Abstract: The invention provides conjugates, comprising an organ, tissue or tumor cell homing molecule linked to a moiety. Such a moiety can be, for example, an oligonucleotide, small interfering RNA, gene, virus, protein, pharmaceutical or detectable agent. In addition the invention provides methods to diagnose or treat neuronal or neuromuscular disease, or a pathology of the brain, or a tumor of neuronal or neuroectodermal origin, by administrating to a subject having or suspected of having a pathology a molecule or conjugate that homes to, binds to and is taken up by the brain cells or neuronal cells, or by the tumor cells of neuronal or neuroectodermal origin. The invention also provides a method of identifying and measuring neurite growth in neuronal cells.

Abstract: A conjugate of human albumin (HA) and 2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (p-SCN-Bn-DOTA) insoluble in aqueous medium at a pH of 3-8.5 and whose IR spectrum shows an absorption at about 700 cm?1 is described; a complex is further described consisting of a conjugate of HA and p-SCN-Bn-DOTA (HAC) according to claim 1 or 2 and a radioactive isotope of an element selected among the group consisting of P, Sr, Rh, Pd, I, Sm, Er, Au, At Bi, In, Lu, Y, Re, Cu and Ag, as well as procedures for preparing said conjugate and said complex as well as the use of such conjugate in the identification of mammalian neoplastic lesions by the R.O.L.L. methodology (“Radioguided Occult Lesion Localization”).

Abstract: The present invention is directed to novel non-invasive diagnostic tools/compounds comprising a cyclic peptide wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. The present invention represents a step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma.

Abstract: Disclosed are Drug Delivery Molecules (DDMs) which both facilitate functional imaging, as by PET, MRI or SPECT, and create a biological effect and methods of their use. These DDMs which are variously designed to target specific receptors, internalized and then function biologically, as for purposes of cell destruction or therapy.

Abstract: Provided herein are novel compounds based on xanthene, for example biarsenical compounds, which are useful as molecular probes. The compounds contain at least one isotope atom, such as a radioisotope atom. Methods for visualizing tetracysteine-tagged analyte molecules such as proteins using said compounds, methods for synthesizing said compounds, and methods for treating cancer or other hyperproliferative disorders using said compounds are also provided.

Abstract: Radiolabeled bombesin (BBN) analogs that bind to the gastrin-releasing peptide receptor (GRPR) represent a topic of active investigation for the development of molecular probes for positron emission tomography (PET) or single-photon emission computed tomography (SPECT) of prostate cancer (PCa). RM1 and AMBA have been identified as the two most promising BBN peptides for GRPR-targeted cancer imaging and therapy. In this study, to develop a clinically translatable BBN-based PET probe, we synthesized and evaluated 18F—AlF- and 64Cu-radiolabeled RM1 and AMBA analogs for their potential application in PET imaging of PCa.

Abstract: The present invention relates to the diagnosis, treatment and monitoring of mood disorders. For example, a diagnosis may be performed by determining whether a monoamine oxidase in a vertebrate is elevated compared to a healthy control subject. Methods of monitoring treatments and methods for identifying treatments for mood disorders are also provided.

Abstract: The invention provides SPARC and Albumin binding peptides for the targeting of disease sites, such as tumors, with therapeutic and diagnostic agents. In particular, compositions comprising SPARC binding peptide-Antibody Fc domain fusion proteins and methods of their use are disclosed.

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 then 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 bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.

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 invention relates to a sentinel lymph node marker comprising an albumin; a radioactive isotope and/or near infrared dye which is bound to the albumin; and a visible dye which is bound to the albumin, a preparation method thereof, a kit for multimode imaging of a sentinel lymph node to prepare the sentinel lymph node marker, and a method for multimode imaging of a sentinel lymph node using the same. The sentinel lymph node marker of the invention remains in the sentinel lymph node for a long period of time and allows for multimode imaging of the sentinel lymph node. Thus, using this marker the sentinel lymph node can be accurately identified in vivo by near infrared imaging and/or gamma imaging without incision of skin, and the location of the identified sentinel lymph node can be precisely identified with the naked eye during a surgical operation of removing the identified sentinel lymph node.

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: A method including isotope labeling of a newly synthesized protein in a sufficient quantity such that a newly synthesized protein spectra and the pre-existing protein spectra are sufficiently separated. A further method including determining a ratio of a new and a pre-existing protein from mass spectra obtained by using mass spectrometry. In this method a resultant spectrum may be presented as integrated peak heights for a corresponding mass to charge ratio in the “centroid” mode.

Abstract: Substituted aryl-boron compounds comprising at least one 18F atom, as illustrated by the formula (I), where at least one of Y1 or Y2 is 18F and A1 is a substituted aromatic ring, with G1-5 being, independently, C or N, and where the substitutents of the aromatic ring or polycyclic moiety (other than boron) comprise at least one electron-withdrawing group (EWG), providing that sigma total (?total) for all substituents on the aromatic ring or polycyclic moiety except B is about 0.06 or more when said at least one EWG is positioned ortho to B, or about 0.2 or more when no EWG is positioned ortho to B. The compounds include neutral (N=1) and ionic borate (N=2) embodiments. The compounds are useful as positron emission tomography (PET) imaging agents.

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 relates to contrast agents for detection of the Urokinase Plasminogen Activator Receptor (uPAR). More specifically the invention relates to contrast agents comprising a peptidic vector binding to the uPAR, labelled with an imageable moiety.

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: Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.

Abstract: The present invention describes chemically modified avidins that have higher permanence in treated tissues compared to wild type avidin. Avidin oxidation is performed by periodate incubation in the presence of the low affinity ligand HABA which, occupying the biotin binding sites, prevents protein denaturation during the oxidation step. Periodate oxidation generates CHO groups from avidin mannose ring opening that, once injected, react with tissue NH2 residues to form stable Schiff's bases. The anchored avidins maintain the ability to bind biotinylated agents endowed of therapeutic activity, like radiolabeled biotins, stem cells and somatic cells, useful for brachytherapies like Intraoperative Avidination Radionuclide Therapy (IART®) or degenerative or genetic diseases.

Abstract: A method of preparing a fibrinogen rich composition is disclosed. One embodiment of the method involves contacting plasma with a hydrogel capable of increasing in mass upon contact with said plasma; maintaining said contact for a period of time sufficient for said hydrogel to absorb a substantial amount of at least the water from said plasma to produce a swollen hydrogel and a fibrinogen rich phase; and separating said fibrinogen rich phase from said swollen hydrogel; whereby said fibrinogen rich composition is produced.

Abstract: A bifunctional compound with a monosaccharide and a N2S2 ligand, and more particularly, a bifunctional compound with a N2S2 ligand and aminohexylacetyl galactosamine (ah-GalNAc4) is provided. A method for preparing the bifunctional compound with a monosaccharide and a N2S2 ligand is also provided, including activating a carboxyl group in an organic ligand, reacting the activated carboxyl group with a galactopyranoside through amidation, and then hydrolyzing. The bifunctional compound of the present invention is widely useful in nuclear medicine for preparation of liver imaging agents for assisting in correct diagnosis of diseases.

Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.

Abstract: The present invention relates to: TNF-? antagonists containing IGFBP5 protein, variants thereof, or fragments thereof; and the use of the TNF-? antagonists. More specifically, the present invention relates to: a polynucleotide encoding the protein, variants thereof, or fragments thereof; a vector containing the polynucleotide; a transformant containing the vector; and a method for screening a therapeutic agent for TNF-? overexpression-related diseases by checking whether the mutual reaction thereof is facilitated after treating with candidates to the cell expressing the IGFBP5 protein, variants thereof, or fragments thereof, and the TNFR1.

Abstract: The present invention relates to improved radiotracer imaging agent compositions, which comprises 18F-labelled biological targeting moieties, wherein impurities which affect imaging in vivo are identified and suppressed. Also provided are radiopharmaceuticals comprising said improved compositions, together with radiofluorinated aldehyde compositions useful in preparing said radiotracer compositions. The invention also includes methods of imaging and/or diagnosis using the radiopharmaceutical compositions described.

Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.

Abstract: The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to a method of labelling a biological targeting molecule with a radioisotope. The method of the invention is particularly suitable for use with an automated synthesizer apparatus. Also provided are precursors in sterile form, as well as cassettes comprising such precursors useful in the method.

Abstract: The present invention relates to radiopharmaceutical imaging in vivo of apoptosis and other forms of cell death. The invention provides PET imaging agents which target apoptotic cells via selective binding to the aminophospholipid phosphatidylethanolamine (PE), which is exposed on the surface of apoptotic cells. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

Abstract: Porphyrazines capable of localizing in a tumor of a mammal are disclosed. The porphyrazines are used in methods of imaging a tumor and in methods of treating tumors, either alone or in combination with a chemotherapeutic agent and/or radiation.

Abstract: This invention provides a polyvalent vaccine comprising at least two conjugated antigens selected from a group containing glycolipid antigen, polysaccharide antigen, mucin antigen, glycosylated mucin antigen and an appropriate adjuvant. This invention also provides a multivalent vaccine comprising at least two of the following: glycosylated MUC-1-32mer, Globo H, GM2, Ley, Tn(c), sTN(c), and TF(c). This invention provides the vaccine above, wherein the adjuvant is saponin-based adjuvant. This invention provides a method for inducing immune response in a subject comprising administering an effective amount of the vaccine above to the subject. Finally, this invention provides a method for treating cancer in a subject comprising administering an appropriate amount of the vaccine above to the subject.

Abstract: The invention generally features compositions and methods based on the structure-based design of alpha 1-3 N-Acetylgalactosaminyltransferase (alpha 3 GalNAc-T) enzymes from alpha 1-3galactosyltransferase (a3Gal-T) that can transfer 2?-modified galactose from the corresponding UDP-derivatives due to substitutions that broaden the alpha 3Gal-T donor specificity and make the enzyme a3 GalNAc-T.

Abstract: The present invention is directed to the use of an irreversible ligand of a serine protease selected from the group consisting of leukocyte elastase, thrombin, tissue plasminogen activator (t-PA) and plasmin for the molecular imaging of said serine protease and the diagnosis of pathophysiological conditions associated with said serine protease activity.

Abstract: The present invention provides polypeptide inhibitors of HSP27 kinase, compositions thereof, and methods for using such polypeptides and compositions for various therapeutic uses.

Abstract: Substrates for thrombin and assays for determining the level of bioactive thrombin in a sample are disclosed, wherein the substrate has the general formula: A-X—Z-A? wherein one of either A or A? comprises a luminescent chelate and the other one of A or A? comprises a first partner of a binding pair, X forms a tri- or tetra-peptide, and Z comprises a linker.

Abstract: The invention discloses a composition of nanoparticles composed of positively charged chitosan, one negatively charged substrate, and optionally a zero-charge compound or at least one tumor necrosis factor inhibitor for oral delivery. The chitosan-based nanoparticles are characterized with a positive surface charge and enhanced permeability for oral drug delivery.

Abstract: The present invention relates to labelled cMet binding peptides suitable for optical imaging in vivo. The peptides are labelled with an optical reporter group suitable for imaging in the red to near-infrared region. Also disclosed are pharmaceutical compositions and kits, as well as in vivo imaging methods, especially of use in the detection, staging, diagnosis, monitoring of disease progression or monitoring of treatment of colorectal cancer (CRC).

Abstract: Site-specific modifications of proteins at their N-termini are provided. In particular, a chemical modification of proteins at their N-termini via a transamination reaction to form homogeneous adducts such as, the corresponding oxime derivatives is provided. Methods of making and using the adducts in radio-labelling, molecular imaging applications, and treatment of disorders such as cancer, Crohn's disease, arthritis, atherothrombosis and plaque rupture are also provided.

Abstract: The present invention relates to novel histidine derivates that can be used for the labeling of biomolecules with radioactive metal tricarbonyls. The new derivatives have a histidine that is derivatized at the N? and at least protected at the N? and optionally at the N?; or derivatized at the N? and at least protected at the N? and optionally at the N?; or derivatized at the N? and N? and at least protected at the N? and optionally at the N?; or derivatized at the N?; or derivatized at the N?; or derivatized at the N? and N?; or at least protected at the N? and optionally at the N?.

Abstract: The present invention relates to [18F]-fluciclatide radiopharmaceutical compositions, which are stabilised with a radioprotectant. Also described are methods for the preparation of the radiopharmaceutical compositions, including automated synthesizer methods and cassettes for use in such methods. The invention also includes methods of imaging the mammalian body using the radiopharmaceutical compositions.

Abstract: Cancers are extremely heterogeneous in terms of the frequency and types of mutations present in different malignant tumors. Thus, it is likely that uniform clinical treatment is not optimal for all patients, and that the development of individualized therapeutic regimens may be beneficial. Multiple, unique small peptides bind to cell lines derived from different colon adenocarcinomas. Within two hours of contact, the colorectal cancer cells are able to transfer a 32P radioisotope from the small peptides to cellular proteins; the transfer occurs at a substantially higher rate than in the colorectal cancer cells than in cell lines derived from other cancers or from normal tissues.

Abstract: The present invention relates to peptides which home to cells, e.g. heart cells, with high selectivity and which can be useful in the form of compositions. Such compositions can be used, e.g., for selectively targeting a systemically administered therapeutic agent or imaging agent to a cell or tissue in a subject. The present invention further relates to methods of using the compositions for imaging, e.g. PET imaging, and targeting cells, e.g. for delivering a therapeutic agent to one or more target cells in a subject.

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: The present invention relates to methods for the treatment of headache and headache disorders. The methods comprise administration of an oxytocin peptide for the treatment of primary and secondary headaches or trigeminal neuralgia.

Abstract: An embodiment of the invention comprises a ligand of Formula I wherein R1 and R2 are independently an alkyl or cycloalkyl; R3 is and alkyl; X is CO or SO2; Y is (CH2)n, C6H4, (OCH2CH2)n(NHCH2CH2)n and (OCH2CH2CH2)n, or a combination thereof; Z is linker group capable of conjugating to a vector; and n is an integer between 0 and 10. Also included are an imaging agent comprising a compound of Formula I complexed to 99mTc and their method of use to image a subject having a target site using single photon emission computed tomography (SPECT).

Abstract: The present invention relates to radiopharmaceutical imaging in vivo of apoptosis. The invention provides imaging agents which target apoptotic cells via selective binding to the aminophospholipid phosphatidylethanolamine (PE), which is exposed on the surface of apoptotic cells. The radiopharmaceuticals comprise radiometal complexes of chelator conjugates of PE-binding peptides. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

Abstract: A peptide sequence of the form: X(Lys,Arg)XXXXX(Arg,Lys)X, wherein Lys and Arg are replaceable and X is preferably one or more of the following amino acids: hydrophobic amino acid residues (eg Pro, Leu, Met, Ile), basic amino acid residues or threonine; and wherein the sequence is capable of engaging A? and ameliorating its SOD activity and/or metal ion binding.

Abstract: The invention relates to thrombin inhibitors derived from the salivary glands of haematophagous arthropods and in particular to bivalent and trivalent thrombin inhibitors that act by interacting with thrombin at two or three different sites.

Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

Abstract: The present invention provides ?4?1 integrin ligands that display high binding affinity, specificity, and stability. The ligands comprise a peptide having n independently selected amino acids, wherein at least one amino acid is an unnatural amino acid or a D-amino acid, and wherein n is an integer of from 3 to 20. Methods are provided for administering the ligands for treating cancer, inflammatory diseases, and autoimmune diseases. Also provided are methods for administering the ligands for imaging a tumor, organ, or tissue in a subject.

Abstract: The present invention discloses alpha particle emitting, radioactive constructs capable of killing large tumors (>1 mm in diameter), or other cells involved in human or animal diseases such as virus infected cells, autoimmune cells, or other pathological cells, including normal cells, that are targets for destruction, to achieve a therapeutic result. The alpha-emitting constructs have high specific activity.

Abstract: The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).