Polypept(o)id-based graft copolymers for in vivo imaging by tetrazine transyclooctene click chemistry
OwnerAndreas KJÆR, Matthias Manfred HERTH +2inventors
InventorsAndreas KJÆR, Matthias Manfred HERTH, Matthias BARZ, Alexander Oksar BIRKE
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Abstract
There is provided novel polypeptide-based carrier systems, which make it possible to label polymeric nanoparticles in the living organism. This enables new approaches in tumor diagnostics (high signal to background ratio) and radiotherapy (radiotherapy of solid tumors). The polypeptide-based carrier system comprises a polypept(o)idic comb (graft) copolymer, and one or more tetrazine bioorthogonal functional groups each linked to a diagnostic agent
Claims11
A polypept(o)idic comb (graft) copolymer for in vivo imaging by tetrazine transcyclooctene click chemistry, said comb (graft) copolymer having a polyglutamate (pGlu) backbone with transcyclooctene (TCO) bioorthogonal functional groups and polysarcosine chains covalently attached thereto;
- and wherein the comb polymer (graft) copolymer coils in aqueous environment to spherical nanoparticles with diameters between 5-30 nm;
- said copolymer is defined as:
- p(G\Un-graft-(TCO)m-graft-(pSar)k)p
- wherein
- Glun denotes polyglutamate with n number of glutamate units, n ranging from 50 to 400;
- (TCO)m denotes transcyclooctene with m number of transcyclooctene unit ranging from substitution levels of pGlu form 5 to 40%;
- (pSar)k denotes polysarcosine with k number of polysarcosine units, k ranging from 20 to 200;
- and
- p denotes the number of pSar polymers in the comb (graft) copolymer;
- p ranging from 5 to 100 leading to a grafting density of the polysarcosine side chains of 2 to 50%.
Dependencies are inferred from the claim text.