Abstract: The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.

Abstract: The present disclosure relates to a glycopeptide targeting cancer cells and a contrast agent kit containing the same. The glycopeptide is one wherein an azide reporting monosaccharide is bound to a substrate peptide. As the substrate peptide is specifically cleaved by cathepsin B in cancer cells, an azide reporting monosaccharide is expressed onto the cell surface via metabolic glycoengineering, thereby providing a target for action as a contrast agent. Accordingly, because the azide is exposed to the cell surface only by cathepsin B, as it is specifically expressed in cancer cells, in particular in metastatic cancer cells, while it is limitedly expressed in normal cells and is hardly excreted out the cells, the cancer cells can be selectively imaged by an azide-specific contrast agent.

Abstract: Preferred embodiments relate to compositions of inherently radiopaque, biocompatible, bioresorbable polymeric particles and methods of using them for embolizing a body lumen.

Abstract: Described herein are methods, systems, and devices for identifying agents and genetic pathways that modulate the effects of traumatic brain injury (TBI) in invertebrate model systems having a brain, e.g., Drosophila or C. elegans.

Abstract: The present inventors have harnessed the targeting of nanoparticles to tumor sites, combined with the tumor site specific elevated MMP-14 activity within one conjugate to simultaneously deliver a vascular disrupting agent (VDA) and a MRI contrast agent to a tumor site. The MMP activatable conjugate of the present invention provides both therapeutic and diagnostic functions—and is referred to as a “theranostic”. The theranostic conjugate of the present invention achieves the benefits of tumor site specificity, VDA delivery and MRI contrast agent delivery in a single theranostic conjugate. Consequently, the present invention provides a cancer “theranostic” which improves therapeutic efficacy while simultaneously reducing dose-limiting systemic toxicities and provides a tool for rapidly and non-invasively identifying tumor location, monitoring drug delivery and pharmacodynamics.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA. Pharmaceutical compositions may include a complex of a radionuclide and a Formula I compound or a Formula II compound. Methods include using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

Abstract: A subject afflicted with a cancer or precancerous condition is treated by administering an agent that increases expression of somatostatin receptors, and a cytotoxic recognition ligand. In an alternative embodiment, somatostatin analogs, which are radiolabeled are used to treat cancer or precancerous conditions.

Abstract: The present invention is directed to compositions and method for providing radio-imaging and radiotherapy for cancer. In particular, methods for making and using radio-labeled anti-HAAH antibodies for tumor imaging and immunotherapy are provided.

Abstract: The caged cell-penetrating peptide (cCPP) conjugates of this invention are ideal for intracellular delivery of a broad variety of cargoes including various nanoparticulate pharmaceutical carriers (liposomes, micelles, microparticles, nanoparticles, polymer-conjugates). The conjugates comprise a detectable agent or a therapeutic agent, and the conjugates provide a novel strategy for site-specific delivery of the same to appropriate tissues in the subject. Versatile application of the conjugates in diagnostics and imaging is described.

Abstract: Imaging agents comprising an isolated polypeptide conjugated with a radionucleide and a chelator; wherein the isolated polypeptide binds specifically to HER2, or a variant thereof; and methods for preparing and using these imaging agents.

Abstract: The invention provides a conjugate with fluorochrome moiety F coupled to a targeting moiety T. Moiety F is described by formula (I), and the targeting moiety T is characterized in that it has affinity to a tumor marker, such as an antibody or antibody fragment. The conjugate may be used for tumor diagnostics including photodetection of tumor nodules during resection surgery.

Abstract: Somatostatin derivative compounds of general formula (I) that may be readily labelled with the isotope fluorine-18 and that have affinity and selectivity for cellular somatostatin receptors are provided. The labelled compounds are useful clinically as radioactive tracers in various in vivo imaging applications (for example, using positron emission tomography (PET) and related techniques) to detect somatostatin-expressing cells and tissues, including tumors, or as therapeutic agents.

Abstract: The present disclosure relates to new compounds and their use as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.

Abstract: The invention relates to compounds of formula I: and to pharmaceutically acceptable acid addition salts thereof, wherein R1-R6, Ra, and Rb have any of the values defined in the specification. The compounds are suitable as imaging tools.

Abstract: This invention provides a nucleus-permeable small-molecule inhibitor, L2P4 (where L2 is 4-(4-(Diethylamino)styryl)-N-carboxymethylpyridinium chloride and P4 is an amino acid sequence comprising CAhxYFMVFGGRrRK and they were coupled through amide bond) and synthesis thereof, which effectively targets the dimerization interface of EBNA1, a critical process for the growth of EBVs and the associated tumors. The present invention also provides method of treating and imaging EBV-associated cancers.

Abstract: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.

Abstract: Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only ?½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.

Abstract: The present invention is related to a radiolabeled active targeting pharmaceutical composition, including: a bioconjugate and a radionuclide, wherein the bioconjugate includes a biomolecule and a metal nanoparticle, wherein the biomolecule has an affinity for receptors on the surface of a cell membrane and is selected from the group consisting of a peptide and a protein. The present invention further provides a method for evaluating a thermal adjuvant therapy for tumors and a kit thereof. The above-mentioned pharmaceutical composition is applied to evaluate a tumor accumulation time, so as to establish the optimal policy for a radiofrequency- or laser-induced thermal adjuvant therapy for tumors.

Abstract: There is provided a novel conjugate that binds to the cell surface receptor uPA (uPAR). The conjugate is based on a fluorescence-labeled peptide useful as a diagnostic probe to the surfaces of cells expressing uPAR. The conjugate is capable of carrying a suitable detectable and imageable label that will allow qualitative detection and also quantitation of uPAR levels in vitro and in vivo. This renders the surgical resection of tumors more optimal.

Abstract: Novel methods and compositions for treating aged and environmentally damaged skin are disclosed which provide improvements in the skin's visual appearance, function and clinical/biophysical properties by activating at least one proteolytic enzyme in the skin's stratum corneum. The disclosed treatment methods involve topical application of a novel cosmetic composition containing a combination of a cationic surfactant such as N,N,-dimethyldodecyl amine oxide (DMDAO), an anionic surfactant such as sodium dodecyl sulfate (SDS), or monoalkyl phosphate (MAP) and a chelating agent such as ethylene diamine tetraacetate (EDTA) to stimulate a chronic increase in the replacement rate of the skin's stratum corneum by means of corneum protease activation. This chronic, low level stimulation is effective to induce repair and replacement of the stratum corneum, epidermis, and dermis of the skin and improvements in the appearance, function, and anti-aging properties of the skin.