The present invention provides compounds suitable for use in the treatment of conditions where it is beneficial to halt bone loss and kill cancer cells, particularly in metastases to and primary tumors in the bone and surrounding tissues. Consequently the present invention provides compounds comprising a bisphosphonate moiety linked to a phytochemical, pharmaceutical compositions thereof and methods of treatment of bone diseases and/or proliferative disorders.

According to the present invention, it is possible to provide a drug carrier having excellent bioavailability and improved drug encapsulation efficiency by preparing lipoprotein-mimicking solid lipid nanoparticles having a core-shell structure consisting of albumin-conjugated cholesterol, a fusogenic lipid, a cationic lipid, a triglyceride and a cholesteryl ester.

The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases.

The present disclosure relates generally to supramolecular combinatorial therapeutics, compositions comprising same, and uses thereof. In particular, the present disclosure provides hydrophobic taxane-lipid covalent conjugates which create supramolecular assembly, for example, within lipid bilayer, providing an extra stabilization resulting in increased intratumoral concentration and hence increased efficacy. The present disclosure also provides supramolecular combinatorial therapeutics, wherein a taxane-lipid conjugate is combined with one or more of a platinum compound, a kinase inhibitor, and an immunoregulator, each of which is optionally conjugated with a lipid.

Disclosed herein are identified compound fragments, compounds and their pharmaceutically acceptable salts, isotopes or solvates, useful as antiviral drug and/or as a hepatic-targeted drug, such as for the treatment of HBV, HDV and/or HIV. Formula (I).

##STR00001##

Peptides, salts thereof, peptide conjugates, and salts thereof having 5 to 15 amino acids and having an amino acid sequence comprising at least 5 consecutive amino acids from the amino acid sequence LSSTQAQQSX.sub.1 (SEQ ID NO:34).

Nanoparticles include a core, a hydrophilic layer around the core, and one or more mitochondrial targeting moieties, and may optionally include one or more contrast agents or one or more therapeutic agents. For effective mitochondrial targeting the nanoparticles have a diameter of about 200 nm or less or have a zeta potential of about 0 mV or more.

The present invention discloses a bone-targeting therapeutic conjugate comprising a formula of TG-M-D (I) or M-D-TG (II) and methods of making and using the same. The present invention also discloses a composition comprising the conjugate and methods of making and using the composition.

Oxysterol-therapeutic agent derivatives or OXY133-therapeutic agent derivative compounds and methods of synthesizing the same are provided for use in promoting osteogenesis, osteoinduction and/or osteoconduction. Methods of synthesizing in a single container OXY133-therapeutic agent derivatives having high yields and improved process safety are also provided. Methods for synthesizing OXY133-therapeutic agent derivatives that are stereoselective are also provided.

A mitochondria targeted gold nanoparticle (T-3-BP-AuNP) decorated with 3-bromopyruvate (3-BP) and delocalized lipophilic triphenylphosphonium (TPP) cations to target the mitochondrial membrane potential (m) was developed for delivery of 3-BP to cancer cell mitochondria by taking advantage of higher m in cancer cell compared to normal cells. This construct showed remarkable anticancer activity in prostate cancer cells compared to non-targeted construct NT-3-BP-AuNP and free 3-BP. Anticancer activity of T-3-BP-AuNP was further enhanced upon laser irradiation by exciting the surface plasmon resonance band of AuNP and thereby utilizing a combination of 3-BP chemotherapeutic and AuNP photothermal effects. T-3-BP-AuNPs showed markedly enhanced ability to alter cancer cell metabolism by inhibiting glycolysis and demolishing mitochondrial oxidative phosphorylation in prostate cancer cells. Our findings demonstrated that mitochondria targeted and concerted chemo-photothermal treatment of glycolytic cancer cells with a single NP may have promise as a new anticancer therapy.