-PEPTIDE ANTAGONIST DISCRIMINATES VIP RECEPTORS ON GUINEA-PIG TRACHEA AND HUMAN NEUROBLASTOMA-CELLS 10.1016/0167-0115(94)90044-2
Tracheal Relaxant Effect of Triazine Derivatives: Correlation with Phosphodiesterase 4 Inhibitory Activity 10.1211/146080899128734613
Use of a low-density microarray for studying gene expression patterns induced by hepatotoxicants on primary cultures of rat hepatocytes 10.1093/TOXSCI/KFG196
High-Throughput Image-Based Aggresome Quantification 10.1177/2472555220919708
Summary of the Sussex-Huawei locomotion-transportation recognition challenge
Observation of a manifold in the chaotic phase space of an asymmetric optical microcavity
Localized temporal variation of Earth's inner-core boundary from high-quality waveform doublets
Off-axis multi-wavelength dispersion controlling metalens for multi-color imaging
Impact of United States political sanctions on international collaborations and research in Iran