Small organic molecules targeting the energy metabolism of Mycobacterium tuberculosis

M Urban, V Šlachtová, L Brulikova - European Journal of Medicinal …, 2021 - Elsevier
Causing approximately 10 million incident cases and 1.3–1.5 million deaths every year,
Mycobacterium tuberculosis remains a global health problem. The risk is further …

Allosteric inhibition of LRRK2, where are we now

A Soliman, FN Cankara, A Kortholt - Biochemical Society …, 2020 - portlandpress.com
Parkinson's disease (PD) is the second most common neurodegenerative disease. In recent
years, it has been shown that leucine-rich repeat kinase 2 (LRRK2) has a crucial function in …

Tricyclic SpiroLactams kill mycobacteria in vitro and in vivo by inhibiting type II NADH dehydrogenases

S Dam, S Tangara, C Hamela, T Hattabi… - Journal of Medicinal …, 2022 - ACS Publications
It is critical that novel classes of antituberculosis drugs are developed to combat the
increasing burden of infections by multidrug-resistant strains. To identify such a novel class …

FAD/NADH dependent oxidoreductases: from different amino acid sequences to similar protein shapes for playing an ancient function

L Trisolini, N Gambacorta, R Gorgoglione… - Journal of Clinical …, 2019 - mdpi.com
Flavoprotein oxidoreductases are members of a large protein family of specialized
dehydrogenases, which include type II NADH dehydrogenase, pyridine nucleotide …

Counting on fragment based drug design approach for drug discovery

A Kashyap, PK Singh, O Silakari - Current Topics in Medicinal …, 2018 - ingentaconnect.com
Fragment based drug design (FBDD) is a structure guided ligand design approach used in
the process of drug discovery. It involves identification of low molecular weight fragments as …

Uncovering interactions between mycobacterial respiratory complexes to target drug-resistant Mycobacterium tuberculosis

MB McNeil, CY Cheung, NJE Waller… - Frontiers in Cellular …, 2022 - frontiersin.org
Mycobacterium tuberculosis remains a leading cause of infectious disease morbidity and
mortality for which new drug combination therapies are needed. Mycobacterial …

Inhibitors of enzymes in the electron transport chain of Mycobacterium tuberculosis

AM Thompson, WA Denny - Annual reports in medicinal chemistry, 2019 - Elsevier
The increasing prevalence of drug resistant tuberculosis has created an urgent need for new
antibiotics with novel modes of action. New drug targets include various enzymes in the …

Implications of fragment-based drug discovery in tuberculosis and HIV

MK Mallakuntla, NS Togre, DB Santos, S Tiwari - Pharmaceuticals, 2022 - mdpi.com
Tuberculosis (TB) remains a global health problem and the emergence of HIV has further
worsened it. Long chemotherapy and the emergence of drug-resistance strains of …

Synthesis of Functionalised Chromonyl‐pyrimidines and Their Potential as Antimycobacterial Agents

KT Santoso, MW Brett, CY Cheung, GM Cook… - …, 2020 - Wiley Online Library
Drug‐resistant strains of Mycobacterium tuberculosis are on the rise and have resulted in an
urgent need to develop new tuberculosis (TB) drugs. Herein, the development of chromonyl …

Cheminformatics techniques in antimalarial drug discovery and development from natural products 1: Basic concepts

S Egieyeh, SF Malan, A Christoffels - Physical Sciences Reviews, 2019 - degruyter.com
A large number of natural products, especially those used in ethnomedicine of malaria, have
shown varying in vitro antiplasmodial activities. Facilitating antimalarial drug development …