19.10.2021
New paper on total synthesis of Trabectidin degradation product ETM-204
In our newest publication, we describe the first total synthesis of ETM-204, which is a metabolite of the chemotherapeutic agent Trabectidin (Yondelis®). Key step of the synthesis is a modified Pomeranz–Fritsch cyclization to assemble the isoquinoline ring. The paper was published in Monatshefte für Chemie.
https://link.springer.com/article/10.1007/s00706-021-02844-1
27.07.2021
New paper on transition-state based inhibitors of DPP3
In this study, published in Chemistry – A European Journal, we disclose the design, synthesis and biophysical characterization of peptidomimetic inhibitors of dipeptidyl peptidase III (DPP3). The inhibition of this metalloprotease is based on the entropy-driven release of water from the closing binding cleft as confirmed by ITC measurement and X-ray crystallography.
https://chemistry-europe.onlinelibrary.wiley.com/doi/epdf/10.1002/chem.202102204
11.12.2020
Review on water-soluble phosphorus ligands
Hydrophilic phosphorus ligands are crucial for transition metal-catalyzed reactions in water or biphasic solvents. In our latest review, published in Advanced Synthesis & Catalysis, we summarize the progress in the synthesis of novel water-soluble phosphines over the past decade. Additionally, we describe recent applications of transition metal catalysis in aqueous solvents based on hydrophilic P-donor ligands.
https://onlinelibrary.wiley.com/doi/10.1002/adsc.202001278
02.09.2020
Review on ABPP of Oxidoreductases
This minireview summarizes state of the art approaches for the activity-based protein profiling (ABPP) of oxidoreductases and discusses the scope and limitations of established methodologies.
https://chemistry-europe.onlinelibrary.wiley.com/doi/abs/10.1002/cbic.202000542
15.07.2020
New paper on SAR studies of ATGL inhibitors
In our latest publication in Bioorganic & Medicinal Chemistry, we disclose structure–activity relationship (SAR) studies of small molecule inhibitors of murine adipose triglyceride lipase (mATGL) that resulted in the development of Atglistatin as powerful tool compound.
https://www.sciencedirect.com/science/article/pii/S0968089620304405
04.05.2020
New paper on stereoselective synthesis of thiol-containing 1,2-aminoalcohols
In this contribution published in Tetrahedron, we report a synthetic protocol for the stereoselective preparation of highly functionalized aminohydroxythiols. The methodology is based on a SmI2/LiBr-mediated reductive coupling of Ellman N-sulfinylimines with aldehydes.
https://www.sciencedirect.com/science/article/pii/S0040402020303926
19.03.2020
New publication on alpha-helix mimetics
In this study a highly modular synthesis of quateraryl alpha-helix mimetics as inhibitors for protein-protein interactions (PPIs) is presented. The combination of an electroorganic as well as a Pd-catalyzed cross-coupling provides efficient access to quaterarylic systems. This work was published in Catalysts.
https://www.mdpi.com/2073-4344/10/3/340
06.03.2020
Congratulations to Anna Migglautsch
Anna Migglautsch just defended her PhD thesis on “Development of inhibitors of human adipose triglyceride lipase (hATGL)”. We want to thank her for the last years in which she became an essential member of the Institute and congratulate on doing an amazing job at her defense!
06.01.2020
Press release on drug development
The Austrian Research Promotion Agency (FFG) just published a press release on the development of a drug candidate for diabetes treatment. This joint research project between the Institute of Molecular Biosciences (University of Graz) and the Institute of Organic Chemistry (TU Graz) focuses on the synthesis of small molecule inhibitors of the adipolytic enzyme ATGL.
https://www.ffg.at/sites/default/files/allgemeine_downloads/strukturprogramme/RSA/RSA_Studios_A3_Atglistatin.pdf
07.11.2019
New study on highly selective Pd-catalyzed S-allylation
In our latest publication we disclose a palladium-catalyzed protocol for the highly chemo- as well as regioselective S-allylation of thiols. This transformation developed at the Institute of Organic Chemistry offers several advantages over established reaction for the synthesis of thioethers. The paper was published in Advanced Synthesis & Catalysis and highlighted as “very important publication”!
https://onlinelibrary.wiley.com/doi/full/10.1002/adsc.201901250
11.10.2019
Press release on new method for the synthesis of lipidated proteins
TU Graz just published a press release on the development of a new method for the site-selective lipidation of proteins. This palladium-mediated reaction was developed at the Institute of Organic Chemistry (TU Graz) in collaboration with the Institute of Biological Chemistry (University of Vienna) and recently published in the Journal of American Chemical Society.
https://www.tugraz.at/en/tu-graz/services/news-stories/media-service/singleview/article/neues-verfahren-zur-schnelleren-und-einfacheren-herstellung-lipidierter-proteine0/
