43results about "Vasoactive intestinal peptide" patented technology

Methods and compositions are provided for extending the half-life of a therapeutic agent. A modified therapeutic agent (mTA) comprises a therapeutic agent, a staple, and a half-life extending molecule. The mTAs disclosed herein may be used to treat a disease or a condition in a subject in need thereof.

To provide a composition for preventing or treating neurotrophic keratitis.SOLUTION: It is found that a PACAP peptide exerts an inhibitory effect of cornea disorder in a neurotrophic keratitis model, and model axon extension is promoted in a cultured nerve cell. Furthermore, provided are a composition for preventing or treating neurotrophic keratitis which contains a PACAP peptide or a stabilized PACAP peptide in which stability significantly enhances by substituting a carboxyl group of aspartic acid at the 3- and / or 8-position in a sequence of PACAP with tetrazole, and an axon extension promoter.SELECTED DRAWING: Figure 4

To provide a pharmaceutical composition for prevention or treatment of metabolic syndrome.SOLUTION: The present invention provides a composition comprising: a glucagon derivative; and a GLP-1 receptor and GIP receptor dual agonist, and use thereof.SELECTED DRAWING: None

The present invention is entitled Triple Agonists at the Glucagon / GLP-1 / GIP Receptor. The present invention relates to triple agonists that are active at all of the glucagon, GLP-1 and GIP receptors and uses thereof.

Provided is a fusion protein. The fusion protein simultaneously blocks a calcitonin gene-related peptide (CGRP) pathway and a pituitary adenylate cyclase-activating polypeptide (PACAP) pathway, wherein the fusion protein comprises at least one single-domain antibody, at least one Fc fragment, and at least one extracellular domain fragment of pituitary adenylate cyclase 1 (PAC1 ECD). The fusion protein can simultaneously block the CGRP and PACAP pathways, thereby improving the response rate of a drug for treatment of migraine.

Disclosed herein is a novel pharmaceutical composition for treating pain, wherein the pharmaceutical composition targets a transient receptor potential vanilloid 1 (TRPV1) receptor and acts as an antagonist.

The present disclosure provides a method for delivering a neuroprotective polypeptide to at least a portion of a central nervous system (CNS) of a subject. The method includes administering to the systemic blood circulation of the subject a therapeutically effective amount of a neuroprotective polypeptide by a controlled-release formulation or a device providing a sustained release of the neuroprotective polypeptide including at least one neuroprotective polypeptide selected from the group consisting of GLP-1, exendin-4, or a therapeutically effective GLP-1 or exendin-4 analogue; the neuroprotective polypeptide binds to and activates a receptor that binds at least one of GLP-1, exendin-4, or a combination thereof; and the controlled-release neuroprotective formulation or the sustained release of the neuroprotective polypeptide enhances the delivery of the neuroprotective polypeptide across a blood-brain barrier (BBB) of the subject to at least a portion of the CNS relative to a rapid release formulation of the neuroprotective polypeptide. Also disclosed is a method of treating a subject with a CNS-related disease or reducing at least one symptom of a CNS-related disease in a subject in need thereof.

Disclosed are VIP-R antagonists for uses in managing the treatment or prevention of cancer and viral infections. In certain embodiments, this disclosure relates to chimeric variants of VIP-R antagonists, as peptides disclosed herein, and pharmaceutical composition comprising the same. In certain embodiments, this disclosure contemplates methods of treating subjects with cancer or infection with VIP-R antagonists or stimulating immune cells to target cancer by mixing immune cells in vitro with peptides disclosed herein and further administering an effective amount of stimulated immune cells to a subject in need of cancer treatment.

The invention provides a fusion protein for treating metabolic diseases, and a preparation method and use thereof. The fusion protein has a general formula of R1-L-R2 or R2-L-R1, wherein R1 is FGF21 protein, an FGF21 protein analog, or a similar peptide with the biological function of FGF21 protein; R2 is GIP, mutant GIP or a similar peptide with the biological function of GIP; and L is a linker peptide. The fusion protein of the present invention is used as a therapeutic agent or a pharmaceutical composition in the treatment of diseases associated with hyperglycemia and hyperlipidemia, including diabetes, obesity, steatohepatitis or cardiovascular diseases,

The present invention relates to glucose-dependent insulinotropic peptide (GIP) receptor (GIPR) antagonist GIP peptides in combination with glucagon-like peptide-1 (GLP-1) receptor agonists, such as GLP-1 peptides, for use in the treatment of obesity and obesity-related disorders, and GIPR antagonist GIP peptides for treating a subset of obesity-related disorders.

To provide a composition for preventing or treating neurotrophic keratitis.SOLUTION: It is found that a PACAP peptide exerts an inhibitory effect of cornea disorder in a neurotrophic keratitis model, and model axon extension is promoted in a cultured nerve cell. Furthermore, provided are a composition for preventing or treating neurotrophic keratitis which contains a PACAP peptide or a stabilized PACAP peptide in which stability significantly enhances by substituting a carboxyl group of aspartic acid at the 3- and / or 8-position in a sequence of PACAP with tetrazole, and an axon extension promoter.SELECTED DRAWING: Figure 4

Provided are a recombinant microorganism expressing a vasoactive intestinal peptide (VIP) gene, and a composition including the microorganism for preventing or treating a disease causing damage to the gastrointestinal tract.

The present invention relates to a novel brain disease therapeutic agent and a use thereof. The peptide or the pharmaceutical composition according to the present invention can improve the delivery level to a target site (particularly an inflamed region of the brain) due to having a high blood-brain barrier penetration level, can have an improved half-life in the blood flow, and can exhibit anti-inflammatory activity and treat or prevent brain diseases by reducing the level of inflammation.

The invention provides a novel oral blood sugar reducing polypeptide. The polypeptide is an improved derivative based on Exendin-4. According to the present invention, the Exendin-4 is analyzed so as to obtain the core sequence of 28 amino acids, wherein the core sequence is HGEGTFTSDLSKQMEEEAVRLFIEWLKN; in order to improve the stability and bioavailability, four key sites are subjected to amino acid substitution (K12H, R20H, F22A and K27H), AF and FK are respectively added at the N end and the C end, and finally a complete sequence with 32 amino acids is formed. The structural modifications significantly improve the oral absorption efficiency of the polypeptide. Compared with an Exendin-4 prototype, the antihyperglycemic polypeptide Ex32 disclosed by the invention has the advantages that the enzymolysis resistance is obviously improved, and the obtained Ex32-containing polypeptide has good physical and chemical stability and bioavailability and can be directly used for preparing various dosage forms, for example, the Ex32-containing polypeptide can be used for treating type II diabetes mellitus.

A fusion protein is provided that blocks both a calcitonin gene related peptide (CGRP) pathway and a pituitary adenylate cyclase activated peptide (PACAP) pathway, where the fusion protein comprises at least one single domain antibody, at least one Fc fragment, and at least one extracellular domain fragment of pituitary adenylate cyclase 1 (PAC1 ECD). The fusion protein can block CGRP and PACAP pathways at the same time, and the response rate of drugs for treating migraine is improved.

Provided are a fusion protein of an exenatide precursor and a use thereof. The fusion protein comprises an exenatide precursor and a tag protein fused at an N terminus of the exenatide precursor. The exenatide precursor has an amino acid sequence as shown in SEQ ID NO: 1. The tag protein is selected from any one of Fh8 tag protein, Ffu209 tag protein, CBM tag protein, Sumo tag protein, or Trx tag protein. The exenatide precursor is fused with the tag protein, and the exenatide precursor carrying the tag protein exhibits a high expression level, enabling the preparation of large quantities of high-purity exenatide precursors, thereby facilitating industrial-scale production and use of exenatide.

Disclosed are VIP-R antagonists for uses in managing the treatment or prevention of cancer and viral infections. In certain embodiments, this disclosure relates to chimeric variants of VIP-R antagonists, as peptides disclosed herein, and pharmaceutical composition comprising the same. In certain embodiments, this disclosure contemplates methods of treating subjects with cancer or infection with VIP-R antagonists or stimulating immune cells to target cancer by mixing immune cells in vitro with peptides disclosed herein and further administering an effective amount of stimulated immune cells to a subject in need of cancer treatment.

The present invention relates to the technical field of polypeptide drug preparation methods. Provided is a solid-phase preparation method for high-yield and high-purity tirzepatide. An amino resin is used as a starting resin; amino acids and small-fragment peptides are sequentially coupled according to the amino acid sequence of tirzepatide using a solid-phase synthesis method to synthesize a tirzepatide resin; and the tirzepatide resin is cleaved and purified to obtain a pure tirzepatide product. The small-fragment peptides include a 1-4 tetrapeptide fragment Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH, a 5-6 dipeptide fragment Fmoc-Thr(tBu)-Phe-OH, a 7-8 dipeptide fragment Fmoc-Thr(tBu)-Ser(tBu)-OH, a 10-11 dipeptide fragment Fmoc-Tyr(tBu)-Ser(tBu)-OH, a 12-13 dipeptide fragment Fmoc-Ile-Aib-OH, a 17-18 dipeptide fragment Fmoc-Ile-Ala-OH, a 20-side-chain peptide Fmoc-Lys(AEEA-AEEA-γ-Glu(α-OtBu)-Eicosanedioic acid(mon-tBu))-OH, a 28-30 tripeptide fragment Fmoc-Ala-Gly-Gly-OH, a 32-34 tripeptide fragment Fmoc-Ser(tBu)-Ser(tBu)-Gly-OH, and a 36-38 tripeptide fragment Fmoc-Pro-Pro-Pro-OH. A coupling agent for coupling the amino acid and the small-fragment peptide is selected from Oxyma and DIC, TPTU and TMP, or COMU and DIEA.

The invention title of the present invention is a long-acting conjugate of a glucagon / GLP-1 / GIP receptor triple agonist. The present invention relates to a long-acting conjugate of a triple agonist that is active against all of the glucagon, GLP-1, and GIP receptors and its uses.

The present disclosure relates to a VIP antagonist for use in the management of the treatment or prevention of cancer and viral infections. In certain embodiments, the present disclosure relates to chimeric variants of VIP antagonists, such as the peptides disclosed herein, and pharmaceutical compositions comprising the same. In certain embodiments, the present disclosure contemplates methods of stimulating immune cells to target cancer by mixing immune cells with a peptide disclosed herein in vitro and further administering an effective amount of the stimulated immune cells to a subject in need of cancer treatment.

The invention discloses a method for purifying retaglutide, which adopts a gradient elution precise regulation and control method, is combined with segmented gradient, reduces the duration of high-concentration acetonitrile, shortens the overall time of preparation, adds the time of elution and column flushing, ensures that the preparation completion time is less than 60 minutes, reduces the use of a large amount of acetonitrile, saves the dissolution cost, and improves the purification efficiency of the retaglutide. The purification efficiency is improved, the time of the purification process is shortened, and the purposes of energy conservation and environmental protection benefits are achieved in large-scale production requirements.

An object of the present invention is to provide a composition for preventing or treating neurotrophic keratitis. The present inventors found that PACAP peptide exhibits an inhibitory effect on corneal injury in a neurotrophic keratitis model and promotes neurite outgrowth in a cultured nerve cell model. Furthermore, there are provided a composition for preventing or treating neurotrophic keratitis containing a PACAP peptide or a stabilized PACAP peptide, in which the carboxyl group of aspartic acid at positions 3 and / or 8 in the sequence of PACAP is replaced with tetrazole, and the stability is significantly enhanced, and a neurite outgrowth promoter.

There is provided compound for use in the treatment of vaginal laxity or a related disorder, which compound consists essentially of between 3 and 21 N-terminal amino acids of the peptide sequence: His-Ser-Asp-X4-X5-Phe-Thr-Asp-X9-Tyr-X11-Arg-X13-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys (SEQ ID No: 1) wherein: each of X4, X5, X9, X11 and / or X13 independently represent an amino acid selected from the group Ala, Val, Ile, Gly, Asn, Ser, Thr, Tyr and Leu; which peptide sequence is optionally coupled to the group Y or, in cases where the C-terminal amino acid is not Lys, to the group -Lys-Y; and Y represents one or more latanoprost molecules and / or one or more lipid, which lipid is selected from the group consisting of vitamin A, vitamin E, cholesterol and a fatty acid comprising one or more carboxylic acid groups, 1 to 50 carbons, and / or one or more cyclic rings, is linear or branched, saturated or unsaturated with between 1 and 10 carbon-carbon double bonds and / or substituted by between 1 to 10 -OH groups, or a derivative of any of these lipids; or a regioisomer, a stereoisomer, or a pharmaceutically-or cosmetically-acceptable salt thereof.

The invention discloses an Ex4-Fc-III-4C conjugate with a broad-spectrum antibody binding function as well as synthesis and application of the Ex4-Fc-III-4C conjugate, and belongs to the technical field of medical chemistry. Specifically, a series of bifunctional molecule Ex4-Fc-III-4C conjugates are synthesized by means of two chemical selectivity methods, i.e., click chemistry and SML technology, and the bifunctional molecule Ex4-Fc-III-4C conjugates are found to use Fc domain high-affinity cyclic peptide as an adhesive of an endogenous antibody to interact with the endogenous antibody on the basis of retaining the original GLP-1R activation ability, so that the GLP-1R-GLP-1R-GLP-1R-GLP-1R-GLP-1R-GLP-1R-GLP-1R-GLP-1R-GLP-1R-GLP-1R-GLP-1R- A polypeptide-hapten-antibody compound is formed in vivo, so that the effect of prolonging the half-life period of a drug by a similar polypeptide-Fc fusion strategy is generated, the immunogenicity problem existing in the Fc fusion strategy is avoided, and the polypeptide-hapten-antibody compound becomes a more effective strategy for improving the pharmacokinetic properties of protein / polypeptide drugs.

A recombinant protein comprising multiple multi-peptide sets includes first through fifth sequencing primers and first through fourth multi-peptide regions. The first multi-peptide region is between the first and the second sequencing primers. The second multi-peptide region is between the second and the third sequencing primers. The third multi-peptide region is between the third and the fourth sequencing primers. The fourth multi-peptide region is between the fourth and the fifth sequencing primers. In each of the multi-peptide regions, multiple functional peptides can be inserted, and manufacturing thereof can be done through expression of the recombinant protein, thereby significantly enhancing the concentrations of the functional peptides. With the combination of peptide having different functions, the recombinant protein product can provide more complete and more comprehensive functionality. This application also discloses a pharmaceutical composition comprising the recombinant protein and a method for preparing the recombinant protein.

Disclosed are VIP-R antagonists for uses in managing the treatment or prevention of cancer and viral infections. In certain embodiments, this disclosure relates to chimeric variants of VIP-R antagonists, as peptides disclosed herein, and pharmaceutical composition comprising the same. In certain embodiments, this disclosure contemplates methods of treating subjects with cancer or infection with VIP-R antagonists or stimulating immune cells to target cancer by mixing immune cells in vitro with peptides disclosed herein and further administering an effective amount of stimulated immune cells to a subject in need of cancer treatment.

A Fusion Peptide for Activation of the APJ and / or GLP-1 Receptors This invention relates to a fusion peptide comprising a GLP-1 receptor agonist (GLP-1 RA) and an APJ receptor agonist; wherein the GLP-1 RA is covalently linked to the APJ receptor agonist by a link; and wherein the fusion peptide retains at least some activity of at least one of the GLP-1 RA and the APJ receptor agonist.

The present invention relates to a novel therapeutic agent for brain diseases and its use. The peptide or pharmaceutical composition of the present invention has a high blood-brain barrier penetration level, which can enhance delivery and reach to the site of action (particularly, inflammatory sites in the brain), and can increase the blood half-life. Furthermore, by improving inflammation levels, it is possible to reduce inflammation and treat or prevent brain diseases.

Glycopeptide analogs of secretin family peptides, including PACAP and VIP, are described herein. These glycopeptides analogs can have neuroprotective properties and enhanced ability to cross the blood brain barrier (BBB) and / or enhanced stability. These glycosylated peptides can be used as drugs for treatment of CNS disorders, such as Parkinson's disease.