Approaches for targeting the mycobactin biosynthesis pathway for novel anti-tubercular drug discovery: where we stand

Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition

(2022) Mousumi Shyam et al.   JOURNAL OF MEDICINAL CHEMISTRY

In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas

(2022) Samantha Ottavi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Superior efficacy of a bedaquiline, delamanid and linezolid combination regimen in a mouse-TB model

(2021) Elise D Pieterman et al.   JOURNAL OF INFECTIOUS DISEASES

Genetic variants and their association with phenotypic resistance to bedaquiline in Mycobacterium tuberculosis: a systematic review and individual isolate data analysis

(2021) Nabila Ismail et al.   Lancet Microbe

Advances in the development of HIV integrase strand transfer inhibitors

(2021) Yue Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Biophysical analysis of the Mycobacteria tuberculosis peptide binding protein DppA reveals a stringent peptide binding pocket

(2021) Dinesh M. Fernando et al.   TUBERCULOSIS

Flavonoids as Novel Efflux Pump Inhibitors and Antimicrobials Against Both Environmental and Pathogenic Intracellular Mycobacterial Species

(2020) Julia Solnier et al.   MOLECULES

Molecular characteristics and in vitro susceptibility to bedaquiline of Mycobacterium tuberculosis isolates circulating in Shaanxi, China

(2020) Jian Yang et al.   INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES

Shedding X-ray Light on the Role of Magnesium in the Activity of Mycobacterium tuberculosis Salicylate Synthase (MbtI) for Drug Design

(2020) Matteo Mori et al.   JOURNAL OF MEDICINAL CHEMISTRY

In vitro Study of Bedaquiline Resistance in Mycobacterium tuberculosis Multi-Drug Resistant Clinical Isolates

(2020) Giulia Degiacomi et al.   Frontiers in Microbiology

The Mycobactin Biosynthesis Pathway: A Prospective Therapeutic Target in the Battle against Tuberculosis

(2020) Mousumi Shyam et al.   JOURNAL OF MEDICINAL CHEMISTRY

Direct Inhibition of MmpL3 by Novel Antitubercular Compounds

(2019) Wei Li et al.   ACS Infectious Diseases

Mutations in Efflux Pump Rv1258c (Tap) Cause Resistance to Pyrazinamide, Isoniazid, and Streptomycin in M. tuberculosis

(2019) Jiayun Liu et al.   Frontiers in Microbiology

Opposing reactions in coenzyme A metabolism sensitize Mycobacterium tuberculosis to enzyme inhibition

(2019) Elaine Ballinger et al.   SCIENCE

Scaffold Based Search On The Desferithiocin Archetype

(2019) Mousumi Shyam et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents

(2019) Laurent R. Chiarelli et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Empirical ways to identify novel Bedaquiline resistance mutations in AtpE

(2019) Malancha Karmakar et al.   PLoS One

Exploration of 5‐(5‐nitrothiophen‐2‐yl)‐4,5‐dihydro‐1H‐pyrazoles as selective, multitargeted antimycobacterial agents

(2019) Neha Agre et al.   Chemical Biology & Drug Design

Structural insights into phosphopantetheinyl hydrolase PptH from Mycobacterium tuberculosis

(2019) John Mosior et al.   PROTEIN SCIENCE

WHO global progress report on tuberculosis elimination

(2019) Emilia Harding   Lancet Respiratory Medicine

Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents

(2018) Laurent R. Chiarelli et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Bedaquiline and delamanid in the treatment of multidrug‐resistant tuberculosis: Promising but challenging

(2018) Yang Li et al.   DRUG DEVELOPMENT RESEARCH

The diverse family of MmpL transporters in mycobacteria: from regulation to antimicrobial developments

(2017) Albertus Viljoen et al.   MOLECULAR MICROBIOLOGY

Virtual Screening, pharmacophore development and structure based similarity search to identify inhibitors against IdeR, a transcription factor of Mycobacterium tuberculosis

(2017) Akshay Rohilla et al.   Scientific Reports

Iron Acquisition Pathways as Targets for Antitubercular Drugs

(2016) Fiorella Meneghetti et al.   CURRENT MEDICINAL CHEMISTRY

Post-translational Acetylation of MbtA Modulates Mycobacterial Siderophore Biosynthesis

(2016) Olivia Vergnolle et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Design, Synthesis, and Evaluation of Novel Hybrid Efflux Pump Inhibitors for Use against Mycobacterium tuberculosis

(2016) Malkeet Kumar et al.   ACS Infectious Diseases

The Structure and Interactions of Periplasmic Domains of Crucial MmpL Membrane Proteins from Mycobacterium tuberculosis

(2015) Nicholas Chim et al.   CHEMISTRY & BIOLOGY

Mechanism of Iron-Dependent Repressor (IdeR) Activation and DNA Binding: A Molecular Dynamics and Protein Structure Network Study

(2015) Soma Ghosh et al.   PLoS Computational Biology

Bedaquiline for the treatment of multidrug-resistant tuberculosis: great promise or disappointment?

(2015) Stephen K. Field   Therapeutic Advances in Chronic Disease

Cross-Resistance between Clofazimine and Bedaquiline through Upregulation of MmpL5 in Mycobacterium tuberculosis

(2014) R. C. Hartkoorn et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

ATP synthase in mycobacteria: Special features and implications for a function as drug target

(2014) Ping Lu et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS

Iron-Regulated Protein HupB of Mycobacterium tuberculosis Positively Regulates Siderophore Biosynthesis and Is Essential for Growth in Macrophages

(2014) S. D. Pandey et al.   JOURNAL OF BACTERIOLOGY

Siderophore Receptor-Mediated Uptake of Lactivicin Analogues in Gram-Negative Bacteria

(2014) Jeremy Starr et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transcriptional regulation of Mycobacterium tuberculosis hupB gene expression

(2014) S. D. Pandey et al.   MICROBIOLOGY-SGM

Acquired Resistance of Mycobacterium tuberculosis to Bedaquiline

(2014) Koen Andries et al.   PLoS One

Self-poisoning ofMycobacterium tuberculosisby interrupting siderophore recycling

(2014) Christopher M. Jones et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting Mycobacterium tuberculosis nucleoid-associated protein HU with structure-based inhibitors

(2014) Tuhin Bhowmick et al.   Nature Communications

A Trojan Horse Strategy to Deliver Amikacin to Mycobacterial Granulomas

(2013) Ana Montes-Worboys et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

Pharmacokinetic andIn VivoEfficacy Studies of the Mycobactin Biosynthesis Inhibitor Salicyl-AMS in Mice

(2013) Shichun Lun et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Iron in Infection and Immunity

(2013) James E. Cassat et al.   Cell Host & Microbe

IdeR is required for iron homeostasis and virulence inMycobacterium tuberculosis

(2013) Ruchi Pandey et al.   MOLECULAR MICROBIOLOGY

4′-Phosphopantetheinyl Transferase PptT, a New Drug Target Required for Mycobacterium tuberculosis Growth and Persistence In Vivo

(2013) Cécile Leblanc et al.   PLoS Pathogens

Discovery of a Siderophore Export System Essential for Virulence of Mycobacterium tuberculosis

(2013) Ryan M. Wells et al.   PLoS Pathogens

Implications of Binding Mode and Active Site Flexibility for Inhibitor Potency against the Salicylate Synthase from Mycobacterium tuberculosis

(2012) Gamma Chi et al.   BIOCHEMISTRY

Analyses of MbtB, MbtE, and MbtF Suggest Revisions to the Mycobactin Biosynthesis Pathway in Mycobacterium tuberculosis

(2012) M. D. McMahon et al.   JOURNAL OF BACTERIOLOGY

Inhibition of mycolic acid transport across the Mycobacterium tuberculosis plasma membrane

(2012) Anna E Grzegorzewicz et al.   Nature Chemical Biology

Syntheses of mycobactin analogs as potent and selective inhibitors of Mycobacterium tuberculosis

(2012) Raúl E. Juárez-Hernández et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Totally Drug-Resistant Tuberculosis in India

(2011) Z. F. Udwadia et al.   CLINICAL INFECTIOUS DISEASES

Mutational and Phylogenetic Analyses of the Mycobacterial mbt Gene Cluster

(2011) S. S. Chavadi et al.   JOURNAL OF BACTERIOLOGY

Design, Synthesis, and Study of a Mycobactin−Artemisinin Conjugate That Has Selective and Potent Activity against Tuberculosis and Malaria

(2011) Marvin J. Miller et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibitors of the Salicylate Synthase (MbtI) from Mycobacterium tuberculosis Discovered by High-Throughput Screening

(2010) Mahalakshmi Vasan et al.   ChemMedChem

Structure–activity relationship of new anti-tuberculosis agents derived from oxazoline and oxazole benzyl esters

(2010) Garrett C. Moraski et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Utilization of the Suzuki Coupling to Enhance the Antituberculosis Activity of Aryloxazoles

(2010) Marvin J. Miller et al.   HETEROCYCLES

Efflux-Mediated Drug Resistance in Bacteria

(2009) Xian-Zhi Li et al.   DRUGS

Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis

(2008) Karen L. Stirrett et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Mycobacterium tuberculosis IdeR is a dual functional regulator that controls transcription of genes involved in iron acquisition, iron storage and survival in macrophages

(2003) Benjamin Gold et al.   MOLECULAR MICROBIOLOGY