The Mycobactin biosynthesis pathway: A prospective therapeutic target in the battle against tuberculosis

M Shyam, D Shilkar, H Verma, A Dev… - Journal of Medicinal …, 2020 - ACS Publications
The alarming rise in drug-resistant clinical cases of tuberculosis (TB) has necessitated the
rapid development of newer chemotherapeutic agents with novel mechanisms of action. The …

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

M Shyam, D Shilkar, G Rakshit… - Expert opinion on drug …, 2022 - Taylor & Francis
Introduction Several decades of antitubercular drug discovery efforts have focused on novel
antitubercular chemotherapies. However, recent efforts have greatly shifted toward …

Breaking a pathogen's iron will: Inhibiting siderophore production as an antimicrobial strategy

AL Lamb - Biochimica et Biophysica Acta (BBA)-Proteins and …, 2015 - Elsevier
The rise of antibiotic resistance is a growing public health crisis. Novel antimicrobials are
sought, preferably developing nontraditional chemical scaffolds that do not inhibit standard …

In Silico Strategies in Tuberculosis Drug Discovery

SJY Macalino, JB Billones, VG Organo, MCO Carrillo - Molecules, 2020 - mdpi.com
Tuberculosis (TB) remains a serious threat to global public health, responsible for an
estimated 1.5 million mortalities in 2018. While there are available therapeutics for this …

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

LR Chiarelli, M Mori, D Barlocco, G Beretta… - European journal of …, 2018 - Elsevier
We report on the virtual screening, synthesis, and biological evaluation of new furan
derivatives targeting Mycobacterium tuberculosis salicylate synthase (MbtI). A receptor …

Advances in menaquinone biosynthesis: sublocalisation and allosteric regulation

JM Johnston, EMM Bulloch - Current opinion in structural biology, 2020 - Elsevier
Highlights•Menaquinones (MKs) are involved in bacterial electron transport and
adaptation.•The Men pathway is the most predominant of two bacterial pathways to make …

The tryptophan biosynthetic pathway is essential for Mycobacterium tuberculosis to cause disease

JS Lott - Biochemical Society Transactions, 2020 - portlandpress.com
Mycobacterium tuberculosis, the causative agent of tuberculosis (TB), is the most significant
cause of death from a single infectious agent worldwide. Antibiotic-resistant strains of M …

Targeting Mycobacterium tuberculosis iron-scavenging tools: A recent update on siderophores inhibitors

G Kumar, PA Adhikrao - RSC Medicinal Chemistry, 2023 - pubs.rsc.org
Among the various bacterial infections, tuberculosis (TB) remains a life-threatening
infectious disease responsible as the most significant cause of mortality and morbidity …

Drug Discovery for Mycobacterium tuberculosis Using Structure-Based Computer-Aided Drug Design Approach

MA Ejalonibu, SA Ogundare, AA Elrashedy… - International Journal of …, 2021 - mdpi.com
Developing new, more effective antibiotics against resistant Mycobacterium tuberculosis that
inhibit its essential proteins is an appealing strategy for combating the global tuberculosis …

When does chemical elaboration induce a ligand to change its binding mode?

S Malhotra, J Karanicolas - Journal of medicinal chemistry, 2017 - ACS Publications
Traditional hit-to-lead optimization assumes that upon elaboration of chemical structure, the
ligand retains its binding mode relative to the receptor. Here, we build a large-scale …