Reversible Cathepsin B Inhibitor Lead Series
Cathepsin B is an abundant and ubiquitously expressed cysteine peptidase involved in many pathological processes, such as inflammation, parasite infection and cancer. To date, most cathepsin B inhibitors are short peptides or small molecules that bind covalently to the enzyme, which is a generally unfavoured feature for drugs. A novel lead series of non-covalent cathepsin B inhibitors has been identified and characterized. Ease of synthesis and favourable properties like good solubility will allow further development and optimization for preclinical testing on a short timescale. Activity, selectivity, cytotoxicity and solubility data has been compiled for a series of about 50 compounds and an SAR has been established. Next steps will involve in vivo testing and further optimization of the lead series.
Further Information: PDF
Bayerische Patentallianz GmbH
Phone: +49 89 5480177-0
Contact
Peer Biskup
Media Contact
All latest news from the category: Technology Offerings
Newest articles
Economies take off with new airports
A global study by an SUTD researcher in collaboration with scientists from Japan explores the economic benefits of airport investment in emerging economies using nighttime satellite imagery. Be it for…
CAR T–cell immunotherapy targets
Pan-cancer analysis uncovers a new class of promising CAR T–cell immunotherapy targets. Scientists at St. Jude Children’s Research Hospital found 156 potential CAR targets across the brain and solid tumors,…
Stony coral tissue loss disease
… is shifting the ecological balance of Caribbean reefs. The outbreak of a deadly disease called stony coral tissue loss disease is destroying susceptible species of coral in the Caribbean…