Tuberculosis drug discovery: challenges and new horizons

GFS Fernandes, AM Thompson… - Journal of Medicinal …, 2022 - ACS Publications
Over the past 2000 years, tuberculosis (TB) has claimed more lives than any other infectious
disease. In 2020 alone, TB was responsible for 1.5 million deaths worldwide, comparable to …

Targeting mycobacterial membranes and membrane proteins: Progress and limitations

G Kumar, S Kapoor - Bioorganic & Medicinal Chemistry, 2023 - Elsevier
Among the various bacterial infections, tuberculosis continues to hold center stage. Its
causative agent, Mycobacterium tuberculosis, possesses robust defense mechanisms …

[PDF][PDF] Cryo-EM structure and resistance landscape of M. tuberculosis MmpL3: An emergent therapeutic target

O Adams, JC Deme, JL Parker, PW Fowler, SM Lea… - Structure, 2021 - cell.com
Tuberculosis (TB) is the leading cause of death from a single infectious agent and in 2019
an estimated 10 million people worldwide contracted the disease. Although treatments for …

Identification of anti-mycobacterial agents against mmpL3: virtual screening, ADMET analysis and MD simulations

KA Bhakhar, ND Gajjar, KB Bodiwala, DK Sureja… - Journal of Molecular …, 2021 - Elsevier
Tuberculosis has been the communicable disease being one of the top 10 causes of deaths
worldwide and the leading cause of deaths from a single infectious agent (ranking above …

MmpL3 inhibition: a new approach to treat nontuberculous mycobacterial infections

JP Sethiya, MA Sowards, M Jackson… - International journal of …, 2020 - mdpi.com
Outside of Mycobacterium tuberculosis and Mycobacterium leprae, nontuberculous
mycobacteria (NTM) are environmental mycobacteria (> 190 species) and are classified as …

Molecular mechanisms of MmpL3 function and inhibition

JT Williams, RB Abramovitch - Microbial Drug Resistance, 2023 - liebertpub.com
Mycobacteria species include a large number of pathogenic organisms such as
Mycobacterium tuberculosis, Mycobacterium leprae, and various non-tuberculous …

Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening

A Kumar, S Chettiar, BS Brown, J Early, J Ollinger… - Scientific Reports, 2022 - nature.com
We performed a high-throughput phenotypic whole cell screen of Mycobacterium
tuberculosis against a diverse chemical library of approximately 100,000 compounds from …

Synthesis, biological evaluation and docking studies of silicon incorporated diarylpyrroles as MmpL3 inhibitors: An effective strategy towards development of potent …

N Vasudevan, Z Motiwala, R Ramesh, SB Wagh… - European Journal of …, 2023 - Elsevier
Growing global demand for new molecules to treat tuberculosis has created an urgent need
to develop novel strategies to combat the menace. BM212 related compounds were found to …

The Mycobacterium tuberculosis MmpL3 inhibitor MSU-43085 is active in a mouse model of infection

JT Williams, M Giletto, ER Haiderer, B Aleiwi… - Microbiology …, 2024 - Am Soc Microbiol
Addressing drug resistance in Mycobacterium tuberculosis (Mtb) requires the development
of new drugs with new targets. We previously identified 13 MmpL3 inhibitors from a screen …

Discovery and biological evaluation of an adamantyl-amide derivative with likely MmpL3 inhibitory activity

E Kapp, H Calitz, EM Streicher, A Dippenaar… - Tuberculosis, 2023 - Elsevier
A series of molecules containing bulky lipophilic scaffolds was screened for activity against
Mycobacterium tuberculosis and a number of compounds with antimycobacterial activity …