40results about "Neurotensin" patented technology

The present invention is directed to conjugates that include a polypeptide capable of crossing the blood-brain barrier or entering one or more cell types attached to a transport vector, i.e., a composition capable of transporting an agent (e.g., a therapeutic agent). In certain cases, the polypeptides are directly conjugated to a lipid or polymeric vector to allow targeted application of a therapeutic agent to treat, for example, a cancer, a neurodegenerative disease, or a lysosomal storage disorder.

The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

This invention relates to methods of synthesis of amino acid analogs contained within peptide sequences that is adapted for preparation of peptides containing analogs of basic amino acids lysine and arginine.

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer and increasing cellular internalization of said peptide compounds. The peptide compounds are selected from the following group consisting of; GVRAKAGVRNMFKSESY as set forth in SEQ ID NO: 9; GVRAKAGVRN(Nle)FKSESY as set forth in SEQ ID NO: 10; and YKSLRRKAPRWDAPLRDPALRQLL as set forth in SEQ ID NO: 11; and wherein at least one protecting group and / or at least one labelling agent is connected to said peptide compound.

The present invention describes a system of gene carrier nanoparticles capable of specifically internalize into cancer cells, eg, cancer cells involved in breast cancer, in vitro and in vivo. The system described allows the introduction of therapeutic genes specifically into target cells through NSTR1 receptor-mediated endocytosis of said system, making it possible to provide treatment for this type of conditions, for example by systemic, intravenous, or in situ administration.

Peptide analogs of neurotensin are disclosed which are resistant to enzymatic degradation and which retain high binding affinity for neurotensin receptors. Pharmaceutical compositions of these compounds are useful for diagnostic and therapeutic purposes.

The present invention relates to a multimeric molecule having the general formula (A) or (B): and its use in the diagnosis and / or therapy of tumors

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treatment of cancer or aggressive cancer. For example, the compounds can comprise compounds of formula X1 X2X3X4X5GVX6AKAGVX7NX8FKSESY (I) (SEQ ID NO: 1) (X9)nGVX10AKAGVX11NX12FKSESY (II) (SEQ ID NO: 2) YKX13LRRX14APRWDX15PLRDPALRX16X17L (III) (SEQ ID NO: 3) YKX18LRR(X19)nPLRDPALRX20X21L (IV) (SEQ ID NO: 4) IKLSGGVQAKAGVINMDKSESM (V) (SEQ ID NO: 5) IKLSGGVQAKAGVINMFKSESY (VI) (SEQ ID NO: 6) IKLSGGVQAKAGVINMFKSESYK (VII) (SEQ ID NO: 7) GVQAKAGVINMFKSESY (VIII) (SEQ ID NO: 8) GVRAKAGVRNMFKSESY (IX) (SEQ ID NO: 9) GVRAKAGVRN(Nle)FKSESY (X) (SEQ ID NO: 10) YKSLRRKAPRWDAPLRDPALRQLL (XI) (SEQ ID NO: 11) YKSLRRKAPRWDAYLRDPALRQLL (XII) (SEQ ID NO: 12) YKSLRRKAPRWDAYLRDPALRPLL (XIII) (SEQ ID NO: 13) wherein X1 to X21 and n can have various different values and wherein at least one protecting group and / or at least one labelling agent is optionally connected to said peptide compound at an N- and / or C-terminal end, for use in inhibiting vasculogenic mimicry and / or for treating a cancer.

Analogs for CLR / RAMP receptor ligands are provided that have agonist, superagonist, antagonist, super-antagonist, or multiple receptor modulating activity. The analogs can be selective for one or more CLR / RAMP receptors, or can be pan-specific for multiple G protein-coupled receptors.

The invention discloses a neuropeptide and a synthesis method and application thereof, wherein the neuropeptide has an amino acid sequence shown by SEQIDNO:1. According to the amino acid sequence represented by the SEQIDNO:1, valine is used as a first amino acid,-NH2 of the valine is exposed, then the-NH2 of the valine is condensed with-COOH of second amino acid-arginine to form an amide bond, other amino acids are sequentially connected, and finally tyrosine is to obtain the neuropeptide. Compared with the prior art, the neuropeptide has the following advantages: 1. the neuropeptide product can effectively improve defects of experimental animal social memory, and no adverse reaction is observed; 2. functional areas of the neuropeptide is a sequence on an endogenous protein, and cell rejection reaction may not be caused; 3. a signaling pathway activated by the neuropeptide is a known nervous system specific signaling pathway; 4. the product can effectively change the activity and state of neurons; and 5. the essence of the product is an amino acid sequence, is easy to degrade, and may not cause bodily organ loads.

A thio-selective radioactive labeling agent has the following general formula:*R-L-VS,wherein said *R is a radioisotope, L is a linking group, and VS is a vinylsulfone functional group.

The present invention relates to activated neurotensin, pharmaceutical compositions comprising the same, and the uses thereof. The compounds and compositions of the invention may be used, e.g., to reduce body temperature, attenuate or halt seizures, reduce excitotoxicity, promote neuroprotection, reduce neuroinflammation and aberrant axonal sprouting or reduce pain.

Microarrays employing a fluorescent ligand including a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about −3 to about +5, or more preferably, about −2 to about +2 or most preferably for small compound ligands about −1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions). In some embodiments, the ligand includes fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.