Explanipedia

Towards the Use of Metabolic Volatiles in Breath for Determining Drug Response: Gstachamine as an Unlabeled Substrate to Measure CYP3A4 Activity Open

Valentina Stock, Rebecca Hofer, Klaus R. Liedl, Jakob Troppmair, Thierry Langer , et al. · 2025

Breath analysis is a promising noninvasive diagnostic tool, but the clinical applicability of breath tests depends on several factors. A salient criterion pertains to the presence of substrates with the ability to produce detectable volati…

Diisopromine as a non-labelled CYP3A4 substrate: Implications for breath test development Open

Valentina Stock, R Höfer, Vera A. Spanke, Klaus R. Liedl, Jakob Troppmair , et al. · 2025

Breath tests for the prediction of patient-specific drug response require suitable substrates that when metabolised in the human body yield specific, unlabelled volatile metabolites. This study explores diisopromine as a potential substrat…

ATG8ylation of vacuolar membrane protects plants against cell wall damage Open

Jose Julian, Peng Gao, Alessia Del Chiaro, Juan Carlos De la Concepción, Laia Armengot , et al. · 2025

Vacuoles are essential for cellular metabolism and growth and the maintenance of internal turgor pressure. They sequester lytic enzymes, ions and secondary metabolites that, if leaked into the cytosol, could lead to cell death. Despite the…

Tolterodine is a novel candidate for assessing CYP3A4 activity through metabolic volatiles to predict drug responses Open

Valentina Stock, R Höfer, Franziska Lochmann, Vera A. Spanke, Klaus R. Liedl , et al. · 2025

ATG8ylation of vacuolar membrane protects plants against cell wall damage Open

Jose Julian, Peng Gao, Alessia Del Chiaro, Juan Carlos De la Concepción, Laia Armengot , et al. · 2024

Vacuoles are essential for cellular metabolism, growth, and the maintenance of internal turgor pressure. They sequester lytic enzymes, ions, and secondary metabolites that, if leaked into the cytosol, could lead to cell death. Despite thei…

Syntheses, reactivity, and biological applications of coumarins Open

Andrea Citarella, Serena Vittorio, Christian Dank, Laura Ielo · 2024

This comprehensive review, covering 2021–2023, explores the multifaceted chemical and pharmacological potential of coumarins, emphasizing their significance as versatile natural derivatives in medicinal chemistry. The synthesis and functio…

Discovery and Characterization of a Chemical Probe Targeting the Zinc-Finger Ubiquitin-Binding Domain of HDAC6 Open

Rachel Harding, Ivan Franzoni, Mandeep Mann, Magdalena M. Szewczyk, Bijan Mirabi , et al. · 2023

Histone deacetylase 6 (HDAC6) inhibition is an attractive strategy for treating numerous cancers, and HDAC6 catalytic inhibitors are currently in clinical trials. The HDAC6 zinc-finger ubiquitin-binding domain (UBD) binds free C-terminal d…

Heterocyclic Compounds as Synthetic Tyrosinase Inhibitors: Recent Advances Open

Serena Vittorio, Christian Dank, Laura Ielo · 2023

Tyrosinase is a copper-containing enzyme which is widely distributed in nature (e.g., bacteria, mammals, fungi) and involved in two consecutive steps of melanin biosynthesis. In humans, an excessive production of melanin can determine hype…

Synthetic Ionizable Colloidal Drug Aggregates Enable Endosomal Disruption Open

Eric N. Donders, Kai V. Slaughter, Christian Dank, Ahil N. Ganesh, Brian K. Shoichet , et al. · 2023

Colloidal drug aggregates enable the design of drug‐rich nanoparticles; however, the efficacy of stabilized colloidal drug aggregates is limited by entrapment in the endo‐lysosomal pathway. Although ionizable drugs are used to elicit lysos…

Discovery and characterization of a chemical probe targeting the zinc-finger ubiquitin-binding domain of HDAC6 Open

Rachel Harding, Ivan Franzoni, Mandeep Mann, Magdalena M. Szewczyk, Bijan Mirabi , et al. · 2023

Histone deacetylase 6 (HDAC6) inhibition is an attractive strategy for treating numerous cancers, and HDAC6 catalytic inhibitors are currently in clinical trials. The HDAC6 zinc-finger ubiquitin-binding domain (UBD) binds free C-terminal d…

Discovery and characterization of a chemical probe targeting the zinc-finger ubiquitin-binding domain of HDAC6 Open

Rachel Harding, Ivan Franzoni, Mandeep Mann, Magdalena M. Szewczyk, Bijan Mirabi , et al. · 2023

These data are the R scripts, environments, output used for analyzing chemoproteomics data. The volcano plot shown in the manuscript is based on the DEP R package. To validate the enrichment output from DEP, the proteomics data was also pr…

Recent advances in the accessibility, synthetic utility, and biological applications of aziridines Open

Christian Dank, Laura Ielo · 2023

Recent methodologies regarding the syntheses and transformations of aziridine bearing compounds are presented as well as their biological activities.

CCDC 1956222: Experimental Crystal Structure Determination Open

Nicolas Zeidan, Matthew T. Zambri, Sven Unger, Christian Dank, Alexa Torelli , et al. · 2020

Synthesis and Reactions of 3,3-Difluoro-2-<i>exo</i>-methylidene Indolines Open

Nicolas Zeidan, Matthew T. Zambri, Sven Unger, Christian Dank, Alexa Torelli , et al. · 2020

A dearomative electrophilic fluorination of 2-methylindoles is reported, delivering 3,3-difluoroindolines bearing an exomethylidene. The model substrate was synthesized on up to a 20 mmol scale and was purified by a practical recrystalliza…

CCDC 1973089: Experimental Crystal Structure Determination Open