The glomerular filtration barrier: a structural target for novel kidney therapies

IS Daehn, JS Duffield - Nature Reviews Drug Discovery, 2021 - nature.com
Loss of normal kidney function affects more than 10% of the population and contributes to
morbidity and mortality. Kidney diseases are currently treated with immunosuppressive …

Clofazimine for the treatment of tuberculosis

JAM Stadler, G Maartens, G Meintjes… - Frontiers in …, 2023 - frontiersin.org
Shorter (6–9 months), fully oral regimens containing new and repurposed drugs are now the
first-choice option for the treatment of drug-resistant tuberculosis (DR-TB). Clofazimine, long …

Dose predictions for drug design

TS Maurer, D Smith, K Beaumont… - Journal of Medicinal …, 2020 - ACS Publications
The efficacious dose of a drug is perhaps the most holistic metric reflecting its therapeutic
potential. Dose is predicted at many stages in drug discovery and development. Prior to the …

Critical assessment of artificial intelligence methods for prediction of hERG channel inhibition in the “big data” era

VB Siramshetty, DT Nguyen, NJ Martinez… - Journal of Chemical …, 2020 - ACS Publications
The rise of novel artificial intelligence (AI) methods necessitates their benchmarking against
classical machine learning for a typical drug-discovery project. Inhibition of the potassium …

Modified curcumins as potential drug candidates for breast cancer: An overview

AL Flint, DW Hansen, LVD Brown, LE Stewart, E Ortiz… - Molecules, 2022 - mdpi.com
Breast cancer (BC), the most common malignancy in women, results from significant
alterations in genetic and epigenetic mechanisms that alter multiple signaling pathways in …

[HTML][HTML] Addressing antimicrobial resistance with the IDentif. AI platform: Rapidly optimizing clinically actionable combination therapy regimens against …

D Mukherjee, P Wang, L Hooi, V Sandhu, K You… - Theranostics, 2022 - ncbi.nlm.nih.gov
Background: Current standard of care (SOC) regimens against nontuberculous
mycobacteria (NTM) usually result in unsatisfactory therapeutic responses, primarily due to …

Molecular hybridization of alkaloids using 1, 2, 3-triazole-based click chemistry

D Buchanan, AM Pham, SK Singh, SS Panda - Molecules, 2023 - mdpi.com
Alkaloids found in multiple species, known as 'driver species', are more likely to be included
in early-stage drug development due to their high biodiversity compared to rare alkaloids …

Optimization of the urea linker of triazolopyridazine MMV665917 results in a new anticryptosporidial lead with improved potency and predicted hERG safety margin

E Oboh, TJ Schubert, JE Teixeira… - Journal of medicinal …, 2021 - ACS Publications
Cryptosporidiosis is caused by infection of the small intestine by Cryptosporidium parasites,
resulting in severe diarrhea, dehydration, malabsorption, and potentially death. The only …

QT prolongation in the STREAM stage 1 trial

G Hughes, H Bern, CY Chiang… - … of Tuberculosis and …, 2022 - ingentaconnect.com
BACKGROUND: STREAM (Standardized Treatment Regimen of Anti-TB Drugs for Patients
with MDR-TB) Stage 1 demonstrated non-inferior efficacy of a shortened regimen (the Short …

[HTML][HTML] Human ileal organoid model recapitulates clinical incidence of diarrhea associated with small molecule drugs

DG Belair, RJ Visconti, M Hong, M Marella, MF Peters… - Toxicology in Vitro, 2020 - Elsevier
Drug-induced gastrointestinal toxicity (GIT) is a common treatment-emergent adverse event
that can negatively impact dosing, thereby limiting efficacy and treatment options for …