Use of Parabulin for Targeting Protozoan Tubulin for the Inhibition of Protozoan Replication

Simple SummaryContent extracted from patent full text and abstract with AI.

The invention describes the use of a compound called parabulin (and its derivatives) to specifically inhibit the replication of protozoan parasites within mammalian hosts by targeting and disrupting protozoan tubulin, a key component for parasite cell division and invasion. Parabulin binds selectively to parasite tubulin, destabilizing their microtubules, effectively blocking parasite growth without affecting mammalian (human) cells. This offers a new, targeted approach to combating protozoan infections and addresses the problem of drug resistance.

Use CasesContent extracted from patent full text and abstract with AI.

• Developing new anti-parasitic drugs for diseases caused by protozoans such as malaria or toxoplasmosis.
• Treating infections in humans or animals where protozoan parasites are resistant to current therapies.
• Combination therapies for protozoan infections using parabulin with other agents to prevent or slow drug resistance.
• Veterinary treatments for parasites in livestock and companion animals.

BenefitsContent extracted from patent full text and abstract with AI.

• Parabulin selectively targets protozoan tubulin, avoiding toxicity to mammalian cells and minimizing side effects.
• Effective inhibition of parasite replication tackles diseases that threaten global health.
• Provides a novel mechanism of action, helping to overcome existing drug resistance in parasites.
• Facilitates development of combination therapies by exploiting unique parasite tubulin drug-binding sites.
• Enables targeted anti-parasitic strategies, potentially improving patient outcomes and reducing treatment failures.

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Inventors & Applicants

Patent Abstract

The present invention determines apicomplexan tubulin, an essential parasite components, as an excellent drug target. Here, it is shown that it is possible to specifically target parasite tubulins, without harming the mammalian host. A compound has been identified that destabilizes specifically parasite MTs and inhibits essential parasite processes of replication and host cell invasion. The present invention thus offers a new strategy to tackle the issue of drug resistance development.In detail, the present invention discloses the use of the compound parabulin and/or its derivates in the process of targeting protozoan tubulin for the inhibition of the replication of protozoans in mammalian organism, wherein parabulin has the following molecular weight, sum formula, name and structure:MW: 373.4 Da;Formula: C20H23NO6;Name(s): 3-(3,4-dimethoxyphenyl)-N-[(3,4,5-trimethoxyphenyl)methyl]prop-2-enamide; (2E)-3-(3,4-Dimethoxyphenyl)-N-(3,4,5-trimethoxyphenyl)acrylamid;SMILES:O(C1=C(OC)C=CC(=C1)C=CC(=O)N(CC2=CC(=C(OC)C(=C2)OC)OC)[H])C.