Embodiments of the present disclosure pertain to methods of opening a lipid bilayer by associating the lipid bilayer with a molecule that includes a moving component capable of moving (e.g., rotating) in response to an external stimulus; and exposing the molecule to an external stimulus before, during or after associating the molecule with the lipid bilayer. The exposing causes the moving component of the molecule to move and thereby open the lipid bilayer (e.g., by pore formation). The external stimuli may include an energy source, such as ultraviolet light. The opened lipid bilayer may be a component of cell membranes in vitro or in vivo. The opening of the lipid bilayer may allow for the passage of various materials (e.g., active agents, such as peptide-based drugs) through the lipid bilayer and into cells. Additional embodiments of the present disclosure pertain to the aforementioned molecules for opening lipid bilayers.

Provided herein is a pharmaceutical composition comprising an effective amount of cypate-Cyclo(Cys-Gly-Arg-Asp-Ser-Pro-Cys)-Lys-OH (LS301), cypate-Cyclo(Cys-Gly-Arg-Asp-Ser-Pro-Cys)-Tyr-OH (LS838) or pharmaceutically acceptable salts thereof, wherein each amino acid residue is independently in a D or L configuration; a divalent metal ion; and a pharmaceutically acceptable carrier. Further provided are lyophilized products comprising a dye-conjugate and m methods for identifying compromised and for binding phosphorylated annexin A2 (pANXA2) protein in a biological sample using a composition described herein.

The present invention relates to tumor-targeted probes for use as medicaments and for use in treatment of cancer and to methods of treatment wherein such probes are used. The probes consist of a light-absorbing molecule linked directly or via a spacer to a peptide targeting the urokinase-type plasminogen activator receptor (uPAR). When irradiating the light-absorbing molecule of the probe with laser beams from an external source heat will be released locally to tumor cells expressing uPAR resulting in tumor ablation.

Compositions and methods are provided to determine occupancy level of opioid receptors in a subject. The disclosed methods may be performed non-invasively in the inner ear of the subject, and may be performed at a point-of-care location to provide guidance to a practitioner on tapering on pharmacotherapy or on a patient's risk of relapse for substance abuse.

Described herein are therapeutic pH responsive compositions comprising a block copolymer and a therapeutic agent useful for the treatment of cancer.

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: A compound or a pharmaceutically acceptable salt thereof of formula (I): (A)-x.sub.1-(B)-x.sub.2-(C), wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x.sub.1 is a spacer covalently connecting (A) and (B); x.sub.2 is a spacer or a chemical single bond connecting (B) and (C); wherein (C) has the formula

##STR00001##

wherein R.sup.1 to R.sup.4, R.sup.9, a, b, Y and X.sup.1 to X.sup.4 have the meaning as indicated in the claims and description. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition.

Described herein are nanoprobes comprising ultrasmall aminated and cRGDY-conjugated nanoparticles labeled with Zirconium-89 (.sup.89Zr) and methods of their use. The provided compositions are renally clearable and possess suitable blood circulation half-time, high tumor active targeting capability, dominant renal clearance, low liver accumulation, and a high tumor-to-background ratio. The described nanoprobes exhibit great potential as “target-or-clear” tracers to human subjects for systemic targeted imaging (or treatment) of cancer.

Peptides that home, target, migrate to, are directed to, are retained by, or accumulate in and/or bind to the cartilage or kidney of a subject are disclosed. Pharmaceutical compositions and uses for peptides or peptide-active agent complexes comprising such peptides are also disclosed. Such compositions can be formulated for targeted delivery of an active agent to a target region, tissue, structure or cell in the cartilage. Targeted compositions of the disclosure can deliver peptide or peptide-active agent complexes to target regions, tissues, structures, or cells targeted by the peptide.

A PSMA-specific agent comprising a compound according to Formula I or Formula II: wherein S.sub.1 is absent or is an organic spacer group comprising 3-10 carbons; A is an amino acid chain comprising 1 to 5 amino acids wherein at least one of the amino acids is selected from glutamic acid and aspartic acid; S2 is absent or is an organic spacer group comprising 1 to 15 carbons and/or 0 to 2 amino acids; I.sub.1 is an imaging group; and I.sub.2 is absent or is an imaging group. The PSMA-specific agents can be used to image PSMA within a tissue region and/or for the treatment of a cancer, such as prostate cancer.

##STR00001##

The near-infrared window of fluorescent heptamethine cyanine dyes greatly facilitates biological imaging because there is deep penetration of the light and negligible background fluorescence. But dye instability, aggregation, and poor pharmacokinetics are current drawbacks that limit performance and the scope of possible applications. All these limitations are simultaneously overcome with a new molecular design strategy that produces a charge balanced and sterically shielded fluorochrome. The key design feature is a meso-Aryl group that simultaneously projects two shielding arms directly over each face of a linear heptamethine polyene. Cell and mouse imaging experiments compared a shielded heptamethine cyanine dye (and several peptide and antibody bioconjugates) to benchmark heptamethine dyes and found that the shielded systems possess an unsurpassed combination of photophysical, physiochemical and biodistribution properties that greatly enhance bioimaging performance.