Abstract: A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe comprises a polypeptide represented by the following formula (1), (2), or (3), or a polypeptide having homology with the foregoing polypeptide, (SEQ?ID?NO.?1) Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2?(1) (SEQ?ID?NO.?2) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2?(2) (SEQ?ID?NO.?3) B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2?(3) where, in the formulae (1) and (2), “X” represents a lysine residue, an amino group of a side chain of the lysine residue being labeled with a radioactive nuclide, and “Z—” indicates that an ?-amino group at an N-terminus is not modified, or is modified with a modifying group having no electric charge; in the formula (3), “B—” indicates that an ?-amino group at an N-terminus is labeled with a radioactive nuclide; and in the formulae (1), (2), and (3), “—NH2” indicates that a carboxyl group at a C-terminus is amidated.

Abstract: A microreactor for preparing a radiolabeled complex or a biomolecule conjugate comprises a microchannel for fluid flow, where the microchannel comprises a mixing portion comprising one or more passive mixing elements, and a reservoir for incubating a mixed fluid. The reservoir is in fluid communication with the microchannel and is disposed downstream of the mixing portion. A method of preparing a radiolabeled complex includes flowing a radiometal solution comprising a metallic radionuclide through a downstream mixing portion of a microchannel, where the downstream mixing portion includes one or more passive mixing elements, and flowing a ligand solution comprising a bifunctional chelator through the downstream mixing portion. The ligand solution and the radiometal solution are passively mixed while in the downstream mixing portion to initiate a chelation reaction between the metallic radionuclide and the bifunctional chelator. The chelation reaction is completed to form a radiolabeled complex.

Abstract: Polypeptides that target and/or bind to EGFL7 or its receptor and thereby reduce EGFL7 pro-angiogenic activity are provided. In this way, the polypeptides are, in an aspect, useful in the treatment of diseases, disorders, or conditions that involve pathological angiogenesis, such as, for example, cancer.

Abstract: Methods and materials for the imaging of cells containing active proteases such as cathepsin are disclosed. The present materials include activity based probes that bind to an enzyme and are subsequently cleaved. Cleavage results in a fluorescent signal due to removal of a quenching group which, when present on the probe causes altered or no fluorescence. The probes employ an acyloxymethyl ketone reactive group, one or more amino acids for determining specificity, a fluorophore and a quencher. The probes are cell permeable and may use, for example, a QSY7 (diarylyrhodamine) quencher and a BODIPY (bora-diaza-indecene) dye.

Abstract: It is an object of the present invention to provide a targeting agent, which enables the delivery of a drug to tumor sites or the imaging of tumor sites by utilizing its effect of accumulating to such tumor sites. The present invention provides a targeting agent for tumor site, which comprises a hydrophilic polymer-modified carrier coated with a gelatin-like protein that has repeats of a sequence represented by Gly-X-Y characteristic to collagen and has two or more sequences of cell adhesion signals in a single molecule wherein X and Y each independently represent an amino acid and a plurality of Gly-X-Y sequences may be the same or different.

Abstract: A ligand and a metal complex having the ligand are provided. The ligand and a paramagnetic metal ion form a metal complex with high stability, high relaxivity and high biocompatibility. The metal complex of the present invention is applicable to the preparation of MRI contrast agents for detecting atherosclerosis. The MRI contrast agent includes a peptide sequence specific to a matrix metalloprotease, and can be recognized by a pathological thrombocyte to target a specific site, so as to enhance the imaging contrast.

Abstract: The invention provides MRI detectable species of formula (I) Dp-Sn-Nm??(I) wherein D is a MRI detectable moiety S is a spacer N is a molecule of a nutrient or pseudo-nutrient n is 0 or an integer m is an integer and p is an integer. These compounds are useful for internalizing into tumor cells an amount of the MRI detectable moiety that is distinguishably higher than the amount internalized in normal healthy cells thus allowing the diagnosis of tumors. The internalization of the MRI detectable moiety involves the nutrients or pseudo-nutrients transporting system. Preferred compounds of formula (I) are those wherein D is the chelated complex of a paramagnetic metal ion.

Abstract: The present application provides compositions and methods for imaging traumatic brain injury using PET. The present application discloses using PET ligands targeting infiltrating neutrophils, such as a ligand of FPR, is useful for imaging inflammation. In one aspect, the ligand and imaging agent cFLFLF-PEG-64Cu.

Abstract: Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.

Abstract: Provided herein are methods to generate and screen peptides that exhibit drug like stabilities in vitro and in vivo. By selecting for enzyme resistance, Applicants are able to derive peptides that are not only stable to a broad spectrum of proteases, but also stable to other drug processing enzymes such as cytochrome P450s. This approach provides a general method to the rapid development of highly stable peptides for therapeutic development and diagnosis. The peptides are further modified for oral bioavailability.

Abstract: Reduced lysine chlorotoxin polypeptides that may be used to generate single species conjugates of chlorotoxin. Conjugates comprising such chlorotoxin polypeptides and pharmaceutical compositions thereof. Methods of using such compositions and/or conjugates.

Abstract: The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are functionalised BTMs useful in the method, as well as methods of preparing such functionalised BTMs under mild conditions.

Abstract: The present disclosure provides peptide constructs for diagnostic imaging and therapeutic applications, using pegylated peptides which exhibit specific binding for a target molecule of interest, such as a biomarker of a disease or disorder.

Abstract: The invention provides, in some embodiments, methods relating to assessing increased risk of developing atrial fibrillation (AF), and/or the likelihood of responding to particular AF therapies using imaging agents comprising an MMP inhibitor linked to an imaging moiety. The invention further provides methods for evaluating the presence of the risk of developing other cardiovascular conditions and assessing the effectiveness of treatment or other intervention for such conditions by determining MMP levels.

Abstract: The invention described herein pertains to targeted drug delivery conjugates comprising folate receptor ? (FR-?) selective binding ligands and methods for diagnosing, monitoring, and eliminating pathological cells that express FR-?.

Abstract: Provided herein are methods of reducing liver uptake in vivo of a polypeptide that specifically binds to a target comprising: (a) providing a polypeptide that specifically binds to a target; and (b) substituting at least one basic or at least one neutral amino acid residue of the native polypeptide from step (a) with an acidic amino acid residue to produce a modified polypeptide, wherein the modified polypeptide demonstrates an isoelectric point at least 0.05-0.1 pH points less than the isoelectric point of the native polypeptide. Also provided are polypeptides made using the inventive methods as well as imaging techniques that employ the methods and agents.

Abstract: The present invention is directed to methods and compositions for the treatment and diagnosis of neuroectodermally-derived tumors, such as gliomas. The inventive methods of treatment generally include local (e.g., intracavitary) administration of a chloroxotoxin moiety conjugated to a cytotoxic moiety to a patient. Also provided are diagnostic methods for screening neoplastic neuroectodermal tumors.

Abstract: The present invention provides a method for the generation of 223Ra of pharmaceutically tolerable purity comprising i) preparing a generator mixture comprising 227Ac, 227Th and 223Ra; ii) loading said generator mixture onto a strong base anion exchange resin; iii) eluting said 223Ra from said strong base anion exchange resin using a first mineral acid in an alcoholic aqueous solution to give a first eluted 223Ra solution; iv) loading the 223Ra of the first eluted 223Ra solution onto a strong acid cation exchange resin; and v) eluting the 223Ra from said strong acid cation exchange resin using a second mineral acid in aqueous solution to provide a second eluted solution. The invention additionally provides products of corresponding purity and/or products obtained or obtainable by such a method.

Abstract: The invention concerns compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium. The invention also concerns methods for obtaining said compounds, screening methods capable of selecting such compounds for chemical synthesis thereof and their diagnostic applications, in particular in PET, PET/IRM, PET CT imaging.

Abstract: The present invention relates to functional binding fragments comprising the minimal binding fragments of VAR2CSA, to antibodies against such binding fragments of VAR2CSA, nucleic acids encoding such fragments of VAR2CSA as well as methods for their production. The invention further relates to conjugates and fusion proteins of VAR2CSA polypeptides including the minimal binding fragments and their use, in particular in the treatment of conditions associated with expression of chondroitin sulfate A (CSA), such as an inappropriate expression of chondroitin sulfate A (CSA).

Abstract: The present disclosure relates to a method of treating, ameliorating or preventing a disorder by blocking the signaling pathway of c-Met, wherein said method comprises the step of administering a therapeutically effective amount of a composition to a subject in need thereof, which composition contains a lipocalin mutein or a fragment or a variant thereof. In addition, the present disclosure relates to a diagnostic composition suitable for use in, e.g., an immuno-imaging technique to detect the presence of c-Met as well as the uses thereof.

Abstract: It is an object of the present invention to provide a targeting agent, which enables the delivery of a drug to tumor sites or the imaging of tumor sites by utilizing its effect of accumulating to such tumor sites. The present invention provides a targeting agent for tumor site, which comprises a hydrophilic polymer-modified carrier coated with a gelatin-like protein that has repeats of a sequence represented by Gly-X-Y characteristic to collagen and has two or more sequences of cell adhesion signals in a single molecule wherein X and Y each independently represent an amino acid and a plurality of Gly-X-Y sequences may be the same or different.

Abstract: The invention provides an insulin-like growth factor-1 (IGF-1) receptor ligand carrying a therapeutic radionuclide for treatment of cancer is provided. A method of treating cancer using the IGF-1 receptor ligand carrying a therapeutic radionuclide is also provided. An anti-cancer therapeutic agent containing an IGF-1 receptor ligand linked to a toxin is also provided, as are methods of using the toxin conjugates for treatment of cancer.

Abstract: The present application discloses compositions and methods of synthesis and use of 18F or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.

Abstract: The invention relates to methods for producing papilloma-derived nanosphere particles that contain therapeutic, diagnostic, or other agents. The invention also provides nanosphere particle preparations that are useful for selectively delivering therapeutic, diagnostic, and/or other agents to cancer cells of subjects without eliciting a serotype-specific immunogenic response in the subjects.

Abstract: The present invention relates to a method of labelling biological molecules with 18F, via attachment to fluorine to a macrocyclic metal complex of a non-radioactive metal, where the metal complex is conjugated to the biological molecule. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

Abstract: Methods and compositions pertaining to botulinum neurotoxin (BoNT) light chain epitopes are provided. In particular, the methods and compositions relate to the use of real and mimetic BoNT light chain epitopes for generating an immune response in a subject, and for immunization against BoNT toxicity. Methods and compositions for detecting, isolating, and purifying BoNT epitopes and anti-BoNT antibodies are also provided.

Abstract: A method for identifying a molecule that binds an irradiated tumor in a subject and molecules identified thereby. In some embodiments, the method includes the steps of (a) exposing a tumor to ionizing radiation; (b) administering to a subject a library of diverse molecules; and (c) isolating from the tumor one or more molecules of the library of diverse molecules, whereby a molecule that binds an irradiated tumor is identified. Also provided are targeting ligands that bind an irradiated tumor and therapeutic and diagnostic methods that employ the disclosed targeting ligands.

Abstract: The present invention relates to a pharmaceutical composition comprising a cyclotide for use in immune suppression as well as to a method for immune suppression comprising the step of administering an effective amount of a pharmaceutical composition comprising such a cyclotide to a subject in need thereof. The present invention also relates to a pharmaceutical composition comprising a cyclotide for use in treating or preventing a disorder selected from the group consisting of (i) an autoimmune disorder; (ii) a hypersensitivity disorder; and (iii) a lymphocyte-mediated inflammation. Likewise, the present invention also relates to a method for treating or preventing a disorder selected from the group consisting of (i) an autoimmune disorder; (ii) a hypersensitivity disorder; and (iii) a lymphocyte-mediated inflammation.

Abstract: The invention provides an automatic synthesizer apparatus and method for producing radiopharmaceutical tumor imaging agent Gallium-68-DOTATATE with one button control process to effectively isolate the medication in vials from the contamination of environment and manual operations, saving the costs of investment in production with alleviation of the critical standard required for the environmental equipments to be used for production.

Abstract: The invention provides compositions and method for delivering a therapeutic or diagnostic agent to a disease site in a mammal, the method comprising administering to the mammal a therapeutically or diagnostically effective amount of a pharmaceutical composition, wherein the pharmaceutical composition comprises the therapeutic or diagnostic agent coupled to a Procaspase 8 polypeptide and a pharmaceutically acceptable carrier.

Abstract: Disclosed are compositions that contain a plurality of biocompatible self-assembling molecules that transform from isolated molecules or spherical micelles in the circulation into cylindrical nanofibers in the acidic extracellular environment of tumors which can be used to achieve a higher relative concentration of imaging, drug delivery, or radiotherapeutic agents at the tumor site compared to non-tumor tissues. This transition is rapid and reversible, indicating the system is in thermodynamic equilibrium.

Abstract: In some aspects, the present invention provides novel ligands, which may be used to make novel dual-modality imaging agents, for example, for PET and MRI imaging. In further aspects, by the present disclosure also provides methods of use and methods of preparation of the novel ligands, metal complexes, and imaging agents thereof.

Abstract: Provided herein are compositions and methods for the assembly of a bioluminescent complex from two or more non-luminescent (e.g., substantially non-luminescent) peptide and/or polypeptide units. In particular, bioluminescent activity is conferred upon a non-luminescent polypeptide via structural complementation with another, complementary non-luminescent peptide.

Abstract: Systems and reagents for identification, characterization and/or targeting of particular tissue or cell markers are disclosed. Methods and compositions for in vivo and in vitro targeting of particular targets are also disclosed. Peptides are employed for targeted delivery of therapeutic or imaging agents.

Abstract: The present invention relates to hydrophobic modified peptides for the specific delivery of labels to the liver, preferably to hepatocytes, in vitro as well as in vivo. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the label(s) to be specifically delivered to the liver. The present invention furthermore relates to the diagnostic use of the inventive hydrophobic modified peptides as well as to a method for the diagnosis of liver diseases or disorders.

Abstract: The present invention relates to a peptide that passes through a blood-brain barrier and binds specifically to apoptotic cells in neurodegenerative brain disease-affected sites, and uses thereof. Therefore, the peptide of the present invention can be used for detecting and imaging apoptotic cells in neurodegenerative brain disease-affected sites, and for targeted drug delivery and theranosis of neurodegenerative brain diseases.

Abstract: Provided herein are compositions and methods for the assembly of a bioluminescent complex from two or more non-luminescent (e.g., substantially non-luminescent) peptide and/or polypeptide units. In particular, bioluminescent activity is conferred upon a non-luminescent polypeptide via structural complementation with another, complementary non-luminescent peptide.

Abstract: The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.

Abstract: The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using the radioiodinated BTMs.

Abstract: A radiotherapy method, comprising positioning a predetermined amount of a radionuclide selected from the group consisting of Radium-223, Radium-224, Radon-219 and Radon-220, in proximity to and/or within a tumor of a subject, for a predetermined time period. The predetermined amount and the predetermined time period are selected sufficient for the radionuclide to administering a predetermined therapeutic dose of decay chain nuclei and alpha particles into the tumor.

Abstract: There is provided a radiolabelled peptide-based compound for diagnostic imaging using positron emission tomography (PET). The compound may thus be used for diagnosis of malignant diseases. The compound is particularly useful for imaging of somatostatin overexpression in tumors, wherein the compound is capable of being imaged by PET when administered with a target dose in the range of 150-350 MBq, such as 150-250 MBq, preferable in the range of 191-210 MBq.

Abstract: The present invention is related to antigen from Chlamydia trachomatis which are recognized by specific antibodies from individuals infected with Chlamydia or which can induce T cells from the same individuals to secrete gamma-interferon. The T cell reactive antigens are present in a whole-cell lysate and have apparent molecular weights of 5-12, 16-20, 25-35 and 58-74 kDa as determined by SDS-PAGE. The antigens of the invention are believed to be useful in vaccines but also as diagnostic compositions.

Abstract: The present invention provides a pharmaceutical composition containing hemoglobin-based therapeutic agent for treating cancer. The hemoglobin moiety can target cancer cells and the therapeutic moiety (i.e. active agent/therapeutic drug) can kill the cancer cells efficiently. The hemoglobin-based therapeutic agent used in the present invention can be used in the treatment of various cancers such as pancreatic cancer, leukemia, head and neck cancer, colorectal cancer, lung cancer, breast cancer, liver cancer, nasopharyngeal cancer, esophageal cancer, prostate cancer, stomach cancer and brain cancer. The composition can be used alone or in combination with other therapeutic agent(s) such as chemotherapeutic agent to give a synergistic effect on cancer treatment, inhibiting metastasis and/or reducing recurrence. The presently claimed hemoglobin-based 5FU-two-dye conjugate and/or hemoglobin-based 5FU-one-dye conjugate can also be used in live-cell imaging and diagnostic imaging.

Abstract: HER2 binding polypeptides comprising the amino acid sequence EX1 RNAYWEIA LLPNLTNQQK RAFIRKLYDD PSQSSELLX2E AKKLNDSQ wherein X1 in position 2 is M, I or L, and X2 in position 39 is S or C (SEQ ID NO:1) are disclosed. Moreover, such peptides comprising a chelating environment are disclosed. Also radiolabeled polypeptides formed by the peptides comprising a chelating environment and radionuclides are disclosed. Furthermore, methods of in vivo imaging of the body of a mammalian subject having or suspected of having a cancer characterized by overexpression of HER2 comprising administration of such a radiolabeled polypeptide followed by obtainment of an image of the body using a medical imaging instrument and also methods of treating such cancer are disclosed. Furthermore, the use of such a radiolabeled polypeptide in diagnosis and treatment of cancer characterized by overexpression of HER2.

Abstract: It is an object of the present invention to provide a targeting agent that enables drug delivery to a neovascular site and the imaging of such a neovascular site, utilizing the effect of the agent to accumulate in the neovascular site. The present invention provides a targeting agent to a neovascular site, which comprises a gelatin-like protein.

Abstract: Provided are fragments of human p97 (melanotransferrin) polypeptides having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, conjugates comprising said p97 fragments, and related methods of use thereof, for instance, to facilitate delivery of therapeutic or diagnostic agents across the BBB.

Abstract: There is provided a method for preparing a 99mTc labeled gold nanoparticles-gold binding peptide, including: (a) coating gold nanoparticles with a gold binding peptide; and (b) labeling a composed 99mTc tricarbonyl precursor on the gold binding peptide coated on the gold nanoparticles. The 99mTc labeled gold nanoparticles-gold binding peptide prepared by the method according to the present invention is expected to be usefully employed for manufacturing a molecular contrast agent (imaging agent) which is traceable in organisms using imaging apparatuses such as gamma imaging and single photon emission computed tomography due to high labeling yield and good in-vivo stability.

Abstract: The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein 11b/IIIa antagonists for imaging of thrombi.

Abstract: The invention relate to the new conjugated somatostatin analogs of formula (I), wherein A- is H or TAG-B—, wherein —B— is 0 or a spacer, wherein TAG is a chelating agent (e.g. DOTA), a fluorescent dye, (e.g. Bodipy-B derivative, a Rho-damine-B derivative, a Fluorescein-B derivative, a Cyanine-B derivative, a Porphyrin-B derivative), a bimodal agent, or a cytotoxic agent (e.g. a doxorubicin derivative) wherein R1 is CI-C4 alkynyl radical when R2 is CI-C4 azido radical and viceversa and methods for preparing same, pharmaceutical compositions comprising them and their use in imaging and the treatment of cancer.