Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis
Nguyen, Phuong Chi
Delorme, Vincent
Benarouche, Anais
Guy, Alexandre
Landry, Valerie
Audebert, Stephane
Pophillat, Matthieu
Camoin, Luc
Crauste, Celine
Galano, Jean-Marie
Durand, Thierry
Brodin, Priscille
Canaan, Stephane
Cavalier, Jean-Francois
Bioorganic chemistry, 2018
Vincent Delorme
Delorme Vincent
ORCID: 0000-0001-5235-7069
Discovery of thienothiazolocarboxamide analogues as novel anti-tubercular agent.
10.1016/j.bmc.2020.115797
Drug Discovery Platform Targeting M. tuberculosis with Human Embryonic Stem Cell-Derived Macrophages.
10.1016/j.stemcr.2019.10.002
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis.
10.1016/j.bioorg.2018.08.025
Molecular Targets Related Drug Resistance Mechanisms in MDR-, XDR-, and TDR-Mycobacterium tuberculosis Strains.
10.3389/fcimb.2018.00114
Publisher Correction: Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles.
10.1038/s41598-018-25177-2
Mycobacterium tuberculosis Infection and Innate Responses in a New Model of Lung Alveolar Macrophages.
10.3389/fimmu.2018.00438
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton.
10.15252/embr.201744371
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis.
10.1038/s41598-017-11843-4
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling.
10.1016/j.celrep.2017.08.101
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles.
10.1038/s41598-017-05453-3
Efflux Attenuates the Antibacterial Activity of Q203 in Mycobacterium tuberculosis.
10.1128/aac.02637-16
Phenotypic assays for Mycobacterium tuberculosis infection.
10.1002/cyto.a.23129
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays.
10.1021/acschembio.7b00091
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420.
10.1126/science.aag1006
High-Content Screening of Raw Actinomycete Extracts for the Identification of Antituberculosis Activities.
10.1177/1087057116675887
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria.
10.1111/mmi.13535
STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection.
10.1038/srep29297
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters.
10.1039/c5ob02630j
Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays.
10.1007/978-1-4939-2450-9_24
2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.
10.1021/cb5007163
Supported inhibitor for fishing lipases in complex biological media and mass spectrometry identification.
10.1016/j.biochi.2014.07.015
A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening.
10.3791/51114
Analysis of the discriminative inhibition of mammalian digestive lipases by 3-phenyl substituted 1,3,4-oxadiazol-2(3H)-ones.
10.1016/j.ejmech.2012.10.040
MmPPOX inhibits Mycobacterium tuberculosis lipolytic enzymes belonging to the hormone-sensitive lipase family and alters mycobacterial growth.
10.1371/journal.pone.0046493
Inhibition of phospholipase A1, lipase and galactolipase activities of pancreatic lipase-related protein 2 by methyl arachidonyl fluorophosphonate (MAFP).
10.1016/j.bbalip.2012.07.014
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CO2 binding by dynamic combinatorial chemistry: an environmental selection.
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Two cutinase-like proteins secreted by Mycobacterium tuberculosis show very different lipolytic activities reflecting their physiological function.
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Synthesis and kinetic evaluation of cyclophostin and cyclipostins phosphonate analogs as selective and potent inhibitors of microbial lipases.
10.1021/jm301216x
Phenotypic Screening for Drug Discovery in Tuberculosis
https://doi.org/10.1039/9781839160721-00198
Jean-François Cavalier
Cavalier Jean-François
/ J.-F. Cavalier
ORCID: 0000-0003-0864-8314
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10.1016/s0968-0896(00)00321-7
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Covalent Inhibition of Digestive Lipases by Chiral Phosphonates
10.1021/ar990150i
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New Highly Diastereoselective Synthesis of Phosphoramidates. A Route to Chiral Methyl p -Nitrophenyl Alkylphosphonates
10.1055/s-1998-1560
Synthesis, Structure-activity Relationship and In Vitro Evaluation of Coelenterazine and Coelenteramine Derivatives as Inhibitors of Lipid Peroxidation
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Validation of lipolysis product extraction from aqueous/biological samples, separation and quantification by thin-layer chromatography with flame ionization detection analysis using O-cholesteryl ethylene glycol as a new internal standard
10.1016/j.chroma.2009.07.061
In Vitro Gastrointestinal Lipolysis: Replacement of Human Digestive Lipases by a Combination of Rabbit Gastric and Porcine Pancreatic Extracts
10.1007/s13228-011-0014-5
Enantioselective Inhibition of Microbial Lipolytic Enzymes by Nonracemic Monocyclic Enolphosphonate Analogues of Cyclophostin
10.1021/jm4000787
New insights into the pH-dependent interfacial adsorption of dog gastric lipase using the monolayer technique
10.1016/j.colsurfb.2013.06.025
Synthesis and Kinetic Evaluation of Cyclophostin and Cyclipostins Phosphonate Analogs As Selective and Potent Inhibitors of Microbial Lipases
10.1021/jm301216x
Analysis of the discriminative inhibition of mammalian digestive lipases by 3-phenyl substituted 1,3,4-oxadiazol-2(3H)-ones
10.1016/j.ejmech.2012.10.040
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10.1016/j.biochi.2012.07.023
MmPPOX Inhibits Mycobacterium tuberculosis Lipolytic Enzymes Belonging to the Hormone-Sensitive Lipase Family and Alters Mycobacterial Growth
10.1371/journal.pone.0046493
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10.1016/s0927-7765(98)00099-x
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10.1016/s0009-3084(99)00028-6
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10.1016/j.biochi.2014.01.019
An interfacial and comparative in vitro study of gastrointestinal lipases and Yarrowia lipolytica LIP2 lipase, a candidate for enzyme replacement therapy
10.1016/j.biochi.2014.03.004
Supported inhibitor for fishing lipases in complex biological media and mass spectrometry identification
10.1016/j.biochi.2014.07.015
Biochemical characterization of Yarrowia lipolytica LIP8, a secreted lipase with a cleavable C-terminal region
10.1016/j.bbalip.2014.10.012
3-Keto-1,5-bisphosphonates Alleviate Serum-Oxidative Stress in the High-fat Diet Induced Obesity in Rats
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New lipase assay using Pomegranate oil coating in microtiter plates
10.1016/j.biochi.2015.09.004
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Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis
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Cyclophostin and cyclipostins analogs, new promising molecules to treat mycobacterial-related diseases.
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Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis
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10.1093/femsre/fuab029
Priscille Brodin
Brodin Priscille
ORCID: 0000-0003-0991-7344
Email: priscille.brodin@inserm.fr
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2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1
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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
Stéphane Audebert
Audebert Stéphane
ORCID: 0000-0002-9409-2588
Tubulin polyglutamylase: Partial purification and enzymatic properties
10.1021/bi9804131
Tissue-Specific Gain of RTK Signalling Uncovers Selective Cell Vulnerability during Embryogenesis
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hScrib interacts with ZO-2 at the cell-cell junctions of epithelial cells
10.1016/j.febslet.2005.05.062
Tumour-derived SPARC drives vascular permeability and extravasation through endothelial VCAM1 signalling to promote metastasis
10.1038/ncomms7993
Junctional recruitment of mammalian Scribble relies on E-cadherin engagement
10.1038/sj.onc.1208632
AmotL2 disrupts apical–basal cell polarity and promotes tumour invasion
10.1038/ncomms5557
Mammalian Scribble Forms a Tight Complex with the βPIX Exchange Factor
10.1016/j.cub.2004.05.051
The impact of sodium nitroprusside and ozone in kiwifruit ripening physiology: a combined gene and protein expression profiling approach
10.1093/aob/mcv107
Immunoproteomic identification of antigenic salivary biomarkers detected by Ixodes ricinus-exposed rabbit sera
10.1016/j.ttbdis.2013.06.001
Molecular Characterisation of Endogenous Vangl2/Vangl1 Heteromeric Protein Complexes
10.1371/journal.pone.0046213
Poly(ADP-Ribose) Polymerase 1 (PARP1) Overexpression in Human Breast Cancer Stem Cells and Resistance to Olaparib
10.1371/journal.pone.0104302
Identification of salivary antigenic markers discriminating host exposition between two European ticks: Rhipicephalus sanguineus and Dermacentor reticulatus
10.1016/j.cimid.2012.09.003
The carboxy-terminal sequence Asp427-Glu432 of β-tubulin plays an important function in axonemal motility
10.1046/j.1432-1327.1999.00208.x
Assessment of Anopheles salivary antigens as individual exposure biomarkers to species-specific malaria vector bites
10.1186/1475-2875-11-439
Identification of New Mechanisms of Cellular Response to Chemotherapy by Tracking Changes in Post-Translational Modifications by Ubiquitin and Ubiquitin-Like Proteins
10.1021/pr401258d
MCC, a new interacting protein for Scrib, is required for cell migration in epithelial cells
10.1016/j.febslet.2009.06.034
Replisome function during replicative stress is modulated by histone H3 lysine 56 acetylation through Ctf4
10.1534/genetics.114.173856
Essential and nonredundant roles for Diaphanous formins in cortical microtubule capture and directed cell migration.
10.1091/mbc.e13-08-0482
Masked selection: a straightforward and flexible approach for the selection of binders against specific epitopes and differentially expressed proteins by phage display.
10.1074/mcp.o112.025486
The human PDZome: a gateway to PSD95-Disc large-zonula occludens (PDZ)-mediated functions.
10.1074/mcp.o112.021022
Cutting edge: JAM-C controls homeostatic chemokine secretion in lymph node fibroblastic reticular cells expressing thrombomodulin
10.4049/jimmunol.1003441
ZNF703 gene amplification at 8p12 specifies luminal B breast cancer
10.1002/emmm.201100121
The cell polarity PTK7 receptor acts as a modulator of the chemotherapeutic response in acute myeloid leukemia and impairs clinical outcome
10.1182/blood-2010-01-262352
Angiomotin-like protein 1 controls endothelial polarity and junction stability during sprouting angiogenesis.
10.1161/circresaha.109.195156
The Amot/Patj/Syx signaling complex spatially controls RhoA GTPase activity in migrating endothelial cells
10.1182/blood-2008-04-153874
Scrib regulates PAK activity during the cell migration process
10.1093/hmg/ddn248
ICOS ligation recruits the p50alpha PI3K regulatory subunit to the immunological synapse.
10.4049/jimmunol.181.3.1969
Protein profiling of human breast tumor cells identifies novel biomarkers associated with molecular subtypes.
10.1074/mcp.m700487-mcp200
Recruitment of FOR20 and OFD1 onto pericentriolar satellites and centrosomes depends on the formation of a ternary complex with KIAA0753.
10.1186/2046-2530-4-s1-p69
KIT-D816V oncogenic activity is controlled by the juxtamembrane docking site Y568-Y570
10.1038/onc.2013.12
Alternative splicing modulates autoinhibition and SH3 accessibility in the Src kinase Fyn.
10.1128/mcb.00398-09
Lano, a novel LAP protein directly connected to MAGUK proteins in epithelial cells.
10.1074/jbc.c100330200
Inhibition of flagellar beat frequency by a new anti-beta-tubulin antibody.
10.1002/(sici)1097-0169(1996)35:2<100::aid-cm3>3.0.co;2-e
Reversible polyglutamylation of α- and β-tubulin and microtubule dynamics in mouse brain neurons
10.1091/mbc.4.6.615
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis
10.1016/j.bioorg.2018.08.025
Cell polarity and adherens junction formation inhibit epithelial Fas cell death receptor signaling
10.1083/jcb.201805071
Dual protein kinase and nucleoside kinase modulators for rationally designed polypharmacology
10.1038/s41467-017-01582-5
PAXX Is an Accessory c-NHEJ Factor that Associates with Ku70 and Has Overlapping Functions with XLF
10.1016/j.celrep.2016.09.026
Proteomics and breast cancer: A search for novel diagnostic and theragnostic Biomarkers,Protéomique et cancer du sein: À la recherche de nouveaux biomarqueurs diagnostiques et théragnostiques
10.1684/bdc.2010.1061
Genetic, structural, and chemical insights into the dual function of GRASP55 in germ cell Golgi remodeling and JAM-C polarized localization during spermatogenesis
10.1371/journal.pgen.1006803
Molecular architecture of potassium chloride co-transporter KCC2
10.1038/s41598-017-15739-1
Fibronectin-guided migration of carcinoma collectives
10.1038/ncomms14105
Activation peptide of the coagulation factor XIII (AP-F13A1) as a new biomarker for the screening of colorectal cancer
10.1186/s12014-018-9191-3
Quantitative proteomic analysis exploring progression of colorectal cancer: Modulation of the serpin family
10.1016/j.jprot.2016.07.031
Septin 9-i2 is downregulated in tumors, impairs cancer cell migration and alters subnuclear actin filaments
10.1038/srep44976
EB1-binding–myomegalin protein complex promotes centrosomal microtubules functions
10.1073/pnas.1705682114
Expression and purification of native and functional influenza A virus matrix 2 proton selective ion channel
10.1016/j.pep.2016.11.001
PRICKLE1 Contributes to Cancer Cell Dissemination through Its Interaction with mTORC2
10.1016/j.devcel.2016.04.011
Dermal Fibroblast SLC3A2 Deficiency Leads to Premature Aging and Loss of Epithelial Homeostasis
10.1016/j.jid.2018.05.026
Identification of p62/SQSTM1 as a component of non-canonical Wnt VANGL2-JNK signalling in breast cancer
10.1038/ncomms10318
OFIP/KIAA0753 forms a complex with OFD1 and FOR20 at pericentriolar satellites and centrosomes and is mutated in one individual with oral-facial-digital syndrome
10.1093/hmg/ddv488
The scaffolding function of the RLT PR protein explains its essential role for CD28 co-stimulation in mouse and human T cells
10.1084/JEM.20160579
Comprehensive interactome of Otx2 in the adult mouse neural retina
10.1002/dvg.22903
Regulation of NUB1 activity through non-proteolytic Mdm2-mediated ubiquitination
10.1371/journal.pone.0169988
How may targeted proteomics complement genomic data in breast cancer?
10.1080/14789450.2017.1256776
Post-transcriptional gene silencing mediated by microRNAs is controlled by nucleoplasmic Sfpq
10.1038/s41467-017-01126-x
Cancer cell-derived long pentraxin 3 (PTX3) promotes melanoma migration through a toll-like receptor 4 (TLR4)/NF-κB signaling pathway
10.1038/s41388-019-0848-9
ECT2 associated to PRICKLE1 are poor-prognosis markers in triple-negative breast cancer
10.1038/s41416-019-0448-z
Differential modification of the C. elegans proteome in response to acute and chronic gamma radiation: Link with reproduction decline
10.1016/j.scitotenv.2019.04.039
The Tumor Suppressor SCRIB is a Negative Modulator of the Wnt/β-Catenin Signaling Pathway.
10.1002/pmic.201800487
Clustering as a Means To Control Nitrate Respiration Efficiency and Toxicity in Escherichia coli.
10.1128/mbio.01832-19
Epigenetic down-regulation of the HIST1 locus predicts better prognosis in acute myeloid leukemia with NPM1 mutation.
10.1186/s13148-019-0738-6
PML hyposumoylation is responsible for the resistance of pancreatic cancer.
10.1096/fj.201901091r
Cyclipostins and Cyclophostin Analogues as Multitarget Inhibitors That Impair Growth of Mycobacterium abscessus.
10.1021/acsinfecdis.9b00172
Integrative proteomic and phosphoproteomic profiling of prostate cell lines.
10.1371/journal.pone.0224148
Profiling Ubiquitin and Ubiquitin-like Dependent Post-translational Modifications and Identification of Significant Alterations
10.3791/60402
A systems biology approach reveals neuronal and muscle developmental defects after chronic exposure to ionising radiation in zebrafish.
10.1038/s41598-019-56590-w
Tetraspanin-6 negatively regulates exosome production.
10.1073/pnas.1922447117
A feed-forward mechanosignaling loop confers resistance to therapies targeting the MAPK pathway in BRAF-mutant melanoma.
10.1158/0008-5472.can-19-2914
A proximity-labeling proteomic approach to investigate invadopodia molecular landscape in breast cancer cells
10.1038/s41598-020-63926-4
SLX4 interacts with RTEL1 to prevent transcription-mediated DNA replication perturbations
10.1038/s41594-020-0447-z
ZZW-115-dependent inhibition of NUPR1 nuclear translocation sensitizes cancer cells to genotoxic agents.
10.1172/jci.insight.138117
Dissecting the antibacterial activity of oxadiazolone-core derivatives against Mycobacterium abscessus.
10.1371/journal.pone.0238178
ADAMTSL5 is an epigenetically activated gene underlying tumorigenesis and drug resistance in hepatocellular carcinoma.
10.1016/j.jhep.2020.11.008
ARHGAP45 controls naïve T- and B- cell entry into lymph nodes and T-cell progenitor thymus seeding.
10.15252/embr.202052196
Formation of polarized contractile interfaces by self-organized Toll-8/Cirl GPCR asymmetry.
10.1016/j.devcel.2021.03.030
Identification of PDZ Interactions by Affinity Purification and Mass Spectrometry Analysis.
10.1007/978-1-0716-1166-1_2
Mechano-induced cell metabolism promotes microtubule glutamylation to force metastasis.
10.1016/j.cmet.2021.05.009
TNF-α induces endothelial-mesenchymal transition promoting stromal development of pancreatic adenocarcinoma.
10.1038/s41419-021-03920-4
Insights into animal septins using recombinant human septin octamers with distinct SEPT9 isoforms.
10.1242/jcs.258484
Antisense Oligonucleotide-Based Therapeutic against Menin for Triple-Negative Breast Cancer Treatment
10.3390/biomedicines9070795
Characterization of TseB, a new actor in cell wall elongation in Bacillus subtilis.
10.1111/mmi.14798
Céline Crauste
Crauste Céline
ORCID: 0000-0002-5714-8749
Extra Virgin Olive Oil Reduced Polyunsaturated Fatty Acid and Cholesterol Oxidation in Rodent Liver: Is This Accounted for Hydroxytyrosol-Fatty Acid Conjugation?
10.1021/acs.chemrestox.6b00214
Phloroglucinol protects retinal pigment epithelium and photoreceptor against all-trans-retinal-induced toxicity and inhibits A2E formation.
10.1111/jcmm.12857
Omega-3 polyunsaturated lipophenols, how and why?
10.1016/j.biochi.2015.07.018
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
Tuberculosis: the drug development pipeline at a glance.
10.1016/j.ejmech.2012.02.033
Synthesis of 2',3'-dideoxynucleoside phosphoesters using H-phosphonate chemistry on soluble polymer support.
10.1021/jo1022958
Insights into the soluble PEG-supported synthesis of cytosine-containing nucleoside 5'-mono-, di-, and triphosphates.
10.1021/jo901931z
Development of a sensitive and selective LC/MS/MS method for the simultaneous determination of intracellular 1-beta-D-arabinofuranosylcytosine triphosphate (araCTP), cytidine triphosphate (CTP) and deoxycytidine triphosphate (dCTP) in a human follicular lymphoma cell line.
10.1016/j.jchromb.2009.02.071
Magnesium(II)-coordinated Claisen rearrangement: a direct approach towards ulosonic acid derivatives
10.1016/j.tetlet.2006.07.022
Asymmetric Synthesis of New β-Lactam Lipopeptides as Bacterial Signal Peptidase I Inhibitors
10.1002/ejoc.201100148
Total Syntheses of Two bis-Allylic-Deuterated DHA Analogues
10.1002/ajoc.201600565
Synthesis and Evaluation of Polyunsaturated Fatty Acid-Phenol Conjugates as Anti-Carbonyl-Stress Lipophenols
10.1002/ejoc.201402282
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions
10.1002/ejlt.201700171
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis
10.1016/j.bioorg.2018.08.025
LipG a bifunctional phospholipase/thioesterase involved in mycobacterial envelope remodeling
10.1042/bsr20181953
New Lipophenol Antioxidants Reduce Oxidative Damage in Retina Pigment Epithelial Cells
10.3390/antiox7120197
Resveratrol-Linoleate protects from exacerbated endothelial permeability via a drastic inhibition of the MMP-9 activity
10.1042/bsr20171712
Bis-allylic Deuterated DHA Alleviates Oxidative Stress in Retinal Epithelial Cells
10.3390/antiox8100447
Isopropyl-phloroglucinol-DHA protects outer retinal cells against lethal dose of all-trans-retinal.
10.1111/jcmm.15135
Combination of Lutein and Zeaxanthin, and DHA Regulated Polyunsaturated Fatty Acid Oxidation in H2O2-Stressed Retinal Cells.
10.1007/s11064-020-02994-4
