Abstract: 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.

Abstract: The present invention provides 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.

Abstract: The present invention provides herein the design of monodisperse, amphiphilic anticancer drugs—which are now termed “drug amphiphiles” (DAs)—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.

Abstract: The present invention provides herein the design of monodisperse, amphiphilic anticancer drugs—which are now termed “drug amphiphiles” (DAs)—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.

Abstract: The present invention provides herein the design of monodisperse, amphiphilic anticancer drugs—which are now termed “drug amphiphiles” (DAs)—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.

Abstract: The present invention provides herein the design of monodisperse, amphiphilic anticancer drugs—which are now termed “drug amphiphiles” (DAs)—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.

Abstract: Disclosed herein are novel nanobeacon imaging agents having the following formula: wherein: D is 1 to 4 fluorophores; L is 1 to 4 enzymatically cleavable peptide linkers; PEP is a hydrophilic cell penetrating peptide sequence; A is a side chain moiety of an amino acid of PEP; and Q is a fluorescence quencher molecule. The present invention provides a generic design of a new type of supramolecular nanobeacon imaging agents with a well-defined size and surface chemistry for protease detection. In contrast to soluble molecular beacons, the imaging agent molecules are specifically designed to self-assemble into core-shell micellar structures, with the enzyme-sensitive design feature being deeply embedded within the micellar core and thus inaccessible to the enzyme. Only in the monomeric form can these nanobeacon imaging agent molecules be cleaved by the target enzyme to generate fluorescence signals.