Abstract: A method of inhibiting parasitic activity is disclosed in which the biosynthesis of the glycosyl phosphatidylinositol (GPI) anchor of said parasite is inhibited by incorporating into said GPI anchor an oxy-substituted fatty acid analog in place of myristate. The inhibitory compounds ar C.sub.13 and C.sub.14 fatty acids or alkyl esters thereof in which a methylene group normally in carbon position 4 to 13 of said fatty acid is replaced with oxygen.

Abstract: Antiviral O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol are disclosed that contain an N-alkyl or N-aroyl radical in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoro alkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl radical is selected from the group consisting of p-decylbenzoyl, 3-(p-chlorophenoxy)propanoyl, 2-(acetyloxy)benzoyl, [1,1'-biphenyl]-4-ylcarbonyl, 2-thiopheneacetyl, trans-3-furanacryloyl, 3-methoxyphenylacetyl and 3-(trifluoromethyl)benzoyl, and wherein the N-alkyl contains from one to fourteen carbon atoms, provided that when N-alkyl contains from one to five carbon atoms the O-acylated groups are .omega.,.omega.,.omega.-trifluoro alkanoyl or carboxylic cycloalkanoyl.

Abstract: A novel pentadecapeptide is disclosed which is useful for the control of intestinal fluid absorption and that has the following amino acid sequence ##STR1##

Abstract: A novel transposon useful for sequencing long DNAs is disclosed which comprises a partial sequence of transposon Tn5 with the oligonucleotide primers from phages SP6 and T7 inserted near the opposite ends, respectively, of said transposon Tn5.

Abstract: .alpha.-Homojirimycin and 6-dpi-homojirimycin are each synthesized from 2-azido-2-deoxy-3,4:6,7-di-O- isopropylidene-D-glydero-D-talo-heptono-1,5-lactone in which the side chain acetonide is hydrolyzed to give the corresponding diol which is then protected with a silyl protecting agent to form a silyl ether. The latter compound is used as a divergent intermediate in which the piperidine ring is formed by joining the nitrogen function at C-2 to C-6 (A) with inversion of configuration at C-6 to form 6-epi-homomannojirimycin or (B) with retention of configuration at C-6 to form .alpha.-homomannojirimycin.

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: An Entamoeba histolytica specific cDNA clone which encodes an antigenic surface membrane protein possessing multiple tandem repeats and expression in E. coli is disclosed.

Abstract: Novel short peptides are disclosed which are selected from the group consisting of GPAGKDGEAGAQG and fragments thereof containing the minimal sequence Ala Gly Glu Ala. These peptides have inhibitory activity against .alpha..sub.2 .beta..sub.1 -mediated Mg.sup.++ -dependent adhesion of platelets to collagen.

Abstract: A modified heparin cofactor II is disclosed, HCII(Leu.sub.444 .fwdarw.Arg), which has substantially improved inhibitory activity against thrombin compared to native HCII or antithrombin.

Abstract: A method of purifying PAI-1 from a biological fluid source, e.g. conditioned media of Hep G2 or HT 1020 cells, containing PAI-1 is disclosed, which comprises subjecting the biological fluid to a modified urokinase affinity absorbent, e.g. anhydrourokinase ligand bound to a CNBr-activated agarose gel or urokinase mutated at amino acid position 356 from Ser to Gly and bound to the gel, and then eluting PAI-1 from said affinity absorbent. A method of stabilizing and/or activating PAI-1 is also disclosed, which comprises complexing PAI-1 with vitronectin.

Abstract: The disclosure describes novel immunosuppressive agents isolated from syncytiotrophoblast microvilli membranes by preparing a minutely subdivided and solubilized preparation of said membranes and isolating the unreduced N-linked oligosaccharides from an extract of the preparation.

Abstract: Novel blood coagulation inhibitors are disclosed which are peptide fragments comprising (A) Kunitz-type domain two of lipoprotein-associated coagulation inhibitor which inhibits Factor Xa production and (B) Kunitz-type domains one and two of lipoprotein-associated coagulation inhibitor which inhibits Factor VIIa/TF enzymatic complex formation.

Abstract: Novel antiviral peptides are disclosed which have a sequence of about 6 to 30 amino acids and which are substantially identical to a small portion of a glycoprotein in a virus that contains a lipid-bilayer in its structure. A preferred peptide having antiviral activity against influenza virus is the decapeptide amide N-G-S-L-Q-C-R-I-C-I-NH.sub.2 [SEQ ID NO:3].

Abstract: A modified heparin cofactor II is disclosed, HCII (Leu.sub.444 .fwdarw.Arg), which has substantially improved inhibitory activity against thrombin compared to native HCII or antithrombin.

Abstract: A method is provided for converting therapeutic glycosidase inhibitors to novel prodrugs by phosphorylation of a free hydroxyl group on the molecule to substantially reduce the glycosidase inhibitory activity without thereby substantially reducing the therapeutic activity.

Abstract: A modified t-PA having improved in vivo half-life is disclosed comprising in sequence a sequence of two K2 kringle regions and a serine protease region SP.

Abstract: A method of oligosaccharide sequencing in which the components are determined essentially simultaneously is disclosed which comprises a series of steps as follows:A. Placing an identifying label on the reducing terminal residue of the oligosaccharide to be sequenced,B. Dividing said oligosaccharide into a plurality of separate portions of known integer amounts,C. Treating each said portion with a different reagent mix to thereby provide a series of reaction mixtures,D. Pooling known integer amounts of the products from each separate reaction mixture to give a product pool,E. Performing an analysis on said product pool which measures the molar proportions of the reaction products, andF. Reconstructing or identifying the starting oligosaccharide from the molar prevalence of said reaction products.

Abstract: .alpha.-Homojirimycin and 6-dpi-homojirimycin are each synthesized from 2 az ido-2-deoxy-3,4:6,7-di-O-isopropylidene-D-glycero-D-talo-heptono-1,5-la ctone in which the side chain acetonide is hydrolyzed to give the corresponding diol which is then protected with a silyl protecting agent to form a silyl ether. The latter compound is used as a divergent intermediate in which the piperidine ring is formed by joining the nitrogen function at C-2 to C-6 (A) with inversion of configuration at C-6 to form 6-epi-homomannojirimycin or (B) with retension of configuration at C-6 to form .alpha.-homomannojirimycin.

Abstract: The synthesis of the novel fucosidase inhibitors, .beta.-L-homofuconojirimycin and related 1-.beta.-C-substituted deoxymannojirimycins, is disclosed.