30results about "Tachykinins" patented technology

The present invention encompasses novel synthetic peptide analogs that are antagonists to Substance P, substance P like peptides and related peptides and are useful for the treatment of cancer. The invention particularly relates to the design and synthesis of the novel substance P antagonist analogs incorporating alpha,alpha-dialkylated amino acids in a site specific manner. The invention encompasses methods for the generation of these peptides, compositions containing these peptides and pharmacological applications of these peptides specifically in the treatment and prevention of cancer.

The invention relates to the use of peptides individually or in combination, for treating and/or preventing angiogenesis. It also relates to the use of peptide analogs or a combination of peptides referred to as MuJ-7 as anticancer drugs in restricting the tumor growth and spread by inhibiting tumor angiogenesis. MuJ-7, in addition inhibits metastasis through its antiangiogenic activity in all cancers. The invention also relates to a pharmaceutical composition containing either individual peptides or in combination, and methods of treatment of human beings and animals for curing and/or preventing angiogenesis.

The invention pertains to the discovery of novel disulfide linked cell toxins which can ablate NK-1 receptor expressing cells. These toxins are used as pharmaceutical compositions for the ablation of NK1 receptor expressing cells and comprise a substance P (SP)-Pseudomonas exotoxin disulfide linked conjugate. The invention also includes methods of making and using these toxins and pharmaceutical compositions.

A chimeric toxin is disclosed comprising a peptide ligand specifically targeting neurons involved in pain processing; and a clostridial neurotoxin light chain, wherein the ligand is linked to the light chain. The methods of preparing such chimeric toxin and the method of using the chimeric toxin to regulate pain transmission are also disclosed.

Multivalent vaccine comprising peptides from vasoactive intestinal peptide, bombesin, Substance P and epidermal growth factor are described. A method of constructing a multivalent gene for use in various expressions vectors and the protein recombinantly expressed in the prokaryotic expression systems are also described.

This invention provides a conjugate comprising Substance P, or an analog thereof, and a protein, such as Saporin, that inhibits protein synthesis.

This invention provides a method of reducing the perception of pain by a subject comprising administering to the subject an effective amount of the pharmaceutical composition of the conjugate comprising Substance P, or an analog thereof, and a protein such as Saporin that inhibits protein synthesis, so as to reduce the perception of pain by the subject.

This invention provides a method of selectively destroying NK-1R-expressing neuronal cells in a subject comprising administering to the subject an effective amount of the conjugate comprising Substance P, or an analog thereof, and a protein such as Saporin that inhibits protein synthesis, so as to selectively destroy NK-1R-expressing neuronal cells.

Lastly, this invention provides a method for treating a NK-1R-associated disorder in a subject, which comprises administering to the subject an amount of the pharmaceutical composition comprising substance P, or an analog thereof, and a protein such as Saporin that inhibits protein synthesis, in an effective amount to treat the disorder associated with the NK-1R.

The present invention relates to Notch-binding agents and Notch antagonists and methods of using the agents and/or antagonists for treating diseases such as cancer. The present invention provides antibodies that specifically bind to a non-ligand binding region of the extracellular domain of one or more human Notch receptor, such as Notch2 and/or Notch3, and inhibit tumor growth. The present invention further provides methods of treating cancer, the methods comprising administering a therapeutically effective amount of an antibody that specifically binds to a non-ligand binding region of the extracellular domain of a human Notch receptor protein and inhibits tumor growth.

The compounds of the invention are generally described by the formula:

B₁Z*₂B₃Z*₄X*₅Q₆F₇X₈X₉X₁₀X₁₁   (1),

B₁X₂X₃X₄X₅Q₆F₇X₈X₉X₁₀X₁₁   (2), or

B₁Z₂B₃X₄Z₅Q₆F₇Z₈X₉X₁₀X₁₁   (3)

and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic of polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large of hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum b and tetanus toxins.

The invention provides a P substance peptide probe capable of specific recognition of a neurokinin-1 receptor protein. the P substance peptide probe is a polypeptide dimer or a polypeptide polymer, the monomer is formed by a P substance amino acid sequence MLGFFQQPKPR, a bifunctional chelating group, a fluorescence group and a terpyridyl group connected through lysine. The novel peptide probe is used for the preparation of a polypeptide dimer and polypeptide polymer with function of diagnosing multi tumors. The polypeptide dimer and polypeptide polymer marks metal Gd<3+> to a polypeptide molecule by the bifunctional chelating group; the marked P substance peptide probe and the NK-1 receptor protein specifically bind and concentrate to the tumor site in vivo; and magnetic imaging and optical imaging technology are utilized for detection of the neurokinin-1 receptor protein to improve the sensitivity of the detection.

The present invention relates to a method for correlating single nucleotide polymorphisms in the preprotachykinin (NKNA) gene with the efficacy and compatibility of a pharmaceutically active compound administered to a human being. The invention further relates to a method for determining the efficacy and compatibility of a pharmaceutically active compound administered to a human being which method comprises determining at least one single nucleotide polymorphism in the NKNA gene. Said methods are based on determining specific single nucleotide polymorphisms in the NKNA gene and determining the efficacy and compatibility of a pharmaceutically active compound in the human by reference to polymorphism in NKNA. The invention further relates to isolated nucleic acids comprising within their sequence the polymorphisms as defined herein, to nucleic acid primers and oligonucleotide probes capable of hybridizing to such nucleic acids and to a diagnostic kit comprising one or more of such primers and probes for detecting a polymorphism in the NKNA gene, to a pharmaceutical pack comprising NK-1 receptor antagonists and instructions for administration of the drug to human beings tested for the polymorphisms as well as to a computer readable medium with the stored sequence information for the polymorphisms in the NKNA gene.

The present invention provides a simple method for the stabilization of a peptide in a biological sample and a reagent for the stabilization, a simple method for the preservation of a biological sample comprising a peptide and a reagent for the preservation, and a method for the accurate measurement of a peptide in a biological sample and a reagent for the measurement. Addition of a saccharide to a biological sample enables the stabilization of a peptide in the biological sample, the preservation of the biological sample comprising a peptide in a stable condition and the accurate measurement of a peptide in the biological sample. As the present invention can stabilize a peptide in a biological sample collected in the clinical examination, the peptide as a marker in the biological sample can be measured accurately in the clinical examination.

The present disclosure relates to agonists of Tacr2, e.g., peptide agonists of Tacr2, and methods of using the same for the treatment of insulin resistance, obesity, and/or diabetes. The present disclosure also relates to the use of said Tacr2 agonists for increasing the energy consumption in an individual.

Peptide-based neurokinin antagonists of fish reproduction are disclosed. Compositions comprising antagonists of fish neurokinin and methods of inhibiting or delaying puberty, fish maturation or reproduction processes using these compounds are also provided.

Provided herein are conjugates including a targeting vehicle coupled to an agent. The targeting vehicle includes a tachykinin receptor ligand and a reactive moiety. Conjugates including a tachykinin receptor ligand attached to an antibody or fragment thereof that is specific for an intracellular target are also provided. Also provided are methods of delivering agents to cells expressing tachykinin receptors, methods of delivering antibodies or fragments thereof to an intracellular extra-endosomal target, and methods of arresting cell growth or introducing cell death of a cancer cell.

Provided are previously uncharacterised enhancer elements from the preprotachykinin-A (PPTA) which shows transcriptional enhancement activity in Substance P (SP) expressing cells. These are termed ECR1 and ECR2. The invention provides nucleic acids comprising these sequences and variants or fragments thereof, plus methods and materials based thereon, such as transformed host cells, transgenic animals, and screening and expression systems.

Described herein are methods for treating disorders that relate to neurons that express the neurokinin-1 receptor (NK-1R) in a subject which comprises administering to the subject an effective amount of the pharmaceutical composition of the non-cleavable conjugate comprising a molecule that is recognized and internalized by the NK-1R, and a molecule that is taken inside the cell to kill or temporarily alter the cell.