Spiroepoxide, Tetrahydrobenzo-triazoles and -Imidazoles as MetAP-II Inhibitors
Numerous studies have shown that selective inhibition of the MetAP-II subtype halts the growth of endothelial cells in culture, inhibits angiogenesis in animal models, and is a validated strategy for anti-angiogenic cancer therapy. In addition, MetAP-II has also emerged as a promising target for other indications, including malaria, rheumatoid arthritis, pulmonary hypertension, and obesity.
So the invention describes the design of the small molecules which was guided by the chemical structure of fumagillin. The substances have drug-like substructures, exist in novel chemical space, and the active enantiomeric series has been identified. • They are potent MetAP-II inhibitors (low nM) and highly selective over MetAP-I and E. coli MetAP. • They inhibit the growth of HUVEC cells (mid nM GI50), but are not cytotoxic.
Further Information: PDF
Deutsches Krebsforschungszentrum DKFZ
Phone: +49-6221-42 2955
Contact
Dr. Ruth Herzog
Media Contact
All latest news from the category: Technology Offerings
Newest articles
Microscopic basis of a new form of quantum magnetism
Not all magnets are the same. When we think of magnetism, we often think of magnets that stick to a refrigerator’s door. For these types of magnets, the electronic interactions…
An epigenome editing toolkit to dissect the mechanisms of gene regulation
A study from the Hackett group at EMBL Rome led to the development of a powerful epigenetic editing technology, which unlocks the ability to precisely program chromatin modifications. Understanding how…
NASA selects UF mission to better track the Earth’s water and ice
NASA has selected a team of University of Florida aerospace engineers to pursue a groundbreaking $12 million mission aimed at improving the way we track changes in Earth’s structures, such…