37 results about "Αvβ3 integrin" patented technology

An aryl-substituted alicyclic compound of the formula (I):wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is —CONH—, etc., R3 is hydrogen, etc., R5 is hydrogen, aryl, etc., R6 is a mono-substituted amino (e,g., benzyloxycarbonylamino), R7 is hydrogen, etc., and a process for preparation thereof, and a pharmaceutical composition containing the same. The compound of the present invention has a high selectivity for αvβ3 integrin, and exhibits a potent inhibitory activity thereto, and hence, it is useful as a preventive or / and a therapeutic agent for a disease in which αvβ3 integrin is involved.

Disclosed herein are peptides which include an isoDGR motif and which selectively inhibit αvβ3 integrin. In some embodiments, the isoDGR motif results from the deamidation of an NGR motif.

This invention relates to new peptide-based compounds and their use in therapeutically effective treatments as well as for diagnostic imaging techniques. More specifically the invention relates to the use of such peptide-based compounds used as targeting vectors that bind to receptors associated with angiogenesis, in particular the alphavbeta3 integrin receptor. Such contrast agents may thus be used for diagnosis of for example malignant diseases, heart diseases, inflammation-related diseases, rheumatoid arthritis and Kaposi's sarcoma. Moreover such compounds may also be used in therapeutic treatment of these diseases.

The invention generally relates to fusion proteins comprising a rhodostomin variant having an RGD motif variant 48ARLDDL53, wherein the rhodostomin variant is conjugated with a variant of Human Serum Albumin (HSA). The invention also relates to the use of these fusion proteins for treatment and prevention of avss3 integrin-associated diseases.

The invention discloses a USPIO-PLA-RGD compound, a preparation method and application thereof. The USPIO-PLA-RGD compound uses USPIO as a core, is coated by PLA outside, and is labeled as PLA-USPIO; and the USPIO-PLA-GRD compound obtained through covalently coupling carboxyl of a functional group exposed on the surface of PLA and amidogen of RGD peptide has a hydrated grain diameter of between 90 and 105 nm. The USPIO-PLA-RGD compound can be applied as magnetic resonance tumor angiogenesis targeting contrast agent. The invention realizes targeting developing by the characteristics of high affinity of an alpha v beta3 integrin receptor and ligand RGD peptide thereof, and the combination has the characteristics of high specificity, selectivity, saturation and affinity, clear biological effect and the like. The concentration of a medicament in a partial focus can be increased, and toxic and side effects can be reduced by using the ligand RGD peptide as a vector of USPIO through the mediation effect of the receptor, so that the aim of development of a targeting tumor angiogenesis living body is realized.

The invention discloses a nanometer drug of dendrobetin with a small particle size targeting αvβ3 integrin receptor highly expressed tumor cells and a preparation method thereof. The mass ratio of the raw material drug to the carrier is 1:10-1:100, and the carrier includes an amphiphilic polymer and a targeting compound, wherein the molar ratio of the amphiphilic polymer to the targeting compound is 1:100-1: 1. The carrier is a micelle carrier, the surface of which is modified with a high-affinity ligand of the αvβ3 integrin receptor overexpressed on the surface of tumor cells. The invention realizes that the drug can actively target specific tumor cells and can make the drug fast and effective Being taken up by cells, the drug can exert anti-tumor effect to a greater extent, and reduce the distribution of the drug in the whole body and the resulting toxic and side effects.