The zinc finger domains of PARP-1 are selectively and potently inhibited by the Au(I)-based drugs sodium aurothiomalate and aurothioglucose. [PDF]
PARP‐1 is a key enzyme in the DNA damage response, and its inhibition induces cancer cell death via synthetic lethality. Au(I)‐based drugs, such as aurothioglucose and sodium aurothiomalate, block PARP‐1's DNA‐dependent activity by targeting its zinc finger domains.
Bashtanova U, Duer MJ.
europepmc +2 more sources
Harnessing Organometallic Au(III) Complexes as Precision Scaffolds for Next-Generation Therapeutic and Imaging Agents. [PDF]
Cyclometalated gold(III) complexes offer a versatile platform for selective biological interactions, including cysteine arylation, redox modulation, and enzyme inhibition. This review explores their roles in anticancer, antimicrobial, and protein modification strategies, highlighting their ability to disrupt metabolic pathways, modulate aquaporins, and
Thomas SR, Bonsignore R.
europepmc +2 more sources
Disruption of disulfides within RBD of SARS-CoV-2 spike protein prevents fusion and represents a target for viral entry inhibition by registered drugs. [PDF]
Abstract The SARS‐CoV‐2 pandemic imposed a large burden on health and society. Therapeutics targeting different components and processes of the viral infection replication cycle are being investigated, particularly to repurpose already approved drugs. Spike protein is an important target for both vaccines and therapeutics.
Manček-Keber M +11 more
europepmc +2 more sources
DP1 Receptor Blockade Attenuates Microglial Senescence and Cognitive Decline Caused by PTGDS in Exosomes From Aged Brains. [PDF]
DP1 receptor blockade attenuates microglial senescence and cognitive decline caused by PTGDS in exosomes from aged brains. ABSTRACT Aging leads to neurodegenerative diseases, such as cognitive decline, which are induced by persistent chronic low‐grade inflammation in the brain driven by microglial activation.
Liu Y +12 more
europepmc +2 more sources
Chemical Structure Elucidation in the Development of Inorganic Drugs: Evidence from Ru-, Au-, As-, and Sb-based Medicines. [PDF]
The importance of molecular structure elucidation in medicinal inorganic chemistry drug development is discussed and illustrated using three vignettes on Ru‐, Au‐, and As‐based drugs. An outlook on Sb‐based drugs is provided. The development of three classes of medicinal inorganic compounds is reviewed, highlighting the important role of structure ...
Lance-Byrne A +2 more
europepmc +2 more sources
Gold Complexes in Anticancer Therapy: From New Design Principles to Particle‐Based Delivery Systems
Gold compounds have attracted considerable interest as anticancer drugs. However, the clinical translation of this class of compounds is hampered by suboptimal pharmacological performance. To address this problem, strategies based on molecular design principles have been the primary focus.
Guillermo Moreno‐Alcántar +2 more
wiley +2 more sources
Abstract INTRODUCTION Extracellular vesicles (EVs) have been implicated in the spread of neuropathology in Alzheimer's disease (AD), but their involvement in behavioral outcomes linked to AD remains to be determined. METHODS EVs isolated from post mortem brain tissue from control, AD, or frontotemporal dementia (FTD) donors, as well as from APP/PS1 ...
Victor Bodart‐Santos +13 more
wiley +1 more source
Background – Mycophenolate mofetil (MMF) is the prodrug of mycophenolic acid (MPA) which acts as an immunosuppressive agent. During the biotransformation of MMF to MPA, additional metabolites including MPA phenol glucuronide (MPAG), MPA acyl glucuronide (AcMPAG) and MPA phenol glucoside (MPG) are formed.
Dylan L. Burroughs +6 more
wiley +1 more source
Mammalian cells can synthesize nanoparticles from ions from gold salts. Gold salt drugs have been clinically applied for nearly a century, with evidence of nanoparticle formation within those patients. However, the mainstream use of these gold drugs considerably predates popular study of gold particles.
Aaron S. Schwartz‐Duval +1 more
wiley +1 more source
Abstract 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 repurposing plan due to the relevant antineoplastic activity observed both in vitro and in vivo tumor models.
Tania Gamberi +5 more
wiley +1 more source

