Johns Hopkins University

Andrew G Cheetham

Honggang Cui

Pengcheng Zhang

Jeremy D Walston

Peter M Abadir

The present invention provides compounds and a method for the targeted delivery of Mitochondrial Angiotensin Receptor Blockers (MARBs) to the Mitochondrial Angiotensin System (MAS) for the treatment of diseases caused by angiotensin-related mitochondrial dysfunction. The compounds include a mitochondrial targeting signal, a residue of a drug molecule, a functional moiety, and a scaffold moiety.

Selective targeting of an anti-inflammatory receptor in human mitochondria and preservation of mitochondrial functions

The present invention provides herein the design of monodisperse, amphiphilic anticancer drugs&#x2014;which are now termed 'drug amphiphiles' (DAs)&#x2014;that can spontaneously associate into discrete, stable supramolecular nanostructures with the potential for self-delivery (no additional carriers are needed). The quantitative drug loading in the resulting nanostructures is ensured by the very nature of the molecular design. The DA is a composition comprising: D-L-PEP; wherein D is 1 to 4 hydrophobic drug molecules which can be the same or different; L is 1 to 4 biodegradable linkers which can be the same or different; and PEP is a peptide that can spontaneously associate into discrete, stable supramolecular nanostructures. In an alternate embodiment, the DA composition also comprises a targeting ligand (T). Methods of making DA molecules, as well as their use in treatment of disease are also provided.

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Charlottesville, VA, United States of America

Andrew G Cheetham