Project ImproveCRC – Potent and sustained inhibition of p38 for the treatment of colorectal cancer

Basic data

Acronym:
ImproveCRC
Title:
Potent and sustained inhibition of p38 for the treatment of colorectal cancer
Duration:
01/05/2018 to 01/05/2021
Abstract / short description:
Advanced Colorectal Cancer (CRC) represents a major health problem with very limited therapeutic options and a dismal prognosis. It was recently reported that genetic ablation of Mapk14 (p38α) in CRC mouse models results in pronounced tumor remissions and improved survival of tumor bearing mice. Available p38α inhibiting compounds do not mimic the phenotype observed upon genetic Mapk14 ablation due to incomplete pathway inhibition, thus pointing out a strong need for compounds with extreme (picomolar) activity, strongly enhanced or irreversible target residence time and high selectivity. Building upon our recent description of the development of such inhibitors, we are now aiming to advance such compounds into proof of concept studies and to test their potential in predictive CRC mouse models. These studies are prerequisite for later first in man studies in humans.
Keywords:
Colorectal Cancer
p38alpha

Staff

Managers

Faculty of Science
University of Tübingen
Pharmaceutical Institute
Department of Pharmacy and Biochemistry, Faculty of Science

Contact persons

Faculty of Science
University of Tübingen
Pharmaceutical Institute
Department of Pharmacy and Biochemistry, Faculty of Science
Faculty of Medicine
University of Tübingen
Faculty of Medicine
University of Tübingen

Local organizational units

Pharmaceutical Institute
Department of Pharmacy and Biochemistry
Faculty of Science

Funders

Stuttgart, Baden-Württemberg, Germany
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