78 results about "Bifunctional chelator" patented technology

The invention discloses a heavy metal Cu<2+> complete antigen and a preparation method thereof. The preparation method comprises the following steps: Cu<2+> is reacted with a bifunctional chelating agent to form a hapten; and a Cu<2+>-chelating agent hapten is reacted with a carrier protein to form a Cu<2+>-chelating agent-carrier protein complete antigen. The antigen has better immunogenicity; and an immune mice with the antigen can be used for preparing a Cu<2+> specific monoclonal antibody and further preparing a rapid Cu<2+> detection ELISA (enzyme-linked immuno sorbent assay) kit of various heavy metals and colloidal gold immunochromatography assay test paper.

This invention relates to macrocyclic chelants comprised of one or two heteroatom-containing bridges, compositions containing them and their use in medicine, particularly in diagnostic imaging and radiotherapy. This invention relates especially to the use of metal chelates of the macrocyclic chelants as metallopharmaceuticals in Magnetic Resonance Imaging (MRI) and radiopharmaceuticals. This invention also relates to macrocyclic chelants as bifunctional chelating agents (BFC's) for the labeling of biologically active targeting molecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands, with metal ions and radioisotopes.

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.

The invention provides a novel radionuclide labelled somatostatin analogue molecular probe and its application and belongs to the field of radiopharmaceuticals labelling and nuclear medicine technologies. A bifunctional chelator couples cyclic polypeptide Pasireotide, and then radionuclide is used for labelling so as to obtain a radionuclide labelled neuroendocrine neoplasm specific somatostatin analogue radioactive molecular probe. The molecular probe can be combined with a tumor expression somatostatin receptor (SSTR), and SSTR positive tumor tissue can be accurately positioned by means of nuclear medicine. Thus, the purpose of disease target molecular imaging diagnosis and treatment is achieved. The synthesized molecular probe has higher affinity and functional activity for SSTR and is expected to become a somatostatin analogue developer and tumor therapeutic agent with a good prospect.

Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula

The invention relates to a RGD polypeptide radiopharmaceutical used for integrin alphavbeta3 positive tumor. The RGD polypeptide radiopharmaceutical comprises RGD polypeptide, difunctional Chelator and radioactive Nuclide. The RGD polypeptide is RGD cyclic peptide dimer which is RGD cyclic peptide dimer E(L-c(RGDxK))2 which is synthesized by connecting the coupling agent L with RGD polypeptide monomer c(RGDfK) and dimerizing two RGD polypeptide monomer L-c(RGDfK) which are connected with the coupling agent L. The radioactive nuclide marks the RGD cyclic peptide dimer by one difunctional Chelator, and pharmacokinetic modifying molecule PKM is connected between the RGD cyclic peptide dimer and the difunctional chelator. The RGD polypeptide radiopharmaceutical is Nuclide-Chelator-PKM-E(L-c(RGDxK))2, and the RGD polypeptide radiopharmaceutical is colorless transparent liquid injection.

The invention relates to three RGD (Arginine-Glycine-Aspartic acid) polypeptide radioactive medicaments for positive tumor diagnosis of an intergrinalphavbeta3 receptor and preparation methods thereof. The three RGD polypeptide radioactive medicaments are structurally RGD annular dipolymers, and radioactive nuclein 99mTc labeling is performed through a dual-functional chelating agent. The medicaments are mainly characterized in that: a [K(NIC)] structure which is connected with RGD is used for replacing the conventional 99mTc-labeled synergistic ligand, i.e., trisodium salt of tri(m-sulfonphenyl) phosphine (TPPTS), so that the molecular weight of a medicament structure is reduced, and the metabolism velocity of a radioactive medicament in a non-target organ is increased. The three radioactive medicaments include 99mTc-HYNIC-K(NIC)-RGD2, 99mTc-HYNIC-K(NIC)-3G-RGD2 and 99mTc-HYNIC-K(NIC)-3P-RGD2, and are colorless and transparent liquid injections.

The invention provides a polypeptide compound with a HER2 targeting function. The polypeptide compound with the HER2 targeting function is formed by connecting a HER2 affinity with a bifunctional chelating agent through a polypeptide sequence; the polypeptide sequence is Met-Val-Lys; the general structural formula of the polypeptide compound is shown in formula (I) as shown in specification, wherein R is a HER2 affinity molecule and X is a bifunctional chelator group. The invention also provides a radiolabelled complex targeting HER2 by taking the polypeptide compound as a ligand. The radiolabeled complex provided by the invention can be used as a radioactive diagnostic probe for evaluating the HER2 receptor of breast cancer, and the probe can reduce the concentration of the kidney under the condition of keeping the uptake of the tumor unchanged, so that the target-to-non-target ratio of the tumor is improved, and the radiation dose to the kidney is reduced. The invention also provides a preparation method of the polypeptide compound and the radiolabelled complex, and application of the polypeptide compound and the radiolabelled complex in preparation of a HER2 positive breast cancer radioactive diagnosis and treatment probe for humans or animals.

There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the --PR.sub.2 containing biomolecules by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a --PR.sub.2 containing biomolecule.

The invention discloses the radiopharmaceutical targeting galectin-1 and a preparation method thereof. The radiopharmaceutical is the conjugate of radionuclide, a difunctional chelating agent and PEG4-TDGd. The PEG4-TDGd is marked by the radionuclide through the difunctional chelating agent. According to the radiopharmaceutical targeting galectin-1, in vivo, because of specific recognition of TDGdto galectin-1 and modification of PEG4 according to pharmacokinetics, radionuclide is delivered to the surfaces of tumor cells with galectin-1 highly expressed or the hypoxia parts of a tumor with galectin-1 highly expressed, nuclear medicine positron emission computed tomography on the specificity of the tumor and the hypoxia areas of the tumor can be implemented, and monitoring on the therapeutic effect by adopting interventional treatment means such as radiotherapy on the tumor can be implemented.

The invention relates to a Cu2<+> specific monoclonal antibody and a preparation method thereof. The preparation method comprises the following steps of: reacting Cu2<+> with a difunctional chelating agent to form a half hapten; reacting Cu2<+>-chelating agent with carrier protein to form a complete antigen; immuning a BALB (Binaural Alternate Loudness Balance)/c mouse by using the complete antigen; and fusing a splenocyte of the mouse with an SP2/0 cell to prepare a hybridoma cell and obtaining a Cu2<+>-resisting monoclonal antibody. The monoclonal antibody has the specificity on the Cu2<+>, high titer and strong specificity. The invention also provides a preparation method of the Cu2<+>-resisting monoclonal antibody. The antibody and a detection technology are used for detecting residual Cu2<+> in agricultural and animal products and have the advantages of high detection speed, high sensitivity, strong selectivity and low detection cost.

The invention provides a polypeptide with tumor vessel targeting, a molecular probe and a preparation method and application of the polypeptide and the molecular probe, and belongs to the technical field of diagnostic imaging agents. The polypeptide has an amino acid sequence as shown in a sequence table Seq ID No. 1. The single-photon or positive-electron molecular probe has a structure as shown in X-N-G, wherein X is a single-photon developing nuclide or a positive-electron developing nuclide; N is a dual-functional chelating agent; and G is the polypeptide. The fluorescent molecular probe has a structure as shown in X-G, wherein X is fluorescent nuclide; and G is the polypeptide. By the modified polypeptide, the abdomen background can be reduced obviously, and the picture contrast is improved. The obtained molecular probe is simple to prepare, low in price and high in target-to-nontarget ratio.

The invention discloses a tumor PD-L1 targeting PET imaging agent as well as a labeled precursor, a preparation method and application thereof, and belongs to the technical field of radiopharmaceutical chemistry. The structure of a labeled precursor of the tumor PD-L1 targeting PET developer is shown as a formula I, and the structure of the tumor PD-L1 targeting PET developer is shown as a formula II. According to the invention, a bifunctional chelating agent DOTA and a cyclic peptide inhibitor SETSKSF are creatively connected together, and a labeled precursor of a PET imaging agent of a targeted tumor PD-L1 as shown in a formula I is synthesized. After the precursor compound is marked with Ga-68, a compound shown in a formula II can be obtained, and the compound has good stability, excellent pharmacokinetics, good binding specificity with tumor PD-L1 and easy synthesis.

The invention provides a cadmium ion detection kit as well as a preparation method and an application thereof. Complete antigen of a cadmium ion is a complex of the cadmium ion, a chelating agent andcarrier protein, wherein the chelating agent comprises any one of or a combination of any two of EDTA (ethylenediaminetetraacetic acid), DTPA (diethylenetriamine pentaacetic acid), a derivative of DTPA, DOTA (1,4,7,10-tetraazacyclododecane-N,N,N,N-tetraacetic acid) and DOTA-NHS (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-N-hydroxysuccinimide eater). The heavy metal cadmium ion is coupled with the carrier protein through a bifunctional chelating agent, the complete antigen of the cadmium ion is obtained, a cadmium ion monoclonal antibody with high immunogenicity and high valence for the cadmium ion is prepared, and the formed kit has high specificity and sensitivity and can be used for detecting the cadmium ion.

The invention relates to a VQ polypeptide radioactive medicine which comprises VQ polypeptide, a difunctional chelator and a radioactive nuclide, wherein the VQ polypeptide is linear heptad of which the sequence is VRPMPLQ (Val-Arg-Pro-Met-Pro-Leu-Gln, VQ), the radioactive nuclide marks the VQ linear heptad through the difunctional chelator, the VQ polypeptide radioactive medicine is Nuclide-Chelator-VQ, and the VQ polypeptide radioactive medicine is colorless and transparent liquid injection. The VQ polypeptide radioactive medicine can be used for early diagnosis of various tumors, the medicine enables the radioactive nuclide 99 mTc to be marked on the VQ polypeptide molecule through the difunctional chelator, marked medicine in body is concentrated to a tumor part through the targeting effect of the VQ polypeptide, and by using nuclear medicine single photon emission tomograph, imaging diagnosis is performed on various tumors.