79 results about "Arg-Gly-Asp" patented technology

The invention discloses a method for preparing RGD-fatty alcohol series compounds as tumor targeting carrier materials and application thereof. The method comprises the following steps: conjugating n-octa alkyl fatty alcohol, decane-based fatty alcohol, dodecyl fatty alcohol, tetradecyl fatty alcohol, hexadecane fatty alcohol, and octadecyl fatty alcohol with RGD peptide segment respectively, and performing hydrophobic modification on the compounds to synthesize a peptide conjugated compound with different amphiphilic long-chain alkyls and RGD, namely Arg-Gly-Asp-O-CnH[2n +1] (n is equal to 8, 10, 12, 14, 16, or 18), and synthesize a compound of Gly-Gly-Asp-O-C4H29 simultaneously, thus the effectiveness of the targeting materials is further confirmed.

The invention discloses a multifunctional fusion polypeptide and a preparation method and application thereof, and belongs to the field of biological pharmacy. The fusion polypeptide has the structural domains of Pro-(D-Pyr)-(D-Cys)-Bip-Arg-Gly-Glu, Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Ala-Val-Pro, Arg-Gly-Asp and Gly-Gly-Gly-Gly; the fusion polypeptide can treat human lung fibrosis, pathological changes of lung tissue, lung cancers and other tumors, and in a lung fibrosis cell model, the fusion polypeptide can significantly reduce the hydroxyproline content in model group cells and inhibit the process of lung fibrosis. It is shown through MTT tests that the fusion polypeptide can inhibit proliferation of multiple kinds of anthropogenic tumor cells; the fusion polypeptide is prepared through an artificial synthesizing method, the preparation method is simple, and a good application prospect is achieved.

The invention relates to an oxymatrine hepatic targeting nano drug delivery system and a preparation method thereof. The oxymatrine hepatic targeting nano drug delivery system is prepared by the following steps of: with polyethylene glycol-polycaprolactone block polymer as a carrier, preparing polymer nanoparticles by adopting a film dispersion method, a reverse evaporation method or an organic solvent injection method, encapsulating oxymatrine into the polymer nanoparticles, then modifying a new glycoprotein or cyclic octapeptide ligand to be taken as a ligand on the surfaces of the nanoparticles, and constructing an anti-hepatic fibrosis nano targeting drug delivery system for hepatic stellate cells (HSCs). The nano drug delivery system has the advantages that particle size is 50-260nm, encapsulation efficiency is 18-42%, drug loading capacity is 2-12% and the surface of the nano drug delivery system is rich in new glycoprotein M6PHSA (mannose-6-phosphate human serum albumin) or cyclic octapeptide RGD (arg gly asp). The oxymatrine hepatic targeting nano drug delivery system provided by the invention can increase opportunities that nanoparticles enter the liver through blood circulation, is beneficial to targeting distribution of drugs at focus parts of the liver and is beneficial to absorption of drug-carrying nanoparticles at lesion parts of the liver and ingestion of HSCs, so that hepatic fibrosis treatment is enhanced.

Disclosed are thrombin peptide derivatives comprising a polypeptide having the amino acid sequence SEQ ID NO. 2: Arg-Gly-Asp-Ala-Xaa-Glu-Gly-Asp-Ser-Gly-Gly-Pro-Phe-Val, or a C-terminal truncated fragment of the polypeptide having at least six amino acids. Xaa is alanine, glycine, serine, or an S-protected cysteine. Zero, one, two, or three amino acids in the polypeptide or polypeptide fragment differ from the corresponding position of SEQ ID NO. 2. Also disclosed are methods of treating a subject in need of treatment with a thrombin receptor agonist. The methods comprise the step of administering an effective amount of the thrombin peptide derivative described above.

The invention discloses an integrin receptor target lipidosome drug carrier and a preparation method thereof, as well as an application of the drug carrier in preparing antitumor lipidosome drug. Hexadecyl fatty chain is conjugated with RGD peptide segment and is hydrophobic-modified so as to synthesize hexadecyl and RGD peptide conjugate with amphipathy, namely, Arg-Gly-Asp-X-NH-C16H33, and X is selected from valine, serine or phenylalanine. The invention introduces fat-soluble antitumor drug into the conjugate with amphipathy to obtain the antitumor target lipidosome drug, the lipidosome system can increase the concentration of the antitumor drug at the target and can reduce toxic and side effects of the antitumor drug to the non-target part, thereby improving the treatment index of the drug. The invention evaluates the antitumor activity of taxol lipidosome by using a Holland sarcoma S180 mouse as a model, the result shows that the taxol lipidosome has more excellent antitumor activity than each control group.

The present invention is directed to novel non-invasive diagnostic and therapeutic tools/compounds comprising a hybride cyclic peptide which utilizes a cyclic peptide chelating group wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compound according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

A method of treating tumors, such as prostate tumors, breast tumors, non-Hodgkin's lymphoma, and the like, includes the sequential steps of administering to the patient at least one dose of an antiangiogenic cyclo-arginine-glycine-aspartic acid-containing pentapeptide (cRGD pentapeptide); administering to the patient an anti-tumor effective amount of a radioimmunotherapeutic agent (RIT); and then administering to the patient at least one additional dose of cRGD pentapeptide. The cRGD pentapeptide is preferably cyclo-(Arg-Gly-Asp-D-Phe-[N-Me]-Val), and the RIT is preferably a radionuclide-labeled chelating agent-ligand complex in which chelating agent is chemically bonded to a tumor-targeting molecule, such as a monoclonal antibody.

The invention discloses a preparation method of an RGD (Arg-Gly-Asp) and PEG (Polyethylene Glycol) co-modified PAMAM (Polyamide-Amne Dendrimer) arsenic trioxide-loaded medicine delivery system. The preparation method comprises the following steps: enabling a sulfydryl group of an RGD cyclopeptide to react with a maleimide group of MAL-PEG-NHS, thus generating RGD-PEG-NHS; then reacting with a surface amino group of PAMAM, thus generating RGD-PEG-PAMAM; enabling the RGD-PEG-PAMAM to react with mPEG-NHS, thus preparing RGD-PEG-PAMAM-mPEG; enabling an arsenic trioxide solution to react with the RGD-PEG-PAMAM-mPEG, thus preparing the RGD and PEG co-modified PAMAM arsenic trioxide-loaded medicine delivery system. According to the preparation method disclosed by the invention, highly toxic traditional Chinese medicine-arsenic trioxide is firstly loaded in PAMAM; compared with an original medicine, a certain slow release action can be reflected, and the problems that ATO is poor in fat solubility, the blood-brain barrier penetration is difficult, body distribution is lack of specificity, and the like are solved; RGD is used for modifying the PAMAM, so that cellular uptake of tumor cells on the PAMAM is further increased; mPEG is used for modifying residual amino groups on the PAMAM, so that the cytotoxicity of a carrier can be further reduced.

The invention discloses an application of a blocker with integrin affinity and bonding capability and MMPs (matrix metalloproteinases) inhibiting capability, and belongs to the field of medicines. The application comprises a polypeptide I (Arg-Gly-Asp-Gly-Gly-Gly-Gly-Pro-(D-Pyr)-(D-Cys)-Bip-Arg-Gly-Glu) and a polypeptide II (Pro-(D-Pyr)-(D-Cys)-Bip-Arg-Gly-Glu-Gly-Gly-Gly-Gly-Arg-Gly-Asp), wherein the polypeptide I is modified with an integrin ligand sequence (Arg-Gly-Asp-Gly-Gly-Gly-Gly); two types of blood vessel inhibiting polypeptides with integrin affinity and bonding capability are formed. The application has the advantages that because of the targeting property of an RGD (arginine-glycin-aspartate) sequence, the polypeptides can be targeted to the new blood vessel endothelium of the RA (rheumatoid arthritis) pannus forming process, the forming of MMPs (matrix metalloproteinases) and the new blood vessel can be inhibited, and the effect of preventing or treating the blood vessel and inflammatory diseases are realized; the polypeptides can be applied to the treatment of the blood vessel and inflammatory diseases, such as arthritis, inflammation, tumors, and eye diseases.

The invention discloses a polypeptide which is marked by radioactive rhenium and contains RGD amino acid sequence, a preparation method and application thereof, wherein N terminal of the polypeptide is histidine residue which is chelated with radioactive rhenium. The structure of the polypeptide is shown as general formula (I), wherein X is a polypeptide chain containing Arg-Gly-Asp sequence. The polypeptide adopts raw materials available. The whole experiment process has simple operation, does not have special requirements such as high temperature and high pressure, adopts a [Re(CO)3(H2O)3]<+> precursor to mark the polypeptide, does not change the structure of the polypeptide, does not affect the biological activity of the polypeptide, and has important realistic significance on early diagnosis and treatment of angiogenesis and tumor transfer.

The invention provides an anti-tumor peptide molecule with multiplex targeting performance and selectivity and application thereof, and belongs to the field of targeted medicine molecules. The molecule structure completeness and the cell non-toxicity can be maintained in the normal cell positions; cell antipersonnel fragments can be released in the tumor cell positions, so that the selective killing on the tumor cells can be realized; meanwhile, the duplex targeting performance can be realized on the tumor cells. The peptide molecule has the following sequence of Ac-Arg-Gly-Asp-Gly-Pro-Leu-Gly-Leu-Ala-Gly-Ile-Ile-Ile-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-NH2(RR22), and can be subjected to enzymolysis by substrate metalloprotease to release LR15 fragments Leu-Ala-Gly-Ile-Ile-Ile-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-NH2 with the tumor cell killing performance. The anti-tumor peptide molecule provided by the invention can be used for preparing tumor cell selective killing agents, and can be effectively applied to targeted killing of tumor cells. Compared with other targeting medicine, the anti-tumor peptide molecule has wider application values.

The present invention provides structures of small molecules capable of modulating apoptotic cell death. More specifically, the structures relate to the structures of apoptotic active sites of mammalian alpha-fetoprotein (AFP) and albumin. Peptides mimicking the active site contain two sequences, Arg-Gly-Asp and Asp-X-X-Asp, wherein X means any amino acid. These sequences are needed in the same molecule for causing a wide range of biological activities. The peptides can be utilized to suppress apoptotic pathways by inhibiting the cytochrome c-mediated caspaseactivation. Thus, the peptides can be used to inhibit effects of apoptosis induced by oxidative stress, drugs, cytokines, Fas-ligand, alpha-fetoprotein, used to prevent apoptosis in culturing cells, in organ transplantation, in immunological autoimmune disorders and immunodeficiency syndrom induced by viral infection, or to diminish side cytotoxic effects after chemotherapy and radiation therapy.

The invention provides a small molecular polypeptide for reforming RGD tripeptide. According to the characteristic that the RGD is specifically combined with alpha<IIb>beta3, a hydrophobic amino acid and a basic amino acid are added at the N end of the RGD, a hydrophobic amino acid W is added in the fourth site, a basic amino acid R is added in the fifth site, the small peptide sequence is Arg-Gly-Asp-Trp-Arg, the protein primary structure is RGDWR, the capability for specifically being combined with the alpha<IIb>beta3 can be improved, the immunogenicity can also be reduced by smaller molecular weight, and the defects of the existing antithrombotic preparations are overcome.

The present invention relates to the field of pharmaceutics and clinical pharmacy, involving the preparation method and application of a cyclic peptide containing Argnine-Glycine-Aspartate sequence and its active targeting liposomes. The cyclic peptide described here meets the requirement for ligand in that it forms ring by amide linkage with stable sterical structure, it shows low propensity to degrade, and it carries an active hydrosulfide group which is easy to modify carriers. The artificially synthesized peptide, which has a small molecular weight and low propensity to cause immune response, can be used as the ligand to bind with the integrin on the surface of HSC. The active targeting liposome established with the cyclic peptide realized cell-targeted therapy of experimental hepatic fibrosis via receptor-mediated pathway. The invention can target RGD cyclic peptide-labeled interferon-loaded liposomes to the fibrotic liver and its good efficacy in the treatment of hepatic fibrosis has been proven by experiments in rats in vitro and in vivo.