Abstract: A class of compounds is described for use as fluorogenic substrates for herpesvirus proteases and for use in an assay to identify inhibitors of herpesvirus proteases. ##STR1## wherein W is selected from glycine, 4-aminobutyric acid, 5-aminopentanoic acid, 6-aminocaproic acid and 7-aminoheptanoic acid; wherein Y is selected from EDANS, Abz, DANSYL, nicotinic acid, 4-guanidino-benzoic acid, N-methyl-Abz, 4-chloro-Abz, 5-chloro-Abz, 6-chloro-Abz, 3,5-dibromo-Abz, 6-amino-nicotinic acid, 2-amino-nicotinic acid, 2-chloronicotinic acid, niflumic acid and fluorogenic derivatives thereof; and wherein Z is selected from tryptophan, tyrosine, phenylalanine, p-nitrophenylalanine, m-nitrophenylalanine, DABSYL, DABCYL and halogenated derivatives thereof.

Abstract: A class of compounds is described for use as fluorogenic substrates for herpesvirus proteases and for use in an assay to identify inhibitors of herpesvirus proteases. Compounds of particular interest are defined by Formula II ##STR1## wherein W is selected from glycine, 4-aminobutyric acid, 5-aminopentanoic acid, 6-aminocaproic acid and 7-aminoheptanoic acid; wherein Y is selected from EDANS, Abz, DANSYL, nicotinic acid, 4-guanidino-benzoic acid, N-methyl-Abz, 4-chloro-Abz, 5-chloro-Abz, 6-chloro-Abz, 3,5-dibromo-Abz, 6-amino-nicotinic acid, 2-aminonicotinic acid, 2-chloronicotinic acid, niflumic acid and fluorogenic derivatives thereof; and wherein Z is selected from tryptophan, tyrosine, phenylalanine, p-nitrophenylalanine, m-nitrophenylalanine, DABSYL, DABCYL and halogenated derivatives thereof.

Abstract: A novel and unique plasminogen activator inhibitor fragment is obtained from human umbilical vein endothelial cells which has the following characteristics:A. it is derived from a native t-PA inhibitor that binds to and inhibits the activity of t-PA,B. it is dissociated from a complex formed between said native t-PA inhibitor and t-PA, said complex existing in two distinct interconvertible conformations with molecular weight of about 88 KDa and 105 KDa, respectively, and being partially reversible in the presence of fibrin,C. it has a molecular weight of about 40 KDa when dissociated from the complex, andD. it has a novel partial N-terminal amino acid sequence when dissociated from the complex.

Abstract: Plasminogen activators (PA) are obtained from cultured normal human colon cells which are adaptable to large scale production. A purified tissue PA (t-PA) is obtained from CCD-18Co normal human colon fibroblast cells which shows chemical differences from Bowes melanoma t-PA.

Abstract: A method of increasing the specific activity of tissue plasminogen activator is disclosed which comprises increasing the proportion of neutral oligosaccharides in the tissue plasminogen activator glycoprotein.

Abstract: Novel peptide fragments of tissue plasminogen activator are described which have activity for inhibiting (a) the binding of tPA to human endothelial cells, and (b) the inactivation of tPA by plasminogen activator inhibitor-1 (PAI-1). Six peptides or peptide amides with these activities have the sequences, numbered according to the native protein:tPA (31-55),tPA (81-105),tPA (181-205),tPA (301-325),tPA (451-475, andtPA (531-555).It is hoped that small, synthesizeable molecules which prevent the inactivation of tPA by PAI-1 may provide a means for improving the efficacy of therapeutically administered tPA or for reducing the tendency of patients with elevated plasma PAI-1 concentrations to form fibrin clots.

Abstract: Normal human colon fibroblast tissue plasminogen activator is separated by lysine-Sepharose affinity chromatography into Types I and II glycoforms and characterized with respect to the relative incidence of each type of oligosaccharide comprising the respective Types I and II glycoforms.

Abstract: The solubility of tissue plasminogen activator in aqueous solution is enhanced by incorporating therein arginine or a non-toxic salt of arginine in an amount effective to increase the solubility of the t-PA without substantially inhibiting its potential biological activity upon administration.