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115 results about "Disintegrin" patented technology

Disintegrins are a family of small proteins (45–84 amino acids in length) from viper venoms that function as potent inhibitors of both platelet aggregation and integrin-dependent cell adhesion.

Selective inhibition of aggrecanase in osteoarthritis treatment

This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50s of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metalloproteinases (ADAMs or reprolysins). This invention also relates to compounds, methods of treatment and composition of Formula I: or a therapeutically acceptable salt thereof, whereinX is carbon or nitrogen;R1 and R2 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, wherein at least one of R1 and R2 is methyl;R3 and R4 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, or R3 and R4 may be taken together to form a carbonyl group; andR5 and R6 are independent substituents in the ortho, meta, or para positions and are independently selected from the group consisting of hydrogen, halogen, cyano, methyl, and ethyl;with the provisos:when X is carbon, then R7 and R8 are both hydrogen and at least one of R1, R2, R3, and R4 is hydroxy;when X is carbon and R5 is para-halo, then at least one of R6, R3, and R4 is not hydrogen;when X is nitrogen, then R8 is not present and R7 is hydrogen or a group of the formula: wherein, Y is —CH2—NH2 or —NH—CH3; andwhen X is nitrogen and R7 is H, then R3 and R4 are taken together to form a carbonyl group.
Owner:PFIZER INC +1

Selective inhibition of aggrecanase in osteoarthritis treatment

InactiveUS20050227997A1Ease of preparation and delectabilityGood metabolic stabilityAntibacterial agentsSenses disorderProteoglycanaseDisintegrin
This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50s of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metalloproteinases (ADAMs or reprolysins). This invention also relates to compounds, methods of treatment and composition of Formula I: or a therapeutically acceptable salt thereof, wherein X is carbon or nitrogen; R1 and R2 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, wherein at least one of R1 and R2 is methyl; R3 and R4 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, or R3 and R4 may be taken together to form a carbonyl group; and R5 and R6 are independent substituents in the ortho, meta, or para positions and are independently selected from the group consisting of hydrogen, halogen, cyano, methyl, and ethyl; with the provisos: when X is carbon, then R7 and R8 are both hydrogen and at least one of R1, R2, R3, and R4 is hydroxy; when X is carbon and R5 is para-halo, then at least one of R6, R3, and R4 is not hydrogen; when X is nitrogen, then R8 is not present and R7 is hydrogen or a group of the formula: wherein, Y is —CH2—NH2 or —NH—CH3; and when X is nitrogen and R7 is H, then R3 and R4 are taken together to form a carbonyl group.
Owner:PFIZER INC +1

Stapled-RGD polypeptide, and applications thereof in tumor targeting delivery

The invention belongs to the field of pharmacology, and relates to stapled-RGD polypeptide, and applications thereof in tumor targeting delivery. Multifunctional targeting polypeptide molecule stapled-RGD with high combination activity with integrin and biological membrane barrier penetration capacity is designed and prepared based on binding peptide cyclization technology; and preparation of fluorescein, drugs, and high molecule carriers modified by the multifunctional targeting polypeptide molecule stapled-RGD, and applications of the fluorescein, the drugs, and the high molecule carriers in tumor imaging and construction of targeted therapy targeted drug delivery systems are disclosed. It is shown by results that specific uptaking of model drugs carried by stapled-RGD by positive cells, tumor mimicry vessels, and tumor ball tissues of expressed integrin is realized, higher tumor targeting capacity, imaging functions, and membrane barrier cell penetration capacity are achieved; nano targeted drug delivery systems constructed by the high molecule carriers modified by stapled-RGD can be used for delivering carried model drugs to target tissues, antitumor drug effect is improved obviously; and stapled-RGD possesses a promising application prospect in mediating drugs, nano targeted drug delivery system membrane barrier penetration, active target searching, tumor diagnosis, and targeted therapy.
Owner:FUDAN UNIV

Long non-coding RNA AY927503 and application thereof

The invention belongs to technical field of genes, and relates to a long non-coding RNA AY927503 and application thereof. It is proved through experiments that the long non-coding RNA AY927503 can adjust migration of human hepatocellular carcinoma cells, sulfatide can adjust migration of the human hepatocellular carcinoma cells through the long non-coding RNA AY927503, express of integrin alpha V can be adjusted, and the long non-coding RNA AY927503 can adjust migration of the cells through the integrin alpha V; it is proved through experiments that the long non-coding RNA AY927503 is mainly located in cytoplasm and also exists in cell nuclei, the long non-coding RNA AY927503 can adjust the activity of a promoter of the integrin alpha V, and the long non-coding RNA AY927503 is not combined with a transcription factor on the promoter of the integrin alpha V but is directly combined with the promoter of the integrin alpha V. According to the long non-coding RNA AY927503 and the application thereof in gene control, the long non-coding RNA AY927503 can be directly combined with the promoter of the integrin alpha V, adjust the transcriptional activity of the integrin alpha V and then influence the behavior of the cells; the long non-coding RNA AY927503 can be used for preparing a target molecule of the human hepatocellular carcinoma cells.
Owner:FUDAN UNIV
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