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Inhibitors of serine proteases with drug-like characteristics

Country of Origin: Germany
Reference Number: TODE20180807001
Publication Date: 7 August 2018

Summary

A German university found first-in-class inhibitors influencing the serine proteases associated with macular degeneration and reperfusion-ischemia.  So far no inhibitors with drug-like characteristics have been available. The German university offers a license and/or research cooperation agreement.

Description

High Temperature Requirement A (HTRA) proteins are serine proteases of the S1 family (trypsin/chymotrypsin-like). HTRA1 is supposed to play a role in macular degeneration, and HTRA2 has been associated with cell death in reperfusion-ischemia. Therefore, HTRA proteins might represent novel therapeutic targets. However, currently no inhibitors with drug-like characteristics and thus promising potential for pharmaceutical development are available.



Researchers of a German university have now demonstrated that Ahp-cyclodepsipeptides represent a suitable scaffold for generating target-tailored inhibitors of serine proteases. They have developed a practical mixed solid- and solution-phase synthesis that allows the customized synthesis of Ahp-cyclodepsipeptides and thus tailored inhibitor synthesis. The applicability of this approach was shown by the generation of the most potent human HTRA1 as well as HTRA2 protease inhibitors to date (see figure). Inhibitory potency of the synthesized substances was proven in binding studies and cell-based assays.



The university offers a license cooperation agreement to pharmaceutical companies who would integrate the findings in their product development. The invention is in an early stage and that is why a research cooperation agreement is also offered to further advance the invention. Partners would be active in the field of eye diseases or cardiovascular disorders.

Advantages and Innovations

The enzymes HTRA1 and HTRA2 have not yet been pharmacologically addressed. Currently no inhibitors with drug-like characteristics and thus promising potential for pharmaceutical development are available. Ahp-cyclodepsipeptides constitute a novel class of HTRA inhibitors and are thus qualified to be further developed as “first-in-class” drugs for that target.

Stage Of Development

Under development/lab tested

Requested partner

The German university offers a license cooperation agreement to pharmaceutical companies working in the indication field of eye diseases or cardiovascular disorders and who would like to integrate the findings in their product development. The inhibitors are at an early stage of development. Thus a research cooperation agreement is also conceivable in order to adapt for markt readiness. In the initial phase (preclinical), the university could contribute to the optimisation of the substances for further development into a drug.