[HTML][HTML] Recent advances in metabolomics analysis for early drug development

JC Alarcon-Barrera, S Kostidis, A Ondo-Mendez… - Drug discovery today, 2022 - Elsevier
Highlights•Metabolomics has become a widely applied tool in drug development.•
Metabolomics plays a key role for the identification of physiological response markers.• …

Modes‐of‐action of antifungal compounds: Stressors and (target‐site‐specific) toxins, toxicants, or toxin–stressors

D Noel, JE Hallsworth, E Gelhaye… - Microbial …, 2023 - Wiley Online Library
Fungi and antifungal compounds are relevant to the United Nation's Sustainable
Development Goals. However, the modes‐of‐action of antifungals—whether they are …

Cholesterol metabolism is a druggable axis that independently regulates tau and amyloid-β in iPSC-derived Alzheimer's disease neurons

R van der Kant, VF Langness, CM Herrera… - Cell stem cell, 2019 - cell.com
Genetic, epidemiologic, and biochemical evidence suggests that predisposition to
Alzheimer's disease (AD) may arise from altered cholesterol metabolism, although the …

Targeting fungal membrane homeostasis with imidazopyrazoindoles impairs azole resistance and biofilm formation

NM Revie, KR Iyer, ME Maxson, J Zhang, S Yan… - Nature …, 2022 - nature.com
Fungal infections cause more than 1.5 million deaths annually. With an increase in immune-
deficient susceptible populations and the emergence of antifungal drug resistance, there is …

Toxic eburicol accumulation drives the antifungal activity of azoles against Aspergillus fumigatus

H Elsaman, E Golubtsov, S Brazil, N Ng… - Nature …, 2024 - nature.com
Azole antifungals inhibit the sterol C14-demethylase (CYP51/Erg11) of the ergosterol
biosynthesis pathway. Here we show that the azole-induced synthesis of fungicidal cell wall …

[HTML][HTML] Lipidomics analysis in drug discovery and development

S Kostidis, E Sánchez-López, M Giera - Current Opinion in Chemical …, 2023 - Elsevier
Despite being a relatively new addition to the Omics' landscape, lipidomics is increasingly
being recognized as an important tool for the identification of druggable targets and …

The cytochrome P450 reductase CprA is a rate-limiting factor for Cyp51A-mediated azole resistance in Aspergillus fumigatus

A Kühbacher, P Merschak, H Haas… - Antimicrobial Agents …, 2023 - Am Soc Microbiol
Azole antifungals remain the “gold standard” therapy for invasive aspergillosis. The world-
wide emergence of isolates resistant to this drug class, however, developed into a steadily …

A gas chromatography–mass spectrometry-based whole-cell screening assay for target identification in distal cholesterol biosynthesis

C Müller, J Junker, F Bracher, M Giera - Nature protocols, 2019 - nature.com
Distal cholesterol biosynthesis (CB) has recently taken center stage as a promising drug
target in several diseases previously not linked to this biochemical pathway, including …

Discovery of Novel Sertraline Derivatives as Potent Anti-Cryptococcus Agents

W Li, Z Yun, C Ji, J Tu, W Yang, J Li… - Journal of Medicinal …, 2022 - ACS Publications
Treatment of life-threatening cryptococcal meningitis (CM) is highly challenging due to the
limited efficacy of the available antifungal drugs. Antidepressant sertraline (SER) has been …

Essential oils and their components are a class of antifungals with potent vapour-phase-mediated anti-Candida activity

AF Feyaerts, L Mathé, W Luyten, S De Graeve… - Scientific reports, 2018 - nature.com
Multi-resistant microorganisms continue to challenge medicine and fuel the search for new
antimicrobials. Here we show that essential oils and their components are a promising class …