Metallodrugs are unique: Opportunities and challenges of discovery and development

EJ Anthony, EM Bolitho, HE Bridgewater… - Chemical …, 2020 - pubs.rsc.org
Metals play vital roles in nutrients and medicines and provide chemical functionalities that
are not accessible to purely organic compounds. At least 10 metals are essential for human …

Next generation gold drugs and probes: chemistry and biomedical applications

RT Mertens, S Gukathasan, AS Arojojoye… - Chemical …, 2023 - ACS Publications
The gold drugs, gold sodium thiomalate (Myocrisin), aurothioglucose (Solganal), and the
orally administered auranofin (Ridaura), are utilized in modern medicine for the treatment of …

[HTML][HTML] The ferroptosis inducing compounds RSL3 and ML162 are not direct inhibitors of GPX4 but of TXNRD1

DM Cheff, C Huang, KC Scholzen, R Gencheva… - Redox Biology, 2023 - Elsevier
Ferroptosis is defined as cell death triggered by iron-dependent lipid peroxidation that is
preventable by antioxidant compounds such as ferrostatin-1. Endogenous suppressors of …

Molecular mechanisms and clinical implications of the gold drug auranofin

S Shen, J Shen, Z Luo, F Wang, J Min - Coordination Chemistry Reviews, 2023 - Elsevier
Auranofin (AUR) is an orally available lipophilic gold-based anti-inflammatory compound
used for the treatment of rheumatoid arthritis (RA). Recent evidence indicates that AUR may …

Recent advances in identifying protein targets in drug discovery

J Ha, H Park, J Park, SB Park - Cell chemical biology, 2021 - cell.com
Phenotype-based screening has emerged as an alternative route for discovering new
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …

[HTML][HTML] Auranofin reveals therapeutic anticancer potential by triggering distinct molecular cell death mechanisms and innate immunity in mutant p53 non-small cell …

LF Boullosa, J Van Loenhout, T Flieswasser… - Redox biology, 2021 - Elsevier
Auranofin (AF) is an FDA-approved antirheumatic drug with anticancer properties that acts
as a thioredoxin reductase 1 (TrxR) inhibitor. The exact mechanisms through which AF …

Upgrade of an old drug: Auranofin in innovative cancer therapies to overcome drug resistance and to increase drug effectiveness

T Gamberi, G Chiappetta, T Fiaschi… - Medicinal Research …, 2022 - Wiley Online Library
Auranofin is an oral gold (I) compound, initially developed for the treatment of rheumatoid
arthritis. Currently, Auranofin is under investigation for oncological application within a drug …

Drug target identification in tissues by thermal proteome profiling

A Mateus, N Kurzawa, J Perrin… - Annual Review of …, 2022 - annualreviews.org
Drug target deconvolution can accelerate the drug discovery process by identifying a drug's
targets (facilitating medicinal chemistry efforts) and off-targets (anticipating toxicity effects or …

Computational analyses of mechanism of action (MoA): data, methods and integration

MA Trapotsi, L Hosseini-Gerami, A Bender - RSC chemical biology, 2022 - pubs.rsc.org
The elucidation of a compound's Mechanism of Action (MoA) is a challenging task in the
drug discovery process, but it is important in order to rationalise phenotypic findings and to …

[HTML][HTML] Methods to identify protein targets of metal-based drugs

L Skos, Y Borutzki, C Gerner… - Current Opinion in …, 2023 - Elsevier
Metal-based anticancer agents occupy a distinct chemical space due to their particular
coordination geometry and reactivity. Despite the initial DNA-targeting paradigm for this …