The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

Disclosed herein are novel synthetic polypeptides and uses thereof in the preparation of liposomes. According to embodiments of the present disclosure, the synthetic polypeptide comprises a membrane lytic motif, a masking motif, and a linker configured to link the membrane lytic motif and the masking motif. The linker is cleavable by a stimulus, such as, light, protease, or phosphatase. Once being coupled to a liposome, the exposure to the stimulus cleaves the linker that results in the separation of the masking motif from the membrane lytic motif, which in turn exerts membrane lytic activity on the liposome that leads to the collapse of the intact structure of the liposome, and releases the agent encapsulated in the liposome to the target site. Also disclosed herein are methods of diagnosing or treating a disease in a subject by use of the present liposomes.

The present invention relates to a metal phase transformation compound and a method for preparing the same.

The present disclosure provides novel methods for treating or preventing traumatic optic neuropathy (TON), methods for improving visual function in a subject having TON, methods for promoting retinal ganglion cell (RGC) survival or increasing neurite outgrowth of an RGC, and methods for reducing the risk of having or developing TON in a subject that has experienced a traumatic injury. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide.

The present disclosure provides aromatic-cationic peptide compositions and methods of using the same. The methods comprise use of the peptides in electron transport, inhibition of cardiolipin peroxidation, and inhibition of apoptosis and necrosis to treat, prevent or ameliorate the symptoms of autoimmune diseases or condition.

The present invention provides compounds and pharmaceutical compositions of a peptidomimetic ligand, e.g. LLP2A, conjugated with a bisphosphonate drug, e.g. Alendronate. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of osteoporosis and for the promotion of bone growth due to their specificity for the α.sub.4β.sub.1 integrin on mesenchymal stem cells and for the surface of bone.

Disclosed are improved peptides for inhibiting angiogenesis, Ac-RLYE (SEQ ID NO: 1) and R(D)LYE (SEQ ID NO: 6), and a composition for the prevention and treatment of cancers and diseases related to angiogenesis comprising the peptides as an active ingredient. A peptide for inhibiting angiogenesis is disclosed wherein the L-Arg of an N-terminal is acetylated in a peptide consisting of an amino acid sequence of Arg-Leu-Tyr-Glu (SEQ ID NO: 1). A peptide for inhibiting angiogenesis is disclosed wherein L-Arg is substituted with D-Arg in a peptide consisting of the amino acid sequence of Arg-Leu-Tyr-Glu (SEQ ID NO: 6). Methods for using a composition comprising the peptides as active ingredients for the prevention or treatment of diseases (cancer, diabetic retinopathy or senile macular degeneration) caused by excessive angiogenesis are also disclosed. The peptides have a long half-life and are excellent in VEGF-induced angiogenesis inhibitory effect.

Described are compounds for targeting proteases, e.g. serine proteases and their use in the diagnostic methods and methods for treatment of respiratory diseases such as cystic fibrosis. The compounds have the structure [H]—[B]-[A]; wherein [H] is a hydrophilic group, [B] is a subsite recognition group and [A] is a binding group; wherein A has the formula: —C(0)—CH.sub.2—NR.sup.1—COOR.sup.2 and wherein [B] has the structure: (i) —[CO—CH.sub.2—NR.sup.3]m-, or (ii) -[AA1-AA2]- or (iii) -(AA1-C0-CH.sub.2NR.sup.3)— or (iv) —(CO—CH.sub.2—NR.sup.3-AA1)- or (v) —(C0—CH.sub.2—NR.sup.4-AA1-AA3)-.

Disclosed are various crystalline salt forms of Boc-D-Arg-DMT-Lys(Boc)-Phe-NH.sub.2.

Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH.sub.2 and Boc-D-Arg-DMT.