Abstract: Compositions that contain bioactive agent-loaded nanoparticles with heart targeting capabilities and methods of using the same for the treatment of disease are disclosed.

Abstract: Described herein are compositions and methods for diagnosing and/or monitoring pathogenic disease states using positron emission tomography, wherein the pathogenic cells uniquely express, preferentially express, or overexpress vitamin receptors. Also described herein are 18F conjugates of vitamins and vitamin receptor-binding analogs and derivatives.

Abstract: The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide chelated with at least one active agent. Examples of active agents include a paramagnetic element, a radioactive element and a fibrinolytic agent, among others. Paramagnetic agents have a distribution that is relatively easily shown through Magnetic Resonance Imaging (MRI). Radioactive agents have applications in imaging and delivery of radiations, depending on the specific element included in the active agent. Delivery of fibrinolytic agents mainly to a specific organ, such us for example to the lungs, allows to substantially improve the specificity and efficacy of thrombolytic therapy by allowing local delivery of the fibrinolytic agent, thereby reducing the risks of major bleeding in the therapy of the organ. If the organ is the lungs, a non-limiting example of pathology treatable with the fibrinolytic is pulmonary embolus.

Abstract: A vehicle composition in the form of a vesicular composition or a particular composition and, optionally, an active agent associated with the vesicle forming components or particles, and folate receptor alpha is used as a delivery system for the transport of components and/or active agents into the cerebrospinal fluid (CSF) and/or brain and/or central nervous system and/or spinal cord. The composition is used for treating of CSF or brain pertaining diseases, disorders or conditions, such as preventing or treating neurological or neurodegenerative diseases, disorders or conditions.

Abstract: The present application discloses compositions and methods of synthesis and use involving click chemistry reactions for in vivo or in vitro formation of therapeutic and/or diagnostic complexes. Preferably, the diagnostic complex is of use for 18F imaging, while the therapeutic complex is of use for targeted delivery of chemotherapeutic drugs or toxins. More preferably, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment, using a click chemistry reaction involving cyclooctyne, nitrone or azide reactive moieties. In most preferred embodiments, the click chemistry reaction occurs in vivo. In vivo click chemistry is not limited to 18F labeling but can be used for delivering a variety of therapeutic and/or diagnostic agents.

Abstract: The invention relates to micelles that are elaborated with functionality useful for imaging and/or selectively targeting tissue, e.g., in the delivery of hydrophobic agents.

Abstract: NK-2 synthetic peptide derived from cationic core region of porcine NK-lysin has an antimicrobial and antitumor polypeptide that is considered to play a pivotal role in innate defense immunity. To evaluate the antimicrobial properties of synthetic chicken NK-lysin peptides, we investigated cytolytic activity against apicomplexan parasites like Eimeria sporozoites, Neospora tachyzoites and Cryptosporidum sporozoites. The chicken NK-2 (cNK-2) lytic peptide which corresponds to amino acid residues of porcine NK-2 peptide significantly disrupted Eimeria and Cryptosporidum sporozoites and Neospora tachyzoites. In contrast, no bactericidal activity was observed on E. coli BMH71-18. The cNK-2 lytic peptide is novel antimicrobial agent which can be used to intervene and treat economically costly infections in the animal industry.

Abstract: The present disclosure describes techniques used for colorectal cancer detection. Position and distribution of colorectal cancer tumor are detected through nuclear imaging. Alternatively, stage of colorectal cancer is identified by shading value in tumor. Thus, the present disclosure provides a safe and noninvasive clinical method for diagnosing and tracing level and distribution of colorectal cancer before and after treatment.

Abstract: The present invention provides a composition (a blood glucose increase inhibitor) that has an effect of lowering blood glucose level in a hyperglycemic patient and that is therefore used to reduce blood glucose level in the patient. The present invention further provides a composition that is used to prevent or treat diseases caused by hyperglycemia, in particular, diabetes and diabetic complications (a composition for preventing or treating diseases caused by hyperglycemia, an antidiabetic), based on the above-mentioned effect. A feature of the present invention is using a peptide consisting of the amino acid sequence of Leu-Ser-Glu-Leu as an active ingredient.

Abstract: This invention relates to molecular imaging agents comprising an S78C mutant synaptotagmin I C2A domain. These agents may be useful in detecting or assessing cell death in vitro and in vivo, for example in tumors following cancer treatment.

Abstract: The present invention provides soluble single wall nanotube (SWNT) constructs functionalized with a plurality of a targeting moiety and a plurality of one or more payload molecules attached thereto. The targeting moiety and the payload molecules may be attached to the soluble SWNT via a DNA or other oligomer platform attached to the SWNT. These soluble SWNT constructs may comprise a radionuclide or contrast agent and as such are effective as diagnostic and therapeutic agents. Methods provided herein are to diagnosing or locating a cancer, treating a cancer, eliciting an immune response against a cancer or delivering an anticancer drug in situ via an enzymatic nanofactory using the soluble SWNT constructs.

Abstract: The present invention provides a self assembly molecule having an affinity for one or more target molecules, for use in formation of a heptameric complex, comprising: a) a monomer comprising a multimerization domain of Archaeal Sm1 (AF-Sm1) protein or SM-like ribonucleoprotein from other organisms, able to interact with other molecules of the same monomer comprising a multimerization domain of AF-Sm1 protein or SM-like ribonucleoprotein to self-assemble into a heptamer; and b) a target binding domain or peptide attached directly or via a linker to the monomer of (a). Also provided are heptamers comprising these self assembly molecules and methods for their use in therapy, imaging and diagnostics.

Abstract: The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods of making such radiodiagnostic and radiotherapeutic agents and the compounds used in such methods. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

Abstract: The present invention relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of inter alia compromised lactation conditions as well as to a method for treatment of said conditions, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.

Abstract: Disclosed are immunogenic Nogo receptor-1 polypeptides, Nogo receptor-1 antibodies, antigen-binding fragments thereof, soluble Nogo receptors and fusion proteins thereof and nucleic acids encoding the same. Also disclosed are Nogo receptor antagonist polynucleotides. Also disclosed are compositions comprising, and methods for making and using, such Nogo receptor antibodies, antigen-binding fragments thereof, soluble Nogo receptors and fusion proteins thereof, nucleic acids encoding the same and antagonist polynucleotides.

Abstract: An embodiment of the invention comprises method of imaging a target site comprising administrating ligand of Formula I complexed to 99mTc 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.

Abstract: The invention provides conjugates for imaging plaques, such as cardiovascular plaques, as well as associated pharmaceutical compositions. Other aspects of the invention include methods for administering and imaging such conjugates and compositions, and using the imaging to characterise plaques. The conjugates of the invention distinguish between tropoelastin and elastin in plaques. The presence of tropoelastin can act as an indication that a plaque is liable to rupture or erode. Such information allows assessment of disease progression and response to treatment.

Abstract: The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.

Abstract: The invention provides compositions and methods for therapeutic and diagnostic applications.

Abstract: The invention discloses a pharmaceutical composition of pH-sensitive liposome nanoparticles for lodging in a target tissue cell in situ of an animal subject, the nanoparticles comprising a proton-releasing photosensitive compound that releases protons upon photolysis, wherein the compound is in vesicles of the liposomes. A light or UV light is provided to induce the photosensitive compound to release the protons, thus the released protons causing the pH-sensitive liposome to decompose.

Abstract: The present invention relates to bifunctional compounds, the bifunctional compounds for use in molecular imaging and therapy, methods of molecular imaging using the bifunctional compounds and kits including the bifunctional compounds for use molecular imaging. The bifunctional compounds have a tripodal hydroxypyridinone chelating portion and may be conjugated to a targeting group so that the compounds target specific cells or tissues in a subject.

Abstract: The present disclosure provides compositions and methods based on peptide-detectable agent conjugates that are useful for imaging beta cell mass.

Abstract: The present invention is related to peptides, which are suitable for use as cell-penetrating peptides (CPPs), variants thereof and/or complexes, fusion molecules and/or conjugates comprising same, use thereof for manufacture of compositions for diagnosing, treating and/or preventing of medical conditions.

Abstract: The present invention relates to the field of tissue engineering and more specifically to amphiphilic peptides and peptide matrices thereof useful in vitro and in situ biomineralization and inducing bone repair. The present invention provides peptides, which are useful in hydrogels and other pharmaceutical compositions, and methods and kits of use for bone repair and promotion of biomineralization. Certain hydrogels according to the invention comprise cells within or adhered to the peptide matrix.

Abstract: The invention provides a family of agents that target the prostate specific antigen, which can be used as imaging agents or therapeutic agents. The agents can be used to image prostate cancer as well as other physiological processes in a subject.

Abstract: Some embodiments relate to analogs of peptides corresponding to class I MHC-restricted T cell epitopes and methods for their generation. These analogs can contain amino acid substitutions at residues that directly interact with MHC molecules, and can confer improved, modified or useful immunologic properties. Additionally, classes of analogs, in which the various substitutions comprise the non-standard residues norleucine and/or norvaline, are disclosed.

Abstract: The present invention provides improved vaccines comprising an isolated viral antigenic peptide and a synthetic peptide derived from a T cell epitope of HSP60. The invention includes mixtures where the peptide serves as an adjuvant as well as conjugates where the peptide is covalently linked to the viral antigen. The known synthetic peptide carrier, p458, provides significantly improved immunogenicity for synthetic viral epitopes and analogs. Ec27 is a novel peptide derived from HSP60 which increases the immunogenicity substantially of the viral antigen both as a mixture or a covalent conjugate. Some of the isolated viral epitopes are novel and are claimed for diagnostic as well as therapeutic or prophylactic uses.

Abstract: The present invention relates to methods of growing and maintaining pluripotent cells on an insoluble substrate that presents a peptide that binds to glycosaminoglycans, such as heparin. Specifically, methods of growing and maintaining pluripotent cells on substrates having a chemically defined surface presenting at least one peptide having basic amino acid residues separated by one or two hydrophobic amino acid residues.

Abstract: Disclosed are compositions, kits, and methods for inducing an immune response against disease. The dosage of antigen contained or utilized in the presently disclosed compositions, kits, and methods is substantially lower than dosages conventionally used in the field. The compositions, kits, and methods may be utilized to induce a cell-mediated response, such as a T-helper cell response, and/or a humoral response against a pathogen or a disease. In some embodiments, the compositions, kits, and methods may be utilized to induce preferentially a Th1 response versus other types of immune responses such as a Th2 response.

Abstract: Described herein are compositions and methods of use of anti-pancreatic cancer antibodies or fragments thereof, such as murine, chimeric, humanized or human PAM4 antibodies. The subject antibodies show a number of novel and useful therapeutic characteristics, such as binding with high specificity to pancreatic and other cancers, but not to normal or benign pancreatic tissues and binding to a high percentage of early stage pancreatic cancers. In preferred embodiments, the antibodies bind to pancreatic cancer mucins. The antibodies and fragments are of use for the detection, diagnosis and/or treatment of cancer, such as pancreatic cancer. The antibodies, such as PAM4 antibodies, bind to a PAM4 antigen that shows unique cell and tissue distributions compared with other known antibodies such as CA19.9, DUPAN2, SPAN1, Nd2, B72.3, and Lea and Le(y) antibodies that bind to the Lewis antigens.

Abstract: To provide a molecular probe for imaging of pancreatic islets. A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe includes any one of the following polypeptides: polypeptides represented by the following formulae (1), (5), and (9); and polypeptides having homology with the foregoing polypeptides: Z-DLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2? (1) Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2? (5) B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2? (9) where X in the formulae (1) and (5) and B- in the formula (9) indicate that an amino group is labeled with a group represented by the formula (I) below having an aromatic ring, wherein A represents either an aromatic hydrocarbon group or an aromatic heterocyclic group, R1 represents a substituent that contains radioactive iodine, R2 represents either a hydrogen atom or a substituent different from that represented by R1, and R3 represents any one of a bond, a methylene group, and an oxymethylene group.

Abstract: Cyclized peptide compounds containing the NGR motif of formula (I) or a pharmaceutically-acceptable salt thereof are disclosed. Compositions comprising the cyclized peptide compounds and methods of their use are also disclosed.

Abstract: The present invention provides a variety of isolated peptides and peptidomimetics, which can be useful, for example, in constructing the conjugates of the invention or, where the peptide itself has biological activity, in unconjugated form as a therapeutic for treating any of a varirty of cardiovascular diseases as described below. Thus, the present invention provides an isolated peptide or peptidomimetic which has a length of less than 60 residues and includes the amino acid sequence CRPPR (SEQ ID NO: 1) or a peptidomimetic thereof. The invention further provides an isolated peptide or peptidomimetic which has a length of less than 60 residues and includes the amino acid sequence CARPAR (SEQ ID NO: 5) or a peptidomimetic thereof, or amino acid sequence CPKRPR (SEQ ID NO: 6) or a peptidomimtic thereof.

Abstract: The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel aza-bicycloalkane based cyclic peptides, acting as a targeting moiety towards integrin receptors.

Abstract: The invention is directed to novel Lutetium-177-labeled bombesin analogs for treatment of tumor by radiotherapy.

Abstract: The invention provides compositions and methods for therapeutic and diagnostic applications.

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: 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: Provided herein are compounds or conjugates useful for diagnostic imaging and/or therapeutic purposes. Each compound or conjugate comprises a ligand for the chemokine receptor CXCR4 and a detectable label. The ligand has a binding affinity for the CXCR4 receptor, measured as IC50 in the presence of 125I-CPCR4, of 250 nM or lower, and the ligand comprises a cyclic oligopeptide moiety having the motif B-Arg or B-(Me)Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine, provided that the motif is B-Arg when B is a N?-methyl derivative of a basic amino acid.

Abstract: Engineered peptides that bind with high affinity (low equilibrium dissociation constant (Kd)) to the cell surface receptors of fibronectin (?5?1) or vitronectin (?v?3 and ?v?5 integrins) are disclosed as useful as imaging tissue. These peptides are based on a molecular scaffold into which a subsequence containing the RGD integrin-binding motif has been inserted. The subsequence (RGD mimic) comprises about 9-13 amino acids, and the RGD contained within the subsequence can be flanked by a variety of amino acids, the sequence of which was determined by sequential rounds of selection (in vitro evolution). The molecular scaffold is preferably based on a knottin, e.g., EETI (Trypsin inhibitor 2 (Trypsin inhibitor II) (EETI-II) [Ecballium elaterium (Jumping cucumber)], AgRP (Agouti-related protein), and Agatoxin IVB, which peptides have a rigidly defined three-dimensional conformation. It is demonstrated that EETI tolerates mutations in other loops and that the present peptides may be used as imaging agents.

Abstract: Ghrelin analogues having high affinity for a target receptor in diseased cells are provided, as well as methods of diagnosis and treatment utilizing such analogues.

Abstract: Embodiments of the present disclosure provide for RGD mimetic ?-AApeptide compounds, ?-AApeptide compounds capable of binding an RGD binding site on integrin ?v?3, linear ?-AApeptide compounds, cyclic ?-AApeptide compounds and multimeric RGD mimetic ?-AApeptide compounds, methods of making each, and methods of using each, and the like. In embodiments, the RGD mimetic ?-AApeptide compounds can be used in imaging, diagnostics, and treatment of angiogenesis related conditions.

Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.

Abstract: Compositions and methods for targeted delivery to and detection of sites of neovascular growth, including tumor vasculature, are provided. Compositions include polypeptides conjugated to or complexed with a bioactive compound, wherein the polypeptide is capable of binding to an OEC or a circulating progenitor thereof. Methods for identifying additional polypeptides with the same binding characteristics are further provided. Methods for targeted delivery of a bioactive compound to a site of neovascular growth are provided in which polypeptides capable of binding OECs or progenitors thereof are conjugated to or complexed with the bioactive compound and administered to a subject in need thereof. Methods for detecting neovascular growth are also provided, wherein the polypeptides conjugated to or complexed with a detectable label are administered to a subject and the label is detected.

Abstract: The present invention relates to technetium imaging agents comprising radiolabeled c-Met binding peptides suitable for SPECT or PET imaging in vivo. The c-Met binding peptides are labelled via chelator conjugates. Also disclosed are pharmaceutical compositions, methods of preparation of the agents and compositions, plus methods of in vivo imaging using the compositions, especially for use in the diagnosis of cancer.

Abstract: This invention relates to the use of ADNF polypeptides in the treatment of anxiety and/or depression. The present invention also relates to drug discovery assays using the ADNF polypeptide mechanism of action and target interaction, as well as the manufacture of medicaments, methods of application and formulation therefor. Embodiments of the invention provide methods for preventing and/or treating anxiety and depression disorders in a subject by administering a NAP, an 8-amino-acid peptide derived from Activity Dependent Neurotrophic Factor (ADNF III), in an amount sufficient to improve postnatal performance. The ADNF polypeptides include ADNF I and ADNF III (also referred to as ADNP) polypeptides, analogs, subsequences, and D-amino acid versions (either wholly D-amino acid peptides or mixed D- and L-amino acid peptides), and combinations thereof which contain their respective active core sites and provide neuroprotective and anti-anxiety functions.

Abstract: The present invention provides a substantially non-lytic, non-cytotoxic anchor peptide that is capable of stably inserting into lipid membranes. In particular, the invention provides nanoparticles comprising stably inserted anchor peptides, which may be conjugated to a variety of different cargo complexes.

Abstract: Disclosed are compositions and methods useful for targeting tissue undergoing angiogenesis or to cells or tissue expressing ?v integrins. The compositions and methods are based on peptide sequences that selectively bind to and home to tissue undergoing angiogenesis or to cells or tissue expressing ?v integrins in animals. The disclosed targeting is useful for delivering therapeutic and detectable agents to tissue experiencing angiogenesis or to cells or tissue expressing ?v integrins.

Abstract: Novel radiotracer(s) for Positron Emission Tomography (PET) imaging are described. Novel radiotracer(s) for Positron Emission Tomography (PET) imaging of neuorendocrine tumors are described. Specifically the present invention describes novel [18F]Fluoroethyltriazol-[Tyr3]Octreotate analogs; in particular those that target somatostatin receptors found on the cell surface of gastroenteropancreatic neuorendocrine tumors. The present invention also describes intermediate(s), precursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

Abstract: The invention provides an agent comprising an amino acid sequence for use in a method of diagnosis of a synucleinopathic disease.