摘要:
The present invention describes methods for modulating vascular permeability (VP) in tissues using Src or modified Src protein, Yes protein or modified Yes protein, Src family tyrosine kinase protein inhibitors, and nucleic acids capable of expression of Src or modified Src protein, Yes protein or modified Yes protein, and Src family tyrosine kinase protein inhibitors, or mixtures thereof. The invention also describes methods for inhibiting VP using an inactive Src or Yes protein or a mixture thereof, or CSK protein or modified CSK protein, or nucleic acids encoding therefor, or by using chemical Src family tyrosine kinase inhibitors such as PP1, PP2, PD173955, AGL1872, PD162531, Radicicol R2146, and Geldanamycin, or for potentiating VP using an active Src or Yes protein or a mixture thereof, or nucleic acids encoding therefor. Related compositions and articles of manufacture are also disclosed.
摘要:
The invention teaches methods for treating tumors and tumor metastases in a mammal comprising administering, to a mammal in need of treatment, a therapeutic amount of an antagonist sufficient to inhibit angiogenesis in combination with a therapeutic amount of anti-tumor immunotherapeutic agent, such as an anti-tumor antigen antibody/cytokine fusion protein having a cytokine and a recombinant immunoglobulin polypeptide chain sufficient to elicit a cytokine-specific biological response.
摘要:
The present invention describes methods for inhibiting angiogenesis in tissues using vitronectin αvβ5 antagonists. The αvβ5-mediated angiogenesis is correlated with exposure to cytokines including vascular endothelial growth factor, transforming growth factor-α and epidermal growth factor. Inhibition of αvβ5-mediated angiogenesis is particularly preferred in vascular endothelial ocular neovascular diseases, in tumor growth and in inflammatory conditions, using therapeutic compositions containing αvβ5 antagonists.
摘要:
Myocardial infarction in a mammal is treated by administering to the mammal a therapeutically effective amount of a chemical Src family tyrosine kinase protein inhibitor and the use of such inhibitor compounds for the preparation of a medicament for treating myocardial infarction. Myocardial infarction can be prevented by administering to the mammal a prophylactic amount of the inhibitor. The inhibitor preferably is an inhibitor of Src protein selected from the group consisting of a pyrazolopyrimidine class Src family tyrosine kinase inhibitor, a macrocyclic dienone class Src family tyrosine kinase inhibitor, a pyrido[2,3-d]pyrimidine class Src family tyrosine kinase inhibitor, a 4-anilino-3-quinolinecarbonitrile class Src family tyrosine kinase inhibitor, and a mixture thereof. The Src family tyrosine kinase inhibitors can be used to prepare medicaments for the treatment of myocardial infarction. Also disclosed are articles of manufacture containing a chemical Src family tyrosine kinase inhibitor.
摘要:
Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-αvβ3 are inhibited by an inhibitor compound of formula (I): wherein G?1 and G2¿ are each independently NH-C(O)-O-R1, -NH-C(O)-O-(CH¿2?)v-(C6H4)-X?3¿, -NH-C(O)-NH-(CH¿2?)v-(C6H4)-X?3¿, -O-C(O)-NH-(CH¿2?)v-(C6H4)-X?3¿,-O-C(O)-O-(CH¿2?)v-(C6H4)-X?3¿, or NH-C(O)-CH¿2?-(C6H4)-X?3; Y1 and Y2¿ are each independently OH, C¿1?-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl, benzyl, or NH2; R?1 is C¿1-C4 alkyl; X?1 and X2¿ are each independently halo or C¿1?-C4 alkoxy; X?3¿ is halo, nitro, C¿1?-C4 alkyl, C1-C4 alkoxy, or C1-C4 perfluoroalkyl; Z is -C C-, -C6H4-, cis-CH=CH-, trans CH=CH-, cis-CH2-CH=CH-CH2-, trans -CH2-CH=CH-CH2-, 1,4-naphthyl, cis-1, 3-cyclohexyl, trans-1, 3-cyclohexyl, cis-1, 4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each independently an integer having a value of 0 or 1; t is an integer having a value of 0 or 1; and p, r, and v are each independently an integer having a value of 1 or 2; with provisos that when A is H, t is O; when A is a covalent bond, t is 1; when m is 0, Y?1 is C¿1-C4 hydroxyalkyl; and when n is 0, Y2 is C1 C4 hydroxyalkyl.
摘要:
The present invention describes methods for inhibition of angiogenesis in tissues using vitronectin αvβ3 antagonists, and particularly for inhibiting angiogenesis in inflamed tissues and in tumor tissues and metastases using therapeutic compositions containing αvβ3 antagonists.
摘要:
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.
摘要:
Compositions and methods for inhibiting or ameliorating post-operative/post-wounding adhesion formation in patients are disclosed. Such compositions and methods utilize an antagonist molecule that blocks or inhibits alpha V beta 3 integrin binding to an extra cellular matrix protein such as fibronectin.