90 results about "Integrin receptors" patented technology

The present invention is directed to an antibody or derivative thereof of human origin for inhibiting platelet aggregation, characterized in that it is effective by substantially exclusive binding to the activated state of platelet integrin receptor GPIIb / IIIa.

The invention provides a novel polypeptide modified tumor targeted liposome of a targeted integrin receptor. The novel polypeptide is mainly formed by covalent linkage of ring-shaped RGD and cell penetrating peptides, and not only has the selective targeting capability of an integrin receptor, but also can achieve mediated endocytosis; the liposome mainly comprises phospholipid, cholesterol, lipid-polyethyleneglycol and lipid-polyethyleneglycol-novel polypeptide ligand chimeric substance, and is a very potential tumor targeted treatment carrier.

The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel aza-bicycloalkane based cyclic peptides, acting as a targeting moiety towards integrin receptors.

An immunoliposome composition targeted to the alphaV-integrin subunit of integrin receptors comprised of ligand-targeted liposomes bearing at least one targeting-ligand derived from an antibody and having binding specificity for at least one integrin receptor comprising an alpha V subunit including αvβ1, αvβ3 αvβ5, αvβ6, or αvβ8 integrin cell receptors is described. The antibody-derived targeting ligand may be a Fab′ fragment, a scFv, or the like. Binding of the immunoliposome to αv-integrin expressing cells, preferably results in internalization of the immunoliposome for cytoplasmic delivery of a liposome-entrapped agent.

The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise a targeting vector which binds to receptors associated with integrin receptors.

The present invention is directed to an antibody or derivative thereof of human origin for inhibiting platelet aggregation, characterized in that it is effective by substantially exclusive binding to the activated state of platelet integrin receptor GPIIb / IIIa.

The present invention is based on the discovery that a vascular stent or other implantable medical device can be coated with a biodegradable biocompatible polymer to which is attached a bioligand that specifically captures progenitors of endothelial cells (PECs) from the circulating blood to promote endogenous formation of healthy endothelium in Type II diabetics. In one embodiment, the bioligand is a peptide that specifically binds to an integrin receptor on PECs. The invention also provides methods for using such vascular stents and other implantable devices to promote vascular healing in Type II diabetics, for example following mechanical intervention.

The invention relates to engineered antibodies which specifically bind to integrin receptors, especially the alpha V integrin receptor subunit. The antibodies comprise the antigen binding sites (CDRs) of a known mouse anti-integrin antibody, as well as hybrid light chain variable sequences, mutated heavy chain variable sequences (Frs) and modified heavy chain constant sequences. The novel antibodies have improved immunogenic and expression properties and elicit excellent anti-angiogenic as well as anti-tumor activities in humans in monotherapy but also and above all in combination with other angiogenesis and tumor inhibiting agents.

A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of α4β1, α5β1, α4β7, αvβ3 and αLβ2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.

The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.

The invention belongs to the fields of bioengineering pharmacy, protein polypeptide drugs and biomedical engineering and relates to a polypeptide having high affinity with a receptor of integrin alpha v beta3 and application of the polypeptide. The sequence of the polypeptide is Arg-Trp-Arg or Arg-Lys-Tyr. The polypeptide disclosed by the invention has higher affinity with the integrin alpha v beta3 than the traditional RGD (Arginine-Glycine-Aspartic acid) peptide and can be used in diagnosis and treatment of cancer.

The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.

The invention provides a serial cell-penetrating peptide modified tumor targeted and tumor penetrated nano drug delivery system capable of simultaneously identifying an integrin receptor and a transmembrane protein receptor, wherein the serial cell-penetrating peptide is mainly formed by connecting a DGR polypeptide fragment covalently at the C-tail end of polyarginine of the cell-penetrating peptide. The polypeptide not only can selectively identify two highly expressed receptors on the surfaces of the tumor cells, but also can be efficiently mediated into the cells. The nano drug delivery system mainly consists of a nano carrier, a drug and a lipid-polyethylene glycol-serial cell-penetrating peptide ligand interstitial compound and is a potential tumor targeted treatment carrier.

Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 integrins which is useful for prophylactic and / or therapeutic treatment of diseases and conditions associated with α4 integrins or their ligands.

The present invention relates to chimeric biological vectors for gene trnasduction in eukaryotic cells. The invention further relates to a method for producing said chimerized vectors and a method for transduction of eukaryotic cells, in particular cells expressing integrin receptors.

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 invention relates to the technical field of medicine, in particular to an exosome carrier of a target integrin alpha v beta 3 and a preparation method and application of the exosome carrier. Mononuclear suspension cells THP-1 are adopted and stimulated by PMA of the certain concentration to obtain the exosome carrier, the surface of an exosome after separating contains an RGD target molecule metalloprotease disintegrin family 15, and the target integrin receptor alpha v beta 3 can be obtained. The in-vitro releasing experiment shows that the prepared exosome can slowly release loaded chemotherapeutic medicine, and the better capacity of jointly loading genes and the chemotherapeutic medicine is achieved. In the tumor treatment process, the exosome can enhance the effects of cells of aspecificity target overexpression integrin alpha v beta 3 on tumor cells through the chemotherapeutic medicine or gene medicine, apoptosis of tumor cells is promoted, and therefore the exosome carrierforms a targeted and efficient low-toxicity bionic nanoscale delivery system of tumor treatment.

The invention belongs to the technical field of biological medicines, and relates to a combined drug-dosing micelle of a targeted integrin receptor and a preparation method thereof. Pluronic COOH which is modified by a terminal carboxyl is synthesized, and RGD (arginine-glycine-aspartic acid) polypeptides are connected with carboxyl by amido bonds to obtain a RGD polypeptide-modified Pluronic copolymer (RGD-Pluronic); and after copolymerization of drug doxorubicin (DOX) and Pluronic, another drug PTX (paclitaxel) is coated and loaded by a thin-film hydration method to prepare a mixed micelle (RGD-FP-DP). According to the preparation method, drug loading capacity of the micelle can be improved, the drug concentration of anti-tumor drugs in a target site can be increased, accumulation of the anti-tumor drugs in a non target site can be reduced, and the therapeutic index of the drugs can be effectively improved.

Compounds of Formula (I) are described in which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

The invention relates to a targeted adhesion chitosan material and application thereof. Under the action of dual-functional (N-hydroxysuccinimide / azide) light-sensitive cross-linking agent, through grafting reaction by UV photochemical activation, cell adhesion peptide is grafted on the chitosan to obtain the safe (non-toxic and degradable) targeted adhesion chitosan material which is characterized in that the biocompatibility is good, the biological function is good and the dissolubility under faintly acid condition is obviously enhanced. Through self assembling method, the targeted adhesion chitosan material can form stable nano particles with grain size of 100mm-500mm and surface positive charge of 10mV-30mV and the stable nano particles can be used as the carriers of DNA (20bp-10kb) or RNA [dsRNA (500-700bp), small RNA (siRNA, microRNA or shRNA)] and other nucleic acid drugs. When the carried DNA or RNA is protected from being degraded by the corresponding enzyme, the carried DNA or RNA can target at the overexpressed integrin receptors on the surface of tumor cells, so cell transfection and release in cells are facilitated to cure tumors.

Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 integrins which is useful for prophylactic and / or therapeutic treatment of diseases and conditions associated with α4 integrins or their ligands.

αvβ3 Integrin receptor targeting liposomes comprise a cationic amphiphile such as a cationic lipid, a neutral lipid, and a targeting lipid. The targeting lipid includes a non-peptidic αvβ3 integrin antagonist.

An immunoliposome composition targeted to the alphaV-integrin subunit of integrin receptors comprised of ligand-targeted liposomes bearing at least one targeting-ligand derived from an antibody and having binding specificity for at least one integrin receptor comprising an alpha V subunit including αvβ1, αvβ3 αvβ5, αvβ6, or αvβ8 integrin cell receptors is described. The antibody-derived targeting ligand may be a Fab′ fragment, a scFv, or the like. Binding of the immunoliposome to αv-integrin expressing cells, preferably results in internalization of the immunoliposome for cytoplasmic delivery of a liposome-entrapped agent.

The invention belongs to the technical field of biomedicine production or the fields of protein polypeptide drugs and biomedical engineering, and in particular relates to a polypeptide which has high affinity with an integrin receptor and an application of the polypeptide like cancer diagnosis and treatment. The polypeptide is composed of five amino acids, and the sequence is arginine-tryptophan-arginine-asparagine-methionine (Arg-Trp-Arg-Asn-Met). On the basis of an in-vitro flow cytometry affinity determination experiment, the polypeptide disclosed by the invention has quite strong targeting on high-expression cells of the integrin receptor, and through an in-vitro laser confocal cell uptake experiment, the polypeptide can be targeted to high-expression tumor cells of the integrin receptor alpha-v-beta-3 and can basically avoid targeting on low-expression tumor cells and normal cells of the integrin receptor alpha-v-beta-3. An in-vitro cytotoxicity result shows that the 5-peptide disclosed by the invention is basically free from toxicity on cells, and the 5-peptide has a good application prospect in the diagnosis and the treatment of cancers.

Polynucleotides encoding mammalian ECM signaling molecules affecting the cell adhesion, migration, and proliferation activities characterizing such complex biological processes as angiogenesis, chondrogenesis, and oncogenesis, are provided. The polynucleotide compositions include DNAs and RNAs comprising part, or all, of an ECM signaling molecule coding sequence, or biological equivalents. Polypeptide compositions are also provided. The polypeptide compositions comprise mammalian ECM signaling molecules, peptide fragments, inhibitory peptides capable of interacting with receptors for ECM signaling molecules, and antibody products recognizing Cyr61. Also provided are methods for producing mammalian ECM signaling molecules. Further provided are methods for using mammalian ECM signaling molecules to screen for, and / or modulate, conditions and disorders associated with angiogenesis, chondrogenesis, and oncogenesis; ex vivo methods for using mammalian ECM signaling molecules to prepare blood products are also provided. Additionally, modulators, such as peptide modulators, of an ECM signaling molecule activity are provided. Further provided are methods for screening for modulators of a Cyr61 polypeptide-integrin receptor interaction, as well as methods of treating conditions and disorders associated with such an interaction.

The present invention is based on the discovery that a vascular stent or other implantable medical device can be coated with a biodegradable biocompatible polymer to which is attached a bioligand that specifically captures progenitors of endothelial cells (PECs) from the circulating blood to promote endogenous formation of healthy endothelium in Type II diabetics. In one embodiment, the bioligand is a peptide that specifically binds to an integrin receptor on PECs. The invention also provides methods for using such vascular stents and other implantable devices to promote vascular healing in Type II diabetics, for example following mechanical intervention.

The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.

Compounds of Formula (I) are describedin which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.