64 results about "Peptide receptor" patented technology

To provide a radionuclide complex solution of high concentration and high chemical stability which can be used as a medicine for diagnosis and / or treatment.SOLUTION: Provided is a pharmaceutical composition comprising: (a) a complex formed by: (ai) a radionuclide; and (aii) a gastrin releasing peptide receptor peptide antagonist binding moiety linked to a chelating agent; (b) at least two stabilizers against radiolysis; and (c) optionally a surfactant.SELECTED DRAWING: None

The present invention relates to a process for preparing the compound of Formula I in the form of a base or a salt thereof, and its use as an intermediate for the preparation of calcitonin gene- related peptide (CGRP) receptor antagonist active pharmaceutical ingredients, in particular zavegepant, where the compound of Formula I is the following: (I)

The application belongs to the field of marine biotechnology, and specifically discloses a preparation method of a long oyster insulin-like peptide receptor (ILPR) polyclonal antibody and application thereof. The method is characterized by the following steps: specific antigen epitopes of the long oyster ILPR protein are screened through bioinformatics analysis, a pET32a-ILPR recombinant plasmid is constructed and induced to express in Escherichia coli; the purified recombinant protein is used as an immunogen to immunize New Zealand white rabbits, and rabbit antisera are collected after four times of booster immunization; specific polyclonal antibodies are purified by using antigen affinity chromatography technology, and can specifically recognize the ILPR protein in long oyster tissues. The antibody prepared by the application has high specificity and sensitivity, and provides an important biological tool for studying the insulin signal transduction pathway, growth regulation and energy metabolism mechanism of long oysters.

Methods and compositions for controlling, treating, preventing, or ameliorating arthropod infection are provided. Compositions can comprise one or more active agents of small molecules antagonists of arthropod kinin receptor. Methods of preventing disease development and infestation by arthropods are disclosed as well as methods of making, using, and producing such compositions.

The present invention relates to a WKYMVm peptide analogue and uses thereof, and the WKYMVm peptide analogues have increased stability due to an increased in vivo degradation half-life, enhance activity of neutrophils as a formylpeptide receptor agonist, and regulate the activity of immune cells mediating pathology of multiple sclerosis so that they can be effectively used for enhancing immunity or preventing or treating multiple sclerosis.

In certain embodiments, the present invention provides compounds of formula I: TLX and methods of using the same, T is an SST2R targeting ligand; L is a linker, X is a chelating agent.

The present invention discloses a method for alleviating gastrointestinal side effects resulting from the administration of pharmaceutical agents selected from the group including non-steroidal anti-inflammatory drugs (NSAIDs), glucagon-like peptide-1 (GLP-1) receptor agonists, gastric inhibitory polypeptide (GIP) receptor agonists, dual GIP / GLP-1 receptor co-agonists, and combinations thereof, by administering a composition containing colostrum product, bovine colostrum, or combinations thereof to a subject. The present invention discloses compositions and kits related to alleviating gastrointestinal side effects resulting from the administration of pharmaceutical agents selected from a group including non-steroidal anti-inflammatory drugs (NSAIDs), glucagon-like peptide-1 (GLP -1) receptor agonists, gastric inhibitory polypeptide (GIP) receptor agonists, dual GIP / GLP -1 receptor co-agonists, and combinations thereof. This method provides a novel approach to mitigate gastrointestinal side effects associated with the use of these pharmaceutical agents, enhancing patient comfort and compliance during treatment.

The disclosure relates to compounds of formula I, which are formyl peptide 2 (FPR2) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

A pharmaceutical formulation useful for treating metabolic disorders or conditions is provided, comprising a plurality of particles suspended in a carrier system, the particles (a) having an average diameter based on weight, number, or volume of about 10 nm to about 700 μm, and (b) a solid core comprising at least one glucagon-like peptide-1 receptor agonist or a pharmaceutically acceptable salt thereof, at least partially coated with a coating of an inorganic material comprising a mixture of (i) zinc oxide and (ii) one or more other metal and / or metalloid oxides, wherein the atomic ratio ((i):(ii)) is at least about 1:10 and not more than about 10:1. The mixed oxide-coated particles are preferably synthesized by a vapor-phase coating technique, such as atomic layer deposition. The formulation may provide delayed or sustained release of the glucagon-like peptide-1 receptor agonist for treating metabolic disorders or conditions, such as type 2 diabetes and / or obesity, without a burst effect. The glucagon-like peptide-1 receptor agonist is preferably liraglutide.

There is provided peptidic compounds of Formula I, A or B(Rradn6-[linker]-RL-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-ψ-Xaa9-NH2). Xaa1 is D-Phe, Cpa, D-Cpa, Nal, D-Nal, 2-Nal, or D-2-Nal; Xaa2 is Asn, Gln, Hse, Cit or His. Xaa3 is Trp, Bta, Trp(Me), Trp(7-Me), Trp(6-Me), Trp(5-Me), Trp(4-Me), Trp(2-Me), Trp(7-F), Trp(6-F), Trp(5-F), Trp(4-F), Trp(5-OH), or αMe-Trp. Xaa4 is Ala or Ser. Xaa5 is Val, Cpg, or Tle. Xaa6 is Gly, NMe-Gly, or D-Ala. Xaa7 is His or NMe-His. Xaa8 is Leu or Phe. Xaa9-NH2 is a C-terminally amidated amino acid residue selected from Pro, 4-oxa-L-Pro, Me2Thz, or Thz. ψ represents a peptide bond or reduced peptide bond joining Xaa8 to Xaa9. Rradn6 is 1-5 radiolabeling groups. There is also provided the use of such compounds as imaging agents or therapeutic agents.

The invention discloses a selective nematicidal compound I based on a bursaphelenchus xylophilus neuropeptide receptor and application of the selective nematicidal compound I. The invention relates to a small molecular lead compound for killing bursaphelenchus xylophilus and application of the small molecular lead compound, the chemical formula of the small molecular lead compound is C25H27 Cl N2 O3 S, and the median lethal concentration of the small molecular lead compound for killing the bursaphelenchus xylophilus is 9.30 mg / L. The micromolecular lead compound can effectively inhibit the feeding capacity and population number of pine wood nematodes, and shows good nematode killing potential. The small molecular lead compound has a good application prospect in the aspect of preventing and treating pine wood nematode diseases.

This invention relates to a polypeptide compound and its applications, and more specifically, to a dual or triple agonist polypeptide drug that activates glucagon-like peptide-1 receptor and optionally glucose-dependent insulinotropic peptide receptor and glucagon receptor, and its application in the treatment of metabolic syndrome.

The invention relates to the field of medical biology, in particular to a tri-agonist polypeptide compound which has triple agonist activity on a glucagon-like peptide-1 receptor (GLP-1 R), a glucose-dependent insulinotropic polypeptide receptor (GIP R) and a glucagon receptor (GCG R) and is shown in a general formula (I) or salt or solvate of the tri-agonist polypeptide compound, and relates to application of the tri-agonist polypeptide compound in treatment of metabolic syndromes.

Convergent pathways for the preparation of a peptide by solid phase peptide synthesis or liquid phase peptide synthesis, as well as peptide fragments suitable for use in such pathways, are provided. The convergent pathways may be utilized for the synthesis of agonists of the glucagon-like peptide 1 receptor (GLP-1R) such as the peptide component of maridebart cafraglutide.

The invention provides a GLP-1R / GIPR / GCGR triple receptor agonist and an application of the GLP-1R / GIPR / GCGR triple receptor Specifically, the invention provides a polypeptide with GLP-1 (glucagon-like peptide-1) R / GIPR / GCGR triple receptor agonist activity or a pharmaceutically acceptable salt thereof, and the polypeptide or the pharmaceutically acceptable salt thereof has obvious triple agonist activity of a glucagon-like peptide-1 (GLP-1) receptor, a gastric inhibitory polypeptide (GIP) receptor and a glucagon (GCG) receptor. The compound can be used for preparing pharmaceutical compositions for preventing or treating metabolic diseases such as type I diabetes mellitus, type II diabetes mellitus, gestational diabetes mellitus, obesity, non-alcoholic fatty liver disease (NAFLD), obesity, hyperlipidemia and the like.

The present invention relates to a use of a triazole compound as a ghrelin receptor agonist and, more specifically, to a composition for preventing or treating diseases mediated by the ghrelin receptor, the composition being of a triazole compound which strongly binds to the ghrelin receptor with very high specificity. The compound provided by the present invention exhibits a strong binding force to the ghrelin receptor with very high specificity, and thus may be very usefully employed for preventing or developing a therapeutic agent for diseases mediated by the ghrelin receptor.

The present invention provides novel piperidinyl-containing pain-sensitive peptide receptor ligand compounds and pharmaceutical compositions that are useful in the treatment of neurological diseases and disorders wherein such ligands address the negative effects of such disorders. Such neurological diseases and conditions include acute and chronic pain, substance abuse / dependence, alcohol addiction, anxiety, depression, sleep disorders, gastrointestinal disorders, kidney disease, cardiovascular disease, and Parkinson's disease.

Long-acting glucagon like peptide 1 receptor agonists (GLP-1r agonists) reduce and inhibit pathological processes that give rise to long-term neurological impairment. A biotinylated and / or lipidated GLP-1r agonist analogs with enhanced enzymatic stability needed for gastrointestinal absorption, improved bioavailability and pharmacokinetics are described. In preferred embodiments, the GLP-1r agonist analogs have the amino acid sequence of any one of SEQ ID NOs: 9-35. The compositions are typically administered via oral or parenteral routes. The compositions are particularly suited for treating, alleviating, and / or preventing one or more neurological diseases or disorders such as Alzheimer's disease (AD) and Parkinson's disease (PD). Methods of treating a human subject having AD or PD or at risk of AD or PD are provided.

The present invention relates to gastrin-releasing peptide receptor (GRPR)-targeted compounds and their use for imaging and treatment of diseases or conditions characterized by expression of the gastrin-releasing peptide receptor.

The invention discloses umami peptide RCNG from litopenaeus vannamei. The amino acid sequence of the umami peptide RCNG is as shown in SEQ ID NO. 2. The umami peptide RCNG from the litopenaeus vannamei is applied to serving as a flavor enhancer or preparing the flavor enhancer. According to the present invention, the new umami peptide is explored from the litopenaeus vannamei meat protein sequence through the virtual screening, the molecular simulation and other technologies, such that the marine umami peptide library is enriched, the key amino acid combined with the umami peptide receptor and the action mechanism are researched, and the reference is provided for the research of the umami presentation mechanism of the peptides with different structures.

Methods for identifying chronic hydrocephalus include assaying for an amount in a biological sample of one or more biomarkers selected from pyruvate dehydrogenase lipoamide kinase isozyme 4 (PDK4), phosphofructokinase-muscle (PFKM), low density lipoprotein receptor adaptor protein 1 (LDLRAP1), glucagon-like peptide-1 receptor (GLP-1R), hemoglobin subunit alpha 1 (HBA1), hemoglobin subunit alpha 2 (HBA2), heme oxygenase 1 (HMOX1), and combinations thereof. Methods for screening for a compound useful for treating chronic hydrocephalus are also provided and include contacting a cell with an effective amount of a test compound, and then detecting an expression or activity level of one or more of the biomarkers.

Provided herein are peptides and peptide conjugates having activity as triple agonists of the glucose-dependent insulinotropic polypeptide (GIP) receptor, the glucagon-like peptide 1 (GLP-1) receptor, and the glucagon (GCG) receptor. The peptide conjugates provided herein are cross-linked via a half-life extending staple. The peptides and peptide conjugates may be used for blood glucose management and treating conditions such as diabetes mellitus, obesity, dyslipidemia, metabolic syndrome, and metabolic dysfunction-associated steatohepatitis (MASH).

The present disclosure relates to a compound having a novel structure that binds to the glucagon-like peptide-1 receptor (GLP-1R) and acts as an agonist or a modulator thereof, a preparation method thereof, and uses thereof. The compound of the present disclosure can bind to the GLP-1 receptor and exhibit agonist activity thereof, and thus may be usefully employed for the treatment or prevention of GLP-1 receptor activity-associated diseases.

The present disclosure relates to a compound having a novel structure that binds to the glucagon-like peptide-1 receptor (GLP-1R) and acts as an agonist or a modulator thereof, a preparation method thereof, and uses thereof. The compound of the present disclosure can bind to the GLP-1 receptor and exhibit agonist activity thereof, and thus may be usefully employed for the treatment or prevention of GLP-1 receptor activity-associated diseases.

The invention discloses a selective nematicidal compound based on a bursaphelenchus xylophilus neuropeptide receptor and application of the selective nematicidal compound, the chemical formula of small molecule lead compounds is C30H32 N2 O6, and the median lethal concentration of the small molecule lead compounds for killing bursaphelenchus xylophilus is 8.76 mg / L. The micromolecular lead compound can effectively inhibit the feeding capacity and population number of pine wood nematodes, and shows good nematode killing potential. The small molecular lead compound has a good application prospect in the aspect of preventing and treating pine wood nematode diseases.

This disclosure relates to compounds of formula I that are formylpeptide 2 (FPR2) receptor agonists and / or formylpeptide 1 (FPR1) receptor agonists. This disclosure also provides compositions and methods using the compounds for, for example, the treatment of atherosclerosis, heart failure, and related diseases. JPEG2026516737000190.jpg5755I

A method for treating muscular dystrophy of a subject comprising administrating a N-formyl peptide receptor (FPR) agonist to the subject and compositions therefore. An FPR agonist may be used to target the FPR2-mediated pro-resolving pathway, thus facilitating the clearance of inflammation, reducing inflammatory response, enhancing repair processes, enhancing regenerative capacity in muscles, and otherwise improving prognosis of muscular dystrophy.

The present invention relates to gastrin-releasing peptide receptor (GRPR)-targeted compounds and their use for imaging and treatment of diseases or conditions characterized by expression of the gastrin-releasing peptide receptor.

The present invention is related to a compound of formula (I):whereinR1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl;AA-COOH is an amino acid selected from the group consisting of 2-amino-2-adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9-carboxylic acid;R2 is selected from the group consisting of (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkylmethyl, halogen, nitro and trifluoromethyl;ALK is (C2-C5)alkylidene;R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and (C1-C4)alkyl under the proviso that one of R3, R4 and R5 is of the following formula (II)whereinALK′ is (C2-C5)alkylidene;R6 is selected from the group consisting of hydrogen and (C1-C4)alkyl; andR7 is selected from the group consisting of H and an Effector moiety;or a pharmacologically acceptable salt, solvate or hydrate thereof.

Provided herein are compositions, and methods of using the composition as a novel alternative combination therapy, for the preventing, treating, ameliorating, reducing the risks of metabolic syndrome or metabolic diseases or disorders. The composition comprises Oleoylethanolamide, Berberine, and Gymnema sylvestre and targets three different hormone receptors, (1) Glucagon-like peptide 1 (GLP-1) receptors, (2) Glucagon (GCG) receptors, and (3) Glucose-dependent Insulinotropic Polypeptide (GIP) receptors.