Antiangiogenic peptides, process of their preparation, and polynucleotides encoding the same

摘要

The present invention relates to a compound represented by the structural formula A-B-C-X-Y or a pharmaceutically acceptable salt or ester thereof, wherein A is absent or a nitrogen protecting group; Y is absent or a carboxylic acid protecting group; B-C-X are selected from the group consisting from sequences defined by the following positions of amino acids SEQ ID NO:1; (a) a sequence from amino acid position 355 to about amino acid position 543; (b) a sequence from amino acid position 355 to about amino acid position 546; (c) a sequence from amino acid position 443 to about amino acid position 543; (d) a sequence from amino acid position 449 to about amino acid position 543; (e) a sequence from amino acid position 454 to about amino acid position 543; (f) a sequence from amino acid position 443 to about amino acid position 546; (g) a sequence from amino acid position 449 to about amino acid position 546; (h) a sequence from amino acid position 454 to about amino acid position 546; (i) a sequence from amino acid position 525 to about amino acid position 535; (j) a sequence from amino acid position 529 to about amino acid position 535; (k) a sequence from amino acid position 530 to about amino acid position 535; (l) a sequence from amino acid position 529 to about amino acid position 534; (m) a sequence from amino acid position 531 to about amino acid position 534; (n) a sequence from amino acid position 450 to about amino acid position 543. The invention also relates to a composition containing the above-described compound and a pharmaceutically acceptable excipient. The present invention also includes a method of making the above-indicated compound wherein the method comprises the steps of: (a) exposing a mammalian plasminogen to elastase at a ratio of about 1:100 to about 1:300 to form a mixture of said plasminogen and said elastase; (b) incubating said mixture and (c) isolating the indicated compound from said mixture.