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National projects

The kiss of death for key apoptosis players: development of BCL-2 and BAX PROTACs

The intrinsic (mitochondrial) apoptosis pathway is a physiologically dominant form of cell death and is controlled by the BCL-2 family of proteins. The members of this family have opposing effects as some of them promote and others prevent mitochondria-dependent apoptosis. The cross-talk within this family, which is governed by protein-protein interactions between p...

01. September 2020 - 31. August 2023 | 1-09 Natural sciences and Mathematics - Pharmacy

Development of innate immune receptor-targeting chimeras as custom-tailored vaccine adjuvants

Currently, our world is facing an acute shortage of novel vaccine adjuvants. Adjuvants enhance the immunogenicity of vaccines, therefore they constitute essential components of vaccines. They are needed not only to increase the magnitude of the response but also to guide the type of response to produce the most effective type of immunity against distinct pathogens/t...

01. September 2020 - 31. August 2023 | 1-09 Natural sciences and Mathematics - Pharmacy

Photochemistry toolbox for discovery of advanced ATP-competitive chemical probes with Topoisomerase IIalpha inhibitory activity

Due to an ageing population, the challenges associated with cancer treatment are growing. The use of conventional chemotherapeutic agents is often limited because of their side effects. Moreover, resistance of cancer cells to chemotherapeutic drugs often results in failure of treatment. The project aims to contribute to the discovery and development of new anticance...

01. January 2021 - 31. December 2023 | 1-09 Natural sciences and Mathematics - Pharmacy

A Covalent Approach Against Antibiotic Resistance

The increased frequency of resistance among human bacterial pathogens represents a serious public threat in the treatment of infectious diseases. The United Nations, the World Health Organisation and the European Commission, have recently declared antimicrobial resistance (AMR) as a serious global threat to public health that has a tremendous impact on healthcare ex...

01. January 2021 - 31. December 2023 | 1-09 Natural sciences and Mathematics - Pharmacy

Development of antibacterial compounds targeting validated enzymes in peptidoglycan biosynthesis

Infections caused by antibiotic-resistant bacteria continue to challenge health-care systems worldwide. We face a growing resistance of Gram-positive and Gram-negative pathogens that cause infections in hospitals and in the community, with the so-called antibiotic-resistant ‘superbugs’ that now represent a major global health problem. The obstacles of ha...

01. September 2020 - 31. August 2023 | 1-09 Natural sciences and Mathematics - Pharmacy

Radiopharmaceuticals with antagonistic activity on CCK2R

Nuclear medicine investigations have an integral role in timely identification and confirmation of cancer, staging, follow-up of treatment efficiency and identification of the disease relapse. Certain tumour types and entities can be visualized by nuclear medicine imaging techniques because of the (over)expression of different receptors for certain regulatory peptid...

01. September 2020 - 31. August 2023 | 1-09 Natural sciences and Mathematics - Pharmacy

Development of novel Hsp90 inhibitors with anticancer activity

Chaperones are ubiquitous molecular machineries that maintain a balanced protein homeostasis (proteostasis) by continuously sampling and assessing the conformational state of polypeptides by a plethora of cellular processes from de novo, cotranslational and posttranslational folding of nascent polypeptides, polypeptide disaggregation and protein degradation. Several...

01. January 2019 - 30. December 2020 | 1-09 Natural sciences and Mathematics - Pharmacy

Targeted covalent inhibitors: inhibiting monoamine oxidase through non-catalytic amino-acid residues

Monoamine oxidase (MAO) is a flavin-dependent enzyme that catalyzes the oxidation of amines, and has an important role in the homeostasis of biogenic and exogenic amines. Two isoforms of MAO (i.e., MAO-A and MAO-B) are present in most mammalian tissues and are distinguished by their sensitivities to acetylenic inhibitors clorgyline and L-deprenyl, and by their subst...

30. June 2019 - 01. July 2021 | 1-09 Natural sciences and Mathematics - Pharmacy

Identification of non-peptidic inhibitors of the immunoproteasome using fragment based drug discovery methods

The proteasome is an intracellular protease that represents a vital part of the ubiquitin-proteasome system. It degrades a wide range of proteins and has critical functions in many biological processes including cell cycle control, apoptosis, inflammation, and signal transduction. The constitutive isoform (cCP) of the proteasome is expressed in all eukaryotic cells ...

01. November 2017 - 31. October 2020 | 1-09 Natural sciences and Mathematics - Pharmacy

Butyrylcholinesterase inhibitors for alleviating symptoms of Alzheimer's disease

Memory and cognitive deficits of patients with AD are the result of severely decreased brain levels of ACh. Currently approved ChEs inhibitors in AD therapy (donepezil, galantamine and rivastigmine) alleviate symptoms of the disease by increasing brain levels of ACh. They achieve this by preventing the breakdown of ACh through inhibition of the enzymes that hydrolyz...

01. July 2018 - 30. June 2021 | 1-09 Natural sciences and Mathematics - Pharmacy