Abstract: The present invention is in the field of bioluminescence in biology and/or medicine. In particular, the invention provides imidazopyrazine derivatives, processes for preparation thereof, and their uses as luciferins.

Abstract: Some embodiments relate to imageable radioisotopic microspheres. In some embodiments, the imageable microspheres are radiolabeled with imageable radioisotopes. In some embodiments, the imageable radioisotope is directly coupled to a surface of a substrate of the microsphere. In some embodiments, the imageable microspheres can be used as surrogate particles to predict the distribution of therapeutic microspheres comprising radiotherapeutic isotopes.

Abstract: It is an object of the present invention to provide a clearing agent, by which after a fusion of the streptavidin mutant and a molecular probe has been administered, the fusion, which is not localized in a target site such as an affected site but remains in the body, can be promptly removed (cleared) from the body. The present invention provides a compound represented by the following formula (1) or a salt thereof: wherein X1a, X1b, X2a and X2b each independently represent O or NH; Y1 and Y2 each independently represent C or S; Z1 and Z2 each independently represent O, S or NH; V1 and V2 each independently represent S or S+—O?; n1 and n2 each independently represent an integer of 0 or 1; L10 and L12 each independently represent a divalent linking group; L11 represents a trivalent linking group; L14 represents a divalent linking group; and Sugar represents a sugar residue.

Abstract: Described herein are multi-specific binding agents that bind A33 and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid. Also provided herein are methods of using multi-specific binding agents or compositions thereof for the detection, prevention, and/or therapeutic treatment of diseases characterized by expression of the A33 glycoprotein antigen, in particular, colorectal cancer.

Abstract: The invention features a novel precursor provided for radioisotope labeling with ligands for specific binding of prostate-specific membrane antigen (PSMA) for prostate cancer diagnosis and treatment, and the pharmacophore of a PSMA inhibitor composed of three molecules of glutamic acid, urea and lysine is provided with three variable linkers based on pharmacological activity of the PSMA inhibitor for labeling with radioactive nucleus Ga-67, Ga-68, In-111, Lu-177, Cu-64, or Y-90 through a chelating agent for imaging analysis of human tumor models of prostate cancer and serving as a PSMA-targeted radioligand therapy for prostate cancer diseases.

Abstract: This disclosure relates to styrylbenzothiazole derivatives for use as in vivo imaging agents for the diagnosis of Parkinson's disease (PD) or other degenerative disorders or conditions of the central nervous system. Early diagnosis is particularly advantageous as neuroprotective treatment can be applied to healthy neural cells to delay or even prevent the onset of debilitating clinical symptoms.

Abstract: The present disclosure relates generally to the selection of DNA aptamers that prevent aggregation, or fibrilization of alpha-synuclein protein. The aptamers described herein are of use as a therapeutic tool to prevent protein aggregation in neurodegenerative disease.

Abstract: A superconducting coil of embodiments includes a substrate having a curved surface, a superconducting wire wound on the curved surface, the superconducting wire having a first region and a second region facing the first region, a first resin layer surrounding the superconducting wire and including a plurality of first particles and first resin surrounding the first particles, and a second resin layer positioned between the first region and the second region, the second resin layer covering the first resin layer and including a plurality of second particles and second resin surrounding the second particles and being made of material different from material of the first resin.

Abstract: A method for using bodily fluids in determining the cell-specific potency of drugs is provided. A composition comprising a plurality of types of carriers, wherein each carrier comprises a single-cell lethal amount of a therapeutic agent and a unique barcode identifying that agent and wherein the composition comprises equal numbers of each carrier type, equal concentrations of the agent and equal concentrations of each barcode is also provided. Further, methods useful for studying the therapeutic profile of one or more drugs within a cell microenvironment, including but not limited to a tumor, are provided.

Abstract: A process is provided in which the resulting Fe-tCDTA contrast agent has a reduced osmolality. The process according to the invention comprises the following steps: a) preparing an aqueous solution of tCDTA and FeO(OH), tCDTA and FeO(OH) being present in a molar ratio of from 1:1 to 1:1.4; b) b.1) adjusting a pH of the aqueous solution to between pH 2.5 and pH 4.5 by adding a base, preferably meglumine, and separating the precipitate; or b.2) precipitating the Fe-tCDTA contrast agent from the aqueous solution by adding acetone, separating the precipitate, and preparing an aqueous solution from the precipitate; and c) adjusting a pH of the aqueous solution to between pH 6.5 and pH 8.0 by adding a base, preferably meglumine, and separating the precipitated FeO(OH).

Abstract: The present application provides a compound comprising at least one isotopically labeled nitrogen atom for use in diagnosing a condition or disease in a subject, compositions and kits comprising the compound and methods of using the same.

Abstract: The invention relates in general to hydrophilic, biocompatible dendronised polymers, to complexes comprising the dendronised polymers, to methods of preparing the dendronised polymer and to uses of the dendronised polymer as a non-viral transfection agent for the delivery of biomolecules, in particular, genome editing tools, into a cell.

Abstract: Controlled release hydrogel formulations of one or more simvastatin metabolites 3?-hydroxy simvastatin (hSV), 6?-exomethylene simvastatin (eSV), 3?,5?-dihydrodiol simvastatin, 3?,5?-dihydrodiol simvastatin (dSV), simvastatin-beta-hydroxy acid (SVA), and methods for the treatment of patients suffering from injured or degenerating substantially avascular cartilaginous tissue.

Abstract: Heptamethine cyanine fluorophore conjugates and conjugate precursors are disclosed. Methods of using the conjugates and conjugate precursors are also disclosed. The disclosed conjugates are neutral zwitterionic molecules and exhibit little or no aggregation.

Abstract: A molecular probe comprising a linear peptide that includes an amino acid sequence selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, and SEQ ID NO: 9; a contrast agent; and a non-peptide linker that covalently links the peptide to the contrast agent.

Abstract: This invention relates generally to cyanine-containing compounds; pharmaceutical compositions comprising cyanine-containing compounds; and methods of using cyanine-containing compounds for cancer cell imaging, cancer cell growth inhibition, and detecting cancer cells, for example. Compounds of the invention are preferentially taken up by cancer cells as compared to normal cells. This allows many uses in the cancer treatment, diagnosis, tracking and imaging fields.

Abstract: Disclosed herein are methods preparing a purified, carrier-free 68Ga solution. Tire present disclosure also provides systems for preparing a purified, carrier-free 68Ga solution. The present disclosure also provides compositions comprising the purified, carrier-free 68Ga solutions disclosed herein. Also provided are methods of administering compositions of the present disclosure to a patient in need thereof, for example, for imaging a disease or disorder, such as cancer.

Abstract: The present disclosure relates to the fields of near-infrared surgical navigation fluorescent molecules, cell marker imaging and so on, and in particular discloses an active targeting near-infrared fluorescent small molecule structure and a preparation method thereof. The present disclosure prepares the active targeting near-infrared fluorescent small molecule with pemetrexed disodium and derivatives thereof as active targeting groups by utilizing an organic total synthesis method. Such active targeting near-infrared fluorescent molecule has the advantages of high active targeting property, strong specificity, good water solubility, high fluorescence quantum yield and so on.

Abstract: Metal complexes including a radionuclide and a compound of Formula I and Formula II are potent inhibitors of PSMA.

Abstract: In some aspects, the present disclosure provides gadolinium based sensors which may be used to image zinc ions in vivo. In some embodiments, the compounds show appropriate reactivity with zinc ions while maintaining high relaxivity to achieve improved background relative to other sensors.

Abstract: Disclosed are methods of detecting eosinophil degranulation in the respiratory tract of subjects. Also, disclosed are methods of producing medical images of the respiratory tract of subjects. The method can include administering radiolabeled heparin to the respiratory tract of subjects, wherein the radiolabeled heparin binds to one or more eosinophil granule protein in the mucosal tissue of the respiratory tract.

Abstract: The present invention relates to diagnostic and therapeutic agents comprising recombinant antibody fragments to bind a protein associated with cancer and methods of use of these diagnostic and therapeutic agents.

Abstract: The present invention relates to methods of treating or inhibiting keloids in a subject with hypoxia-inducible factor-1 (HIF-1) inhibiting compounds, methods of screening or identifying compounds to induce cell death in keloids, and methods of inducing cell death in keloids.

Abstract: A molecular imaging agent including a detectable moiety, a chelation moiety, and a carrier moiety is provided. In one embodiment, the detectable moiety is coupled to the chelation moiety and the chelation moiety is linked to the carrier moiety. In another embodiment, the detectable moiety is 99mTc; the chelation moiety includes HYNIC; and the carrier moiety includes from N-terminus to C-terminus: a His6 purification tag, a human VEGFA polybasic tag sequence, and a human Fc stabilization segment.

Abstract: Disclosed herein are a dual-targeted carbonic anhydrase IX complex, a contrast agent comprising the same, and a synthesizing method thereof. The dual-targeted carbonic anhydrase IX complex includes a carbonic anhydrase IX (CA9) binding peptide, a sulfonamide derivative, and a metal chelating agent. The dual-targeted carbonic anhydrase IX complex has potential for use as a molecular nuclear drug.

Abstract: Disclosed is the use of a radiolabeled anti-nanobody in the prognosis and diagnosis of cancers. In particular, disclosed is an immunoconjugate for detecting a PD-L1 molecule. The immunoconjugate comprises the VHH chain of a specific anti-PD-L1 nanobody and a radionuclide, and can be used for non-invasive detecting of expression of the object PD-L1 to be detected. The immunoconjugate of the invention has small size and high specificity, and is suitable for systemic detection which simultaneously targets primary and metastatic tumors, and has high accuracy and low radiation dose.

Abstract: Embodiments of the present disclosure provide a nanoparticle based platform, and nanoallergens for identifying, evaluating and studying allergen mimotopes as multiple copies of a single mimotope or various combinations on the same particle. The nanoparticle is extremely versatile and allows multivalent binding to IgEs specific to a variety of mimotopes, simulating allergen proteins. Nanoparticles can include various molecular ratios of components. For example, the nanoallergens can include about 0.1-40% mimotope-lipid conjugate and about 60-99.9% lipid. The mimotope-lipid conjugate includes a mimotope, a first linker, and lipid molecule. Nanoallergens can be used in in vitro and in vivo applications to identify a specific patient's sensitivity to a set of epitopes and predict a symptomatic clinical response, identify allergen epitopes through blind screening peptide sequences from allergen protein, and in a clinical application similar to a scratch test.

Abstract: A method for preparing 18F radiolabeled biomolecules and agents for 18F-PET imaging is disclosed herein. A perfluoroaryl-conjugated target tracer is synthesized and purified with temperature and solvent conditions that are mild for the tracer molecule. The purified perfluoroaryl-conjugated target tracer is then labeled with 18F using 18F salts within a short reaction time, and with temperature and solvent conditions that are mild for the tracer molecule. The method provides a quick and convenient process that maintains the biological activities of the target molecules. The radio-labeled biomolecules may be used as contrast agents for Positron Emission Tomography (PET).

Abstract: Drift reduction adjuvant composition and agricultural sprays containing such agricultural compositions contain water, a Newtonian responding polymer such as guar gum, an emulsifier such as a polyoxyethylene sorbitan emulsifier, and an oil. When the agricultural spray containing the drift reduction adjuvant composition and a pesticide is delivered from an agricultural nozzle, it produces fewer droplets less than 150 ?m in diameter and either reduces, maintains or increases (e.g., by up to 30 percentage points) the number of ultra-coarse droplets above 622 ?m in diameter compared to an agricultural spray of the pesticide without the drift reduction adjuvant composition sprayed under the same conditions.

Abstract: This invention concerns various methods of using labeled HSP90 inhibitors to improve treatment of cancer patients with HSP90 inhibitors, including ex vivo and in vivo methods for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor.

Abstract: The invention provides compositions, kits and methods to treat a hyperproliferative disorder with an agent that increases expression of MCR1 and an MCR1 ligand. The invention also provides a method of treating drug-resistant melanoma, comprising administering an MCR1 ligand to a patient in need thereof. The present invention also provides in certain embodiments a melanoma-targeting conjugate comprising Formula I: T-L-X wherein T is a MCR1 ligand, L is a linker, and X an anti-cancer composition, for the therapeutic treatment of a hyperproliferative disorder. The present invention also provides methods, kits and uses of the conjugate of Formula I.

Abstract: A method of treating a chronic wound may comprise applying to the wound a first scaffold comprising an electrospun polymer fiber. The electrospun fiber may comprise a polymer selected from the group consisting of polyglycolic acid, poly(lactide-co-caprolactone), polylactic acid, polycaprolactone, copolymers thereof, and combinations thereof. The first scaffold may have a thickness from about 50 ?m to about 1 mm, a length from about 1 cm to about 20 cm, and a width from about 1 cm to about 15 cm. The method may further comprise keeping the first scaffold on the chronic wound for a time period of about 3 days to about 21 days. After the time period passes, the chronic wound may have a decreased planimetric area.

Abstract: Provided herein are imaging agents, antidotes to the imaging agents and methods of using the same to image a thrombus or blood clot or thrombin including sites of thrombin accumulation and to diagnose and treat thrombosis. The imaging agents include an aptamer capable of binding the thrombus or thrombin in particular linked to a reporter moiety. The imaging agents may be used to label the thrombus or sites of thrombin accumulation. Antidotes capable of binding to the aptamer in the imaging agent are also provided. The antidotes may further be linked to a quencher capable of quenching the reporter moiety.

Abstract: A cancer targeting composition, kit, and method for treatment of cancer cells overexpressing somatostatin receptors is disclosed. The composition includes a radioisotope, a chelator, and a targeting moiety. The chelator includes a nitrogen ring structure including a tetraazacyclododecane, a triazacyclononane, and/or a tetraazabicyclo [6.6.2] hexadecane derivative. The targeting moiety includes a somatostatin receptor targeting peptide. The somatostatin receptor targeting peptide includes an octreotide derivative. The targeting moiety is chelated to the radioisotope by the chelator whereby the cancer cells are targeted for elimination.

Abstract: The present invention provides 18F-labeled amino acids or derivatives thereof having formula (I) and methods of making same, which can be suitable for PET imaging:

Abstract: Embodiments of the invention provide methods of synthesizing 18F-tetrafluoroborate (18F-TFB) via direct radiofluorination on boron trifluoride (BF3) to enhance both labeling yield and specific activity. Uses of 18F-TFB are also contemplated.

Abstract: Radiolabeled anti-LAG3 antibodies and their use in immuno-PET imaging are provided herein. Included are methods of detecting the presence of LAG3 proteins in a patient or sample.

Abstract: Disclosed herein are multifunctional nanoparticle compositions. The compositions can be useful for the treatment of cancer by enhancing the anti-tumor effectiveness of radiation directed to a tissue, cell or a tumor and the methods of use thereof. The multifunctional nanoparticle composition comprises a metal oxide nanoparticle core; a functional coating on the surface of the metal oxide nanoparticle core; and a matrix carrier in which the coated nanoparticle is embedded.

Abstract: The present disclosure relates to a method for labeling a biomolecule, a fluorescent dye, or a nanoparticle compound with a radioisotope, comprising: (a) providing a cyclooctyne compound represented by the following formula (I) comprising the biomolecule, the fluorescent dye, or the nanoparticle compound which is bound to a cyclooctyne moiety of the cyclooctyne compound; and (b) reacting the cyclooctyne compound of formula (I) with a quinone compound represented by the following formula (II) to give a biomolecule, a fluorescent dye, or a nanoparticle compound labeled with the radioisotope: in formula (I), (Z is the biomolecule, the fluorescent dye, or the nanoparticle compound) in formula (II), (b is 0 or an integer from 1 to 10; L is CH2, —COO—, or —CONH—; M is the radioisotope).

Abstract: The present invention provides bi-terminal PEGylated peptide conjugates that target an integrin such as ?v?6 integrin. In particular embodiments, the peptide conjugates of the present invention further comprise a biological agent such as an imaging agent or a therapeutic agent, e.g., covalently attached to one of the PEG moieties. The peptide conjugates of the present invention are particularly useful for imaging a tumor, organ, or tissue and for treating integrin-mediated diseases and disorders such as cancer, inflammatory diseases, autoimmune diseases, chronic fibrosis, chronic obstructive pulmonary disease (COPD), lung emphysema, and chronic wounding skin disease. Compositions and kits containing the peptide conjugates of the present invention find utility in a wide range of applications including, e.g., in vivo imaging and immunotherapy.

Abstract: The present invention is drawn to the use of the compounds highlighted in Tables 1 & 2 and analogs thereof, for enhancing IR-mediated cellular cannibalism in cancer cells. Said compounds are herein called “enhancers of IR-mediated cellular cannibalism”. They can be used to enhance tumor immunogenicity and/or to induce a significant protective anticancer immune response in subjects that will receive or that have received a radiotherapy treatment. In other words, said compounds can be used to potentiate a radiotherapy treatment in a subject in need thereof. Said compounds are preferably chosen in the group consisting of: Mebhydroline 1,5-napthalene disulfonate salt, Flurbiprofen, Minaprine dihydrochloride, Myricetin, Digoxin, Digitoxin, Lanatoside, LOPA87, VP331, RN-1-026, SG6163F, VP450, and VP43.

Abstract: Provided herein are conjugates including a polypeptide and one or more drug molecules. The polypeptide includes one or more charged motifs, and may further include one or more uncharged motifs. The conjugates may be used to effectively deliver the drug molecule to a subject.

Abstract: The present invention provides bispecific antigen-binding molecules comprising a first antigen-binding domain that specifically binds human CD28, and a second antigen-binding molecule that specifically binds human MUC16. In certain embodiments, the bispecific antigen-binding molecules of the present invention are capable of inhibiting the growth of tumors expressing MUC16, such as ovarian tumors. The antibodies and bispecific antigen-binding molecules of the invention are useful for the treatment of diseases and disorders in which an up-regulated or induced targeted immune response is desired and/or therapeutically beneficial.

Abstract: Described herein are compositions of antibodies and carrier proteins and methods of making and using the same, in particular, as a cancer therapeutic. Also described are lyophilized compositions of antibodies and carrier proteins and methods of making and using the same, in particular, as a cancer therapeutic.

Abstract: The present invention relates to implants comprising a deformable body formed of a polymer comprising functional groups capable of cross-linking to form a cross-link; said body provided in a first configuration which is cross-linked to a second configuration upon application of a selected stimuli; wherein said selected stimuli causes said cross-linking of said functional groups.

Abstract: Methods for producing an anti-tumor effect in a subject suffering from a cancer or a tumor are disclosed. The methods comprise administering to the patient a Vascular Disrupting Agent (VDA) that a combretastatin agent and one or more antibodies selected from the group consisting of: a CTLA-4 antibody, a PD-1 antibody, a PD-L1 antibody, and a PD-L2 antibody in amounts effective therefor. Examples of combretastatin include CA1P, CA4P, and their corresponding salts and prodrugs. The combination of the VDA and one or more of the antibodies produced a synergistic anti-tumor effect.

Abstract: Provided herein are protein contrast agents and targeted protein contrast agents, formulations thereof, and methods of use, including but not limited to, as a magnetic resonance imaging contrast agent.

Abstract: The present invention provides compounds that have motifs that target the compounds to cells that express integrins. In particular, the compounds have peptides with one or more RD motifs conjugated to an agent selected from an imaging agent and a targeting agent. The compounds may be used to detect, monitor and treat a variety of disorders mediated by integrins.

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: Compositions and methods are described for stabilizing a radio-iodinated monoclonal IgG antibody for up to 17 days against radiolytic decomposition. The stabilized radiolabeled murine antibody binding the CD45 antigen expressed on various forms of lymphomas is useful as a radio-therapeutic and diagnostic agent in the treatment of human malignancies of hematopoietic origin, including lymphomas.