ProjectFOR2314 TP11 – HECT ligase inhibition for cancer therapy
Basic data
Acronym:
FOR2314 TP11
Title:
HECT ligase inhibition for cancer therapy
Duration:
01/09/2018 to 31/08/2021
Abstract / short description:
The central goal of this research program is to lay the ground for harnessing the activities of HECT-type ubiquitin ligases in cancer-therapy. With a particular focus on HUWE1, we will pursue two specific aims:
1. Rational optimization of small-molecule HUWE1 inhibitors
Building on two hit compounds from a previous high-throughput screen, we aim to develop high-affinity, specific inhibitors of HUWE1 that are suitable for in vivo applications. By defining the mechanisms and structural determinants of specificity of synthesized compounds for HUWE1 we will provide unprecedented insights into the druggability of HECT E3 enzymes in general.
1. Rational optimization of small-molecule HUWE1 inhibitors
Building on two hit compounds from a previous high-throughput screen, we aim to develop high-affinity, specific inhibitors of HUWE1 that are suitable for in vivo applications. By defining the mechanisms and structural determinants of specificity of synthesized compounds for HUWE1 we will provide unprecedented insights into the druggability of HECT E3 enzymes in general.
Involved staff
Managers
Faculty of Science
University of Tübingen
University of Tübingen
Pharmaceutical Institute
Department of Pharmacy and Biochemistry, Faculty of Science
Department of Pharmacy and Biochemistry, Faculty of Science
Baden-Württemberg Center for Brazil and Latin America
Branch offices and other central facilities
Branch offices and other central facilities
Cluster of Excellence: Image-Guided and Functionally Instructed Tumor Therapies (iFIT)
Centers or interfaculty scientific institutions
Centers or interfaculty scientific institutions
Contact persons
Faculty of Medicine
University of Tübingen
University of Tübingen
Local organizational units
Pharmaceutical Institute
Department of Pharmacy and Biochemistry
Faculty of Science
Faculty of Science
Funders
Bonn, Nordrhein-Westfalen, Germany