prof. dr. A.S.S. Dömling

Design and Synthesis of Novel Bioactive Agents

> p53 Mdm2 and Mdm4 antagonists in collaboration with Prof Tad Holak (Jagiellonian University, Krakow, Poland)

> arginase inhibitors for asthma/COPD applications in collaboration with Profs Herman Meurs (RUG) and in collaboration with Matthew Groves (RUG), Carmolex Inc, STW funded

> potent non covalent caspase-1 inhibitors with the Italian consortium "IDENTIFICATION OF NEW LEAD FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES"

> mll/menin protein protein interaction inhibitors for the treatment of childhood leukemia in collaboration with Prof Matthew Groves (RUG)

> hemagglutinin targeting small moelcules for the tretament of influenza in collaboration with Prof Matthew Groves (RUG)

> CopZ1/2 inhibitors for killing non dividing "dormant" cancer cells in collaboration with Profs Igor Roninson (University of South Carolina), Carlos Camacho (University of Pittsburgh) and Matthew Groves (RUG) and Carmolex Inc

> Development of prodrugs cleaved in the tumor visinity by the clincal agent glucocarpidase in collaboration with Prof Sayed Goda (Qatar) and QNRF funded

> design, synthesis and characterisation of novel amylase inhibitors for the treatment of diabetes in collaboration with Prof Sayed Goda (Qatar) and QNRF funded

> design, synthesis and characterisation of small molecule Il17-Il17 rec antagonists

> design, synthesis and characterisation of small molecule PD1-PD1L antagonists for the treatment of cancer in collaboration with Profs Tad Holak (Jagiellonian University, Krakow, Poland) and Carlos Camacho (University of Pittsburgh)

> allosteric kinase inhibitors targeting the PIF pocket of Pdk1 (diabetes, cancer) in collaboration with Profs Bondi (University Hoaspital Frankfurt)

> p25-CDK5 interaction antagonists in collaboration with Prof Matthew Groves (RUG) and Carmolex Inc.

Multicomponent Reaction Chemistry

> The Domling laboratory is part of the European Lead Factory (ELF) a very large public private partnership program of IMI. Here we design and synthesize the next generation of MCR based scaffolds for the screening decks of ELF.

> in collaboration with Janssen Pharmaceuticals we develop novel MCR synthesis technolgies

> in collaboration with Telesis Pharma we develop novel MCR synthesis technolgies

Development of Novel MRI and Immaging Agents

We are developing the next generation MRI agents. Our compound platform is able to provide multiple answers to strcutural and biochemical recognition in different disease states. A collaboration with UMCG.

Development of Missmutation Correcting Agents for the Treatment of Rare Diseases

We are developing a game changing technology able to address multiple unmet medical needs in a personalized meidicne manner: chemicals able to correct missmutations in a selective manner to treat multiple rare or orphan diseases. Stay tuned!

Novel Software Tools for Pharmacophorically Leverage of the Very Large MCR Space

In collaboration with Prof Carlos Camacho (Computational and Sytems Biology, University of Pittsburgh) the software ANCHOR.QUERY, NUCLEO.QUERY and TPP.QUERY was developed. ANCHOR.QUERY  is a specialized Google-like pharmacophore  search technology that brings interactive virtual screening of novel protein-protein inhibitors to the desktop. Each compound proposed can be instantaneously synthesized with minimal effort using MCR chemistry. This project is NIH-RO1 funded.