58results about "Somatostatins" patented technology

Provided herein are cyclic peptides having avidity for somatostatin receptors and having increased renal clearance. In some embodiments, the cyclic peptides comprise a non-natural tryptophan-lysine dipeptide. In addition, provided herein are radiopharmaceuticals and conjugates comprising the cyclic peptides.

The present application relates to animals or cells having a myostatin gene with a 12 base pair deletion in the second exon. The application may also include compositions capable of engineering a 12 base pair deletion in the myostatin gene to construct animals or cells. The application also relates to the use of the compositions to increase muscle mass.

The present invention relates to fusion proteins that agonise a somatostatin receptor (SSTR), in particular somatostatin receptor 4 (SSTR4), and methods for producing the same. The fusion proteins of the invention comprise a scaffold and a somatostatin (SST)-derived peptide and, optionally, a partner domain.

The present application relates to an animal or cell having a myostatin gene in which 12 base pairs of the second exon are deleted. The present application may also comprise a composition capable of m

The present invention relates to compounds comprising a metal chelating agent and two fragments capable of binding to the somatostatin type 2 receptor, compositions thereof and their use in methods of treatment.

Provided herein are peptides and conjugates (e.g., radiopharmaceutical conjugates) having avidity for a somatostatin receptor and uses thereof. The conjugate can comprise a 6-mer peptide, such as a monocyclic 6-mer peptide, a metal chelator, and optionally a linker connecting the peptide to the chelator. The radiopharmaceutical conjugate can further comprise a radionuclide bound to the metal chelator. Further provided herein are methods of preparing the conjugates, and methods of treating cancer by administering the described conjugates to a subject in need thereof.

# imgabs0. The present invention discloses compounds of formula (I) and complexes thereof with radionuclides, which can recognize both the somatostatin type 2 receptor (SSTR2) and the cholecystoxin 2 receptor (CCK2R) and can be used in the diagnosis and treatment of diseases in which either or both receptors are overexpressed.

The present invention relates to novel structures, synthesis methods, and applications of human somatostatin analogs comprising either a cyclic or non-cyclic hexapeptide unit, wherein the amino acid residues at positions 2 to 5 are represented by -X1-(D / L)-Trp-X2-X3-, or a cyclic or non-cyclic octapeptide unit, wherein the amino acid residues at positions 2 to 7 are represented by -Cys-X1-(D / L)-Trp-X2-X3-Cys-. In these sequences, X1 is an α-amino acid residue containing an aromatic group on the Cα side chain, X2 is a Lys derivative, and X3 is an α-amino acid residue. The Lys derivative has the following structure: wherein n is 0 or 1; A1, A2, and A3 are independently selected from C(R)2, O, S, NR, C=O, C=S, C=NR, and C=C(R)2. The present invention challenges the conventional understanding that modification of the Lys9 residue in somatostatin significantly reduces biological activity. By altering the Lys9 residue in somatostatin analogs, the present invention provides analogs with enhanced or comparable binding affinity to SSTR2, thereby improving their therapeutic efficacy.

A linker for linking a therapeutic agent to another moiety, such as the Fc region of an antibody. A linker having two or more maleimide functional groups capable of undergoing a nucleophilic conjugate addition reaction. A method for increasing the duration of action of a therapeutic agent by conjugating it to a novel linker and the Fc region of an antibody. An antibody-drug conjugate having an increased duration of action over the drug alone.

Provided are a polypeptide-coupled drug and an anti-tumour use thereof. The polypeptide-coupled drug is a compound of formula (I) or a pharmaceutically acceptable salt thereof. In formula (I), P is a cyclic peptide containing 4-9 amino acids, L is a linking group, and D is selected from topoisomerase I inhibitors; the polypeptide-coupled drug has better tumour growth inhibitory activity. P-L-D (I)

The present application relates to an animal or cell having a myostatin gene in which 12 base pairs of the second exon are deleted. The present application may also comprise a composition capable of manipulating the deletion of 12 base pairs of a myostatin gene to construct the animal or the cell. The present application also relates to use of the composition for increasing muscle.

A somatostatin peptide analogue. The somatostatin peptide analogue has a cyclic or non-cyclic hexapeptide unit, and the residue sequence at positions 2 to 5 in the hexapeptide unit is: -X1-(D / L-)Trp-X2-X3-; or the somatostatin peptide analogue has a cyclic or non-cyclic octapeptide unit, and the residue sequence at positions 2 to 7 in the octapeptide unit is: -Cys-X1-(D / L-)Trp-X2-X3-Cys-; wherein X1 is an α-amino acid residue having an aryl group on a Cα side chain, and X3 is an α-amino acid residue, and X2 is a Lys-variant residue: formula (I). The somatostatin peptide analogue breaks the "taboo" that Lys9 residues cannot be substituted, otherwise, the biological activity will be greatly reduced. By varying the Lys9 residues in the somatostatin peptide analogue, the Lys9 residues are varied, which enables the somatostatin peptide analogue to exhibit higher (at least similar) binding affinity to SSTR2.

The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue via 18F-labeled peptide ligands disclosed herein.

To provide effective, shelf-stable and safe biological preparations such as peptides and proteins for non-invasive delivery.SOLUTION: The present invention relates to a pharmaceutical composition for transmucosal administration, comprising a peptide drug or a protein drug in combination with an excipient with a pKa value of 12 or higher.SELECTED DRAWING: None

This application relates to animals or cells possessing a myostatin gene, wherein 12 base pairs of the second exon of the myostatin gene are deleted. This application may also include compositions capable of manipulating the deletion of 12 base pairs of the myostatin gene to construct animals or cells. This application also relates to the use of this composition for increasing muscle mass.

The present disclosure relates to methods for the large scale synthesis of radionuclide complex solutions having high radioactivity for diagnostic and / or therapeutic purposes, their use in the commercial manufacture of radiopharmaceutical substances, and to the respective solutions and containers containing said solutions.

This invention provides a method for preparing sterile lanreotide raw material, comprising the following five steps: (1) preparing a lanreotide cyclic peptide solution; (2) purifying the lanreotide cyclic peptide solution once using HPLC, wherein the mobile phase A is an ammonium salt solution and the mobile phase B is an organic reagent; (3) purifying the once-purified lanreotide cyclic peptide solution a second time using HPLC, wherein the mobile phase A is a sodium salt solution and the mobile phase B is an organic reagent; (4) treating the second-purified lanreotide cyclic peptide solution with an aqueous acetic acid solution to obtain an acetate lanreotide solution; (5) filtering and drying the acetate lanreotide solution to obtain the finished product. The lanreotide raw material obtained by the preparation method of this invention has a purity greater than 99.9% and a single impurity content ≤0.10%.

A composition for modifying a myostatin gene, the composition comprising: a guide RNA; a Cas protein; wherein the target sequence is one selected from: SEQ ID NO: 38-60 and the guide sequence is one s

The present invention provides a use of a polypeptide complex on the basis of Titin-Telethonin beta-pleated sheet structure as a polypeptide or protein drug carrier, a method, and a fusion protein complex thereof. The polypeptide complex is capable of maintaining the activity of polypeptide or protein drugs and prolonging the half-life period simultaneously.

The invention relates to cortistatin analogues and their uses. The compounds of the invention are peptide ligands with potential application in the diagnosis, prevention or therapy of those pathologies where receptors capable of binding to cortistatin, specific or shared with other molecules such as somatostatin and / or ghrelin (GHSR), are expressed, being in addition more stable in serum than cortistatin.

The present invention provides prodrugs of somatostatin peptide and peptide analogs that are tissue permeable and oral bioavailable and enable activity of the somatostatin analog at the circulation or target tissue after cleavage of charge-masking lipophilic moieties. Pharmaceutical compositions comprising these prodrugs and their use in therapy and diagnosis are also provided.

The present invention relates generally to the field of bioconjugation. More particularly, the present invention relates to trivalent phosphonates and their use as reducing disulfide heavy bridging agents. Accordingly, the present invention relates to compounds selected from the group consisting of compounds of formula (la) and (lb), conjugates obtained by linking these compounds to another moiety, methods of modifying disulfide containing compounds using compounds selected from the group consisting of compounds of formula (la) and (lb), and compounds obtained by such methods.

The present invention relates to the field of polypeptide synthesis, and particularly to a method for the directional synthesis of polypeptide dimers. The method comprises the following steps: 1) preparing linear peptide resins A containing aa1(Trt) and aa2(Acm), and linear peptide resins B containing aa1(Acm) and aa2(Trt); 2) cleaving resins A and B with cleavage reagent 1 to obtain linear peptides A1 containing aa1(activated group) and aa2(Acm), and linear peptides B1 containing aa1(Acm) and aa2(activated group); cleaving resins A and B with cleavage reagent 2 to obtain linear peptides A2 containing aa1 and aa2(Acm), and linear peptides B2 containing aa1(Acm) and aa2; 3) cyclizing the linear peptides containing the activated group and the linear peptides without the activated group for the first time; 4) removing Acm and cyclizing for the second time to obtain cis or trans polypeptide dimers. By double selection of the Cys side chain protecting group of the linear peptide resin and the cleavage path, the present invention realizes the directional formation of intermolecular disulfide bonds by means of stepwise oxidation. The obtained main product is single, with high purity and high yield, which is beneficial to the large-scale industrial production of polypeptide dimers.

The present disclosure relates to low affinity chimeric antigen receptors (CARs) and CAR-T cells, which provide cytotoxicity against tumors overexpressing the proto-oncogene c-MET and alleviate on-target, off-tumor toxicities. The CAR-T cells of the present disclosure comprise low affinity anti-c-MET scFvs, which facilitate enhanced anti-tumor activity and a reduced rate of tumor relapse.

The present invention discloses compounds of Formula (I) and their complexes with radionuclides that can recognize both Somatostatin type 2 receptor (SSTR2) and cholecystokinin 2 receptor (CCK2R) and can be used in the diagnosis and treatment of diseases where either or both receptors are overexpressed.

The invention discloses a somatostatin peptide analogue, the somatostatin peptide analogue has a cyclic or non-cyclic hexapeptide unit, and the residue sequence at the position numbered 2 to 5 in the hexapeptide unit is-X1-(D / L-) Trp-X2-X3-, and the residue sequence at the position numbered 2 to 5 in the hexapeptide unit is-X1-(D / L-) Trp-X2-X3-, or, the somatostatin peptide analogue has a ring-forming or non-ring-forming octapeptide unit, and the residue sequence at the position numbered 2 to 7 in the octapeptide unit is-Cys-X1-(D / L-) Trp-X2-X3-Cys-, and the residue sequence at the position numbered 2 to 7 in the octapeptide unit is-Cys-X1-(D / L-) Trp-X2-X3-Cys-; wherein X1 is an alpha-amino acid residue with an aryl group on a C alpha side chain, X3 is an alpha-amino acid residue, and the compound is characterized in that X2 is a Lys-variation residue: # imgabs0 #. The invention breaks through the'taboo 'that the Lys9 residue cannot be replaced, otherwise, the biological activity is greatly reduced. According to the present invention, the Lys9 residue in the somatostatin peptide analogue is changed, and the Lys9 residue is subjected to change variation, such that the somatostatin peptide analogue of the present invention has high (at least similar) binding affinity with SSTR2 due to the change variation;

The present invention discloses compounds of Formula (I) and their complexes with radionuclides that can recognize both Somatostatin type 2 receptor (SSTR2) and cholecystokinin 2 receptor (CCK2R) and can be used in the diagnosis and treatment of diseases where either or both receptors are overexpressed.