The present invention relates to ligands of Fibroblast Activation Protein (FAP) for the active delivery of various payloads (e.g. cytotoxic drugs, radionuclides, fluorophores, proteins and immunomodulators) at the site of disease. In particular, the present invention relates to the development of FAP ligands for targeting applications, in particular diagnostic methods and/or methods for therapy or surgery in relation to a disease or disorder, such as cancer, inflammation or another disease characterized by overexpression of FAP.

The invention is directed to fluorophore-containing compositions and configurations wherein proximity between the fluorophore and one or more protective agents (PAs) modifies the lifetime of fluorescent and/or dark states, their frequency of occurrence, and the total lifetime of fluorescence in order to appropriately modify the photophysical characteristics of the fluorophore. The invention is also directed to methods that utilize these compositions and configurations.

Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin α.sub.vβ.sub.3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin α.sub.vβ.sub.3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.

The present invention relates to a water-soluble, simple, stable tris(N-(tert-butyl)acetamide) cyclen-based europium complex HGEu001 which exhibits the specific subcellular localization in the primary cilium with a quantum yield as high as 10% in water and a lifetime of 0.56 ms lifetime. In particular, the present invention provides simplicity of the design and synthesis of a complex. Comprehensive studies were performed in numerous cell lines, such as HeLa, SN-K-SH and MRC5; the motif structure, HGEu002, has also been synthesized as the negative control for in vitro imaging studies. The two photon in vitro imaging were done in three dimensions to emphasize on the specific localization in primary cilium of HGEu001. This is one of the very limited examples for direct primary cilium imaging.

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

The invention relates to Cathepsin-binding compounds bound to a carrier comprising a diagnostic moiety, for use in the diagnosis of inflammatory diseases, and/or for use in the diagnosis of neoplastic diseases, wherein the Cathepsin-binding compound binds to inflammatory cells of the tumour stroma. The invention also relates to Cathepsin B-targeting compounds and Cathepsin B-binding and liposome-binding compounds.

The invention provides conjugates of cyclic peptides as ligands for cellular surface receptors, in particular, as ligands for αvβ6-integrin. The conjugates further contain effector moieties and are suitable for use as therapeutic agent, diagnostic agent, agent for imaging, targeting moiety and as biomolecular research tool. The invention specifically relates to the use of conjugates with signalling moieties or radionuclides for in-vivo addressing of αvβ6-integrin.

Carbamate and beta-amino acid urea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used for imaging cells and tumors that express PSMA or for cancer radiotherapy. These compounds also can comprise a fluorescent dye and be used for imaging cells and tumors that express PSMA or for photodynamic therapy.

The present invention relates to a composition and a method for use in diagnosing and treating bacterial infection. The composition comprises a novel compound with aggregation-induced emission characteristics adapted to target bacterial and biofilm with fluorescence. The compound is further adapted to generate reactive oxygen species for inhibiting and killing bacteria. The compound can be administered as a stand-alone anti-bacterial fluorescent modular probe or in combination with commercial drugs for enhanced therapeutic efficiencies with fewer side effects.

The present invention provides a conjugate of formula (I) and its use in methods of treatment, and also methods for delivering an active agent into a cell. The methods may be used to deliver an active agent into a nematode, flatworm, parasite or bacterium. The conjugate of formula (I) is: (formula (I)), wherein -D- is C.sub.1-4 alkylene or C.sub.2-4 alkenylene, preferably C.sub.2-4 alkenylene, where the alkylene or alkenylene is optionally substituted with alkyl or halo; A- is an active agent for delivery; and —R.sup.A, —R.sup.B, —R.sup.T1, —R.sup.T2, —R.sup.1, —R.sup.2, —R.sup.3, —X— and -L- are as defined herein.

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