02.02.2024

Congratulations to Till Schreiner

Till Schreiner just defended his PhD thesis on “Chemical Synthesis as a Means
Towards a Deeper Understanding of Lipid Metabolism”. We want to thank him for
the last years in which he became an essential member of the Institute and
congratulate on doing a marvellous at his defense!

24.01.2024

New Paper on Cofactor Specificity in the FMN-dependent Family of Ene-reductases

In this collaboration, published in The FEBS Journal, we postulate that cofactor specificity is determined by the arginine triad/loop 6 and the residue(s) controlling access to a hydrophobic cleft formed by the β-hairpin flap. Our results suggest that in order to switch the coenzyme preference in NADPH-dependent OYEs, the β-hairpin flap region needs to be targeted by structure-based engineering approaches to create a high-affinitybinding site for NADH, for example, by replacing L140 for an adenine ring-stabilizing phenylalanine andadjusting the length of the hairpin so that it resembles more that of NADH-preferring ERs. Conversely, loop 6 should be the engineering target to switch the nico-tinamide affinity in NADH-dependent OYEs. Generation of such SlOPR3 variants with switched coenzyme preference is currently underway.

06.01.2024

New Paper on Design, Synthesis and Catalytic Application of Water-soluble 1,1′-Bis(diphenylphosphino)ferrocene Ligands

In our latest study, published in Molecular Catalysis, we disclose synthetic strategies towards the first hydrophilic dppf derivatives overcoming issues typically encountered due to their intrinsic oxidizability. The novel ligands were spectroscopically characterized and showed their catalytic potential in the Pd-catalyzed Tsuji-Trost allylation of amines in water furnishing pharmaceutically relevant N-allylated products (e.g., naftifine, cinnarizine) through a scalable, safe and environmentally benign process.

15.12.2023

Congratulations to Tobias Huberts

Tobias Huberts just finished his Master studies doing a great job at his exam!
We wish you all the best for your future career!

13.12.2023

Congratulations to Johannes Zechner

Johannes Zechner just finished his Master studies! We wish you all the best for
your PhD studies in Groningen!

21.11.2023

New Review on Recent Advances in Pd-Catalyzed Suzuki-Miyaura Cross-Coupling
Reactions with Triflates or Nonaflates

Pd-catalyzed cross-coupling between aryl- and alkenyl halides and nucleophilic organometallic substrates, such as organoboronic acids (Suzuki-coupling), organostannanes (Stille coupling), or zinc organyls (Negishi coupling) has become one of the most widely used C−C coupling reactions, which has found many applications in medicinal chemistry and material sciences. In our latest review, published in Advanced Synthesis & Catalysis, we aim to systematically review the developments in the Suzuki coupling of organotriflates and nonaflates over the last decade, with a focus on new catalysts and strategies to overcome the described side reactions. Additionally, we provide a matrix table of substrate combinations with reaction conditions, which should enable the practitioners to efficiently find conditions that could be applied for their planned syntheses.

https://doi.org/10.1002/adsc.202301124

23.10.2023

Congratulations to Alexander Wolf

Alexander Wolf just finished his Master studies doing a marvelous job at his exam!
We are looking forward to welcome him as PhD student soon.

19.10.2023

Congratulations to Nadja Lenkova

Nadja Lenkova just finished her Master studies doing a marvelous job at her 
exam! We wish you all the best for your future career!

21.06.2023

Congratulations to Katharina Stracke

Katharina just finished her Master studies doing a marvelous job at her exam!
For the very first time at our institute, it had to be held in hybrid form on a
very short notice, but Katharina did not let these circumstances distract her
from her performance at all! We wish her all the best for her future career!

15.06.2023

Congratulations to Ella Holzinger

Ella just finished her Master studies doing a great job at her exam! We wish her all the best for her
future career!

14.05.2023

New paper on Constraining and Modifying Peptides Using Pd-Mediated Cysteine
Allylation

In this collaboration, published in ChemBioChem, with research groups from the
University of Vienna an extension of the recently introduced chemoselective
Pd-catalyzed cysteine allylation reaction to peptide stapling and further
modification of the resulting alkene-containing staples to introduce additional
probes into such stabilized peptides is reported.

https://doi.org/10.1002/cbic.202300098

11.05.2023

Congratulations to Elisabeth Unger

Elisabeth just finished her Master studies! We wish you all the best for your
future career!

01.03.2023

New MSc-Student: Viktoria Rehbein

We would like to welcome Viktoria Rehbeinfor her Master Thesis at the Institute!

01.03.2023

New MSc-Student: Alexander Wolf

We would like to welcome Alexander Wolf for his Master Thesis at the Institute!

14.02.2023

New Paper on Biocatalytic Production of Polyphenolic Natural Product  Di-C-β-glucosides

In this collaboration with the Institute of Biotechnology and Biochemical Engineering at the Graz University of Technology, published in Biotechnology & Bioengineering, a biocatalytic process technology for reaction-intensified production of the di-C-β-glucosides of two representative phenol substrates (phloretin and phenyl-trihydroxyacetophenone) from sucrose is reported. Collectively, this study demonstrates efficient glycosyltransferase cascade reactions for flexible use in natural product di-C-β-glucoside synthesis from expedient substrates.

https://onlinelibrary.wiley.com/doi/10.1002/bit.28354

01.02.2023

New MSc-Student: Tobias Huberts

We would like to welcome Tobias Huberts for his Master Thesis at the Institute!

18.01.2023

New review on activity-based protein profiling of oxidases and reductases

Activity-based protein profiling (ABPP) as a proteomic tool allows measuring the
activity of enzyme classes or distinct proteins in their cellular context,
annotating the function of uncharacterized proteins, and investigating the
target profile of small molecule inhibitors. In our latest review, published in
the Israel Journal of Chemistry, we provide an update to our previous review,
focussing on the recent advances of ABPP of oxidases and also reductases. This
article will be part of a special issue dedicated to Prof. Benjamin F. Cravatt,
the pioneer of ABPP and recipient of the 2022 Wolf Prize in Chemistry.

https://onlinelibrary.wiley.com/doi/full/10.1002/ijch.202200086 

 

01.12.2022

New PhD-Student: Mark Bieber

Today Mark Bieber started as new PhD-Student and University Assistant at our Institute!

11.11.2022

Loss of Prof. Dr. Klempier

The Institute of Organic Chemistry  mourns the loss of ao.Univ. Prof. Dr. Norbert Klempier (born 7.11.1953), who passed away after enduring  a long fight against cancer on 11.11.2022.  Prof. Klempier studied Chemistry at the University of Graz receiving his PhD in 1981. After post-doctoral research at Northeastern University in Boston/USA and work in industry, he joined the Institute of Organic Chemistry at TU Graz in 1988. Prof. Klempier established a state-of-the-art chiral chromatography lab at our institute  and was an early pioneer in biocatalysis research investigating the synthetic potential of hydroxynitrilases, nitrile hydratases and nitrile reductases. Over many years, Prof. Klempier was organizing the Undergraduate Organic Chemistry lab for BSc Chemistry students, where he inspired students by his passion for chemistry and his great empathy and fairness. We will remember Prof. Klempier as a great scientist and a very fine colleague

03.11.2022

Congratulations to Mark Bieber

Mark Bieber just finished his Master studies doing a marvelous job at his exam!
We are looking forward to welcome him as PhD student in our group soon.

03.10.2022

New MSc-Student: Daniel Griess

We would like to welcome Daniel Griess for his Master Thesis at the Institute!

27.09.2022

Congratulations to Christian Lembacher-Fadum

Today Christian Lembacher-Fadum defended his PhD thesis on "Synthesis of
N-Heterocyclic Inhibitors and Tool Compounds for Drug Discovery and Chemical
Biology". We want to congratulate Christian on this fantastic achievement, as he
has also been working in industry since december 2021 while writing his thesis,
and thank him very much for all the years as a great colleague to all of us at
our institute!

23.08.2022

New MSc-Student: Clemens Hofmann

We would like to welcome Clemens Hofmann for his Master Thesis at the Institute!

14.07.2022

Sub Auspiciis Doctoral Graduation of Dr. Thomas Schlatzer

Today, our group alumni Dr. Thomas Schlatzer received his promotio sub
auspiciis Praesidentis rei publicae
, which is the highest possible distinction
for academic achievements for a doctoral degree in Austria. In this solemn
event, Thomas was awarded with his doctoral degree and a ring of honour by
president Dr. Alexander van der Bellen.

Thomas is currently working as a postdoctoral researcher in the group of Prof.
Veronique Gouverneur at the University of Oxford and we wish him all the best
for his future career!

Bildquelle: Lunghammer - TU Graz

14.05.2022

New paper on fluororethylene-peptidomimetic inhibitors of DPP3

In this study, published in Bioorganic & Medicinal Chemistry, we describe the
design and synthesis of the so far most effective peptide-based inhibtor of
dipeptidyl peptidase III (DPP3). Starting from the slowly converted peptide
substrate tynorphin and by replacing the scissile bond with a fluoroethylene
bioisostere, thenewly reported ground state inhibitor outcompetes the previously
reported transition state mimetic inhibitor HER.

https://doi.org/10.1016/j.bmc.2022.116831 

25.04.2022

New MSc-Student: Nadja Lenkova

We would like to welcome Nadja Lenkova for her Master Thesis at the Institute!

01.04.2022

New Paper on Small-Molecule Inhibitors Targeting Lipolysis in Human Adipocytes

In our latest collaboration with the Institute of Molecular Biosciences at the
University of Graz, published in Journal of the American Chemical Society, we
reportthe development and biological characterization of the first
small-molecule inhibitor of human Adipose Triglyceride Lipase (ATGL), which is a
key enzyme in lipolysis. Detailed insights into the enzyme–inhibitor
interactions could be revealed through combined analysis of mouse- and
human-selective inhibitors, chimeric ATGL proteins, and homology models.

https://pubs.acs.org/doi/full/10.1021/jacs.1c10836
 

10.03.2022

New Senior Post-Doc: Bernhard Wölfl

Today Bernhard Wölfl (alumnus of Prof. Fürstner) arrived back from his post-doctoral stay in the lab of Prof. Aggarwal at the University of Bristol (UK). As a recipient of the Erwin Schrödinger Fellowship, he will now join the group of Prof. Breinbauer for his return phase.

07.03.2022

New MSc-Student: Katharina Stracke

We would like to welcome Katharina Stracke for her Master Thesis at the Institute!

01.03.2022

New MSc-Student: Ella Holzinger

We would like to welcome Ella Holzinger for her Master Thesis at the Institute!

21.02.2022

 New MSc-Student: Mark Bieber

We would like to welcome Mark Bieber for his Master Thesis at the Institute!
 

11.02.2022

New Paper Series on Teraryl-based alpha-Helix Mimetics

In this series of three back-to-back papers, we report about a complete library of building blocks featuring the side chains of all amino acids relevant for protein-protein interactions (PPIs). Via sequential Pd cross-coupling, these building blocks can be connected to form teraryl-based alpha-helix mimetics as inhibitors of PPIs. The papers are referred to as Parts 3-5 as they follow up on our two previous publications in this field.

Parts 3 and 4 describe core fragments with two leaving groups of differentiated reactivity (iodide and triflate or iodide and bromide, respectively). Part 5 describes a complementary set of pyridine boronic acid building blocks.

Part 3: https://doi.org/10.1002/ejoc.202101278

Part 4: https://doi.org/10.1002/ejoc.202101279

Part 5: https://doi.org/10.1002/ejoc.202101280

22.11.2021

New MSc-Student: Elisabeth Unger

We would like to welcome Elisabeth Unger for her Master Thesis at the Institute!
 

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

01.06.2021

New PhD Student: Maria Degli Innocenti

We would like to welcome Maria Degli Innocenti as a new PhD student at our institute!

23.04.2021

Congratulations to Thomas Schlatzer

After successfully defending his PhD thesis on “Labeling and Post Translational Modification of Cysteine-Containing Peptides and Proteins via Pd-Catalyzed S-Allylation”, Thomas Schlatzer became the first PhD-student for more than 50 years in the history of our institute who will receive his doctorate “sub auspiciis praesidentis”. We want to congratulate him on this extraordinary achievement and thank him for the last years in which he became an esteemed member of our Institute!

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

01.09.2020

New PhD-Student: Leo Krammer

We would like to welcome Leo Krammer as new PhD-Student at the Institute!

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

 

14.07.2020

Congratulations to Corina Maller


Corina just finished her Master studies! We wish you all the best for your upcoming PhD studies in Freiburg!

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

30.04.2020

Congratulations to Niklas Pontesegger


Niklas Pontesegger just finished his Master studies doing a marvelous job at his exam! We wish you all the best for your upcoming PhD studies!

23.04.2020

Congratulations to Martin Vařeka


Today Martin Vařeka defended his PhD thesis on quateraryl alpha-helix mimetics as inhibitors for protein-protein interactions (PPIs) in the first-ever online defense at our Institute. We congratulate on this achievement and are looking forward to his party at a later date!

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!

01.02.2020

New Senior Scientist: Rita Fürst

Today Rita Fürst has started her new position as Senior Scientist at our Institute!

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

11.12.2019

Institute tour

Today a group of students from the BORG Birkfeld visited our Institute in the course of their NAWI Graz day at TU Graz. We hope that you enjoyed your tour through our lab facilities!

01.12.2019

New PhD-Student: Till Schreiner

Today Till Schreiner started as new PhD-Student and University Assistant at the Institute!

11.11.2019

 Congratulations to Till Schreiner

Till Schreiner just finished his Master studies! We are looking forward to welcome him as PhD student soon.

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

15.10.2019

New PhD-Student: Michael Frieß

We would like to welcome Michael Frieß as new PhD-Student at the Institute!

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/

10.10.2019

Farewell party for Prof. Norbert Klempier

After a great farewell party at Buschenschank Schneiderannerl, we wish Prof. Norbert Klempier all the best for his retirement!

18.09.2019

New MSc-Student: Corina Maller


We would like to welcome Corina Maller for her Master Thesis at the Institute!

02.09.2019

New MSc-Student: Niklas Pontesegger

We would like to welcome Niklas Pontesegger for his Master Thesis at the Institute!

02.09.2019

New Senior Post-Doc: Melanie Trobe

Today Melanie Trobe (PhD alumnus) arrived back from her two-year post-doctoral stay in the lab of Martin D. Burke at the University of Illinois in the U.S. As a recipient of the Erwin Schrödinger Fellowship, she will now join the group of Prof. Breinbauer for her return phase.