Abstract: Disclosed are methods and compositions for the identification, characterization and inhibition of mammalian farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21.sup.ras. One farnesyl protein transferase which is disclosed herein exhibits a molecular weight of between about 70,000 and about 100,000 upon gel exclusion chromatography. Also disclosed are methods and compositions for the preparation of farnesyl transferase by recombinant means, following the molecular cloning and co-expression of its two subunits, for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21.sup.ras.

Abstract: The present invention relates to the production of nucleoproteins, more especially DNA, and their use in therapeutic compositions suitable for the treatment of neoplasms, pathological conditions, infections, osteoarticular disorders and the like, which comprise said nucleoproteins as active agent.Similarly, the invention comprises compositions which protect against the harmful effects of radiation and poisons in general, which also comprise said nucleoproteins as active agent.Finally, the present invention relates to a method for treating patients suffering from neoplasms and the like, whereby therapeutically effective quantities of said compositions are administered to the patient.

Abstract: The present invention relates to chemically modified hemoglobin produced by a novel and efficient method in which stroma-free hemoglobin is first effectively deoxygenated and reduced and then conjugated with a polyalkylene oxide such as polyethylene glycol (PEG) under conditions which maintain the structural integrity of the heme oxygen binding site. In specific, preferred embodiments of the invention, the deoxygenation and reduction is performed under an inert atmosphere by the amino acid cysteine. In additional specific, preferred embodiments, the structural integrity of the heme oxygen binding site is maintained by a high anionic concentration in the reaction mixture. In further preferred specific emodiments of the invention, the polyalkylene oxide is polyethylene glycol; in still further preferred specific embodiments of the invention, the polyalkylene oxide is linked to hemoglobin via a urethane (carbamate) linkage.

Abstract: A compound of the formula ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group or hydrogenAA is an amino acid residue andX is H or a protecting group useful as a coupling agent in peptide synthesis.

Abstract: A novel, biologically active substance, poststatin, has been isolated from a culture medium of microorganism belonging to Streptomyces. The novel substance is a peptide compound having a novel structure, wherein the peptide chains have ketone radicals. Thus substance has a high endopeptidase inhibition activity. It is possible to chemically synthesize poststatin related compound having ketone radicals in the peptide chains. These compounds also have an endopeptidase inhibition activity.

Abstract: The invention relates to a process for the preparation of an oligopeptide or amino acid alkyl ester.HCl salt, the alkyl group being methyl, ethyl, isopropyl or n-propyl, by converting an oligopeptide.HCl salt or amino acid.HCl salt with an alkanol corresponding to the alkyl group under the influence of an acid catalyst, 0.01-0.5 mol HCl relative to the oligopeptide.HCl salt or amino acid.HCl salt in combination with an acid ion exchange resin being used as acid catalyst.

Abstract: The present invention relates to peptides from the three type I repeats of human endothelial cell thrombospondin, which bind to sulfated glycoconjugates including heparin and sulfatide. Such peptides are useful in glycoconjugate binding pharmaceutical compositions and in a method for binding glycoconjugates in a subject.

Abstract: Compositions of the invention include composites comprising a biomaterial carrying compounds with enhanced cell binding with respect to collagen. These composites are useful for soft and hard tissue repair or reconstruction. Suitable compounds with enhanced cell binding include synthetic peptides that mimic the conformation necessary for recognition and docketing of collagen binding species (such as cell surface receptors for collagen and fibronectin). Hydrogel matrices as the biomaterial promote cell attachment to the matrix and cell migration into the matrix.

Abstract: Disclosed are a novel physiologically active peptide having the following structural formula and an acid addition salt thereof: ##STR1## (where (1)/(2) and (3)/(4) are respectively bonded directly and each of the cysteine residues (Cys) at positions 6 and 22 forms an intramolecular S--S bond).This novel peptide derives from porcine and since it exhibits natriuretic and hypotensive actions, the peptide is useful as a therapeutic for cardiac edema, nephredema, hepatic edema, hypertension, congestive heart failure, acute and chronic renal insufficiency, etc. Further, exhibiting the capability of suppressing the growth of smooth vascular muscle cells and the cGMP producing activity, the novel peptide is anticipated to have the potential for serving as an effective therapeutic for atherosclerosis.

Abstract: The present invention provides a method for the selective cleavage of peptide amide bonds under ambient conditions by treating a peptide comprising the subunit --CO--NH--CH((CH.sub.2).sub.x SY)CONH-- wherein x is 1-2 and Y is H or (C.sub.1 -C.sub.4)alkyl in an aqueous medium with a tetracoordinate Pd(II) or tetracoordinate Pt(II) complex which promotes the hydrolysis of the adjacent amide bond proximal to the carboxy terminus of the subunit.

Abstract: Certain propionitrile compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described. A novel process for their preparation is also described.

Abstract: Novel inhibitors of retroviral protease, e.g., HIV protease, are provided which are peptides having from about 4 to about 8 amino acid residues and which are substrates for said protease derived from known cleavage sites and modified to contain an internal CH.sub.2 NH bond isostere.

Abstract: A peptide composed of 53 amino acid residues represented by the following amino acid sequence: (see SEQ ID NO: 1) ##STR1## and derivatives thereof represented by the following amino acid sequence: (see SEQ ID NO: 2) ##STR2## wherein X is as shown in the specification, are disclosed. These polypeptides are novel and have natriuretic and hypotensive actions.

Abstract: Peptide medicaments, and antibody thereto, useful for treating or preventing diseases, particularly diseases involving an inflammatory response by a host organism against infection, that are preferably derived from the .beta. subunit, CD18, of the leukocyte integrins, and that have the property of either interfering with, or preventing undesirable leukocyte adhesion to biological materials, particular to endothelial cells, or that interfere with, or prevent the chemotaxis of leukocytes through the endothelial cell monolayer, consequently minimizing undesirable cell/tissue leukocyte binding and thus preventing or minimizing diseases resulting therefrom.

Abstract: The present invention provides synthetic antiaggregatory agents for preventing inhibition of fibrinogen-platelet binding. These anti-aggregatory agents have the general formulas (1)-(5).H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --Cx (1)[Ri--C(O)--R--G--D--(AA.sub.j).sub.j --].sub.n --CX (2)Cy--[--AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.i --].sub.n --Z (3)H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --CZ--[--(AA.sub.k).sub.k --R--G--D--(AA.sub.l).sub.l --].sub.m --Z (4)[R.sub.1 --C(O)--R--G--D--(AA.sub.i).sub.i --].sub.n --CZ[--(AA.sub.j).sub.j ]--R--G--D--(AA.sub.k).sub.k --].sub.m --Z (5)in which: R=Arg; G=Gly; D=Asp; AA.sub.i, AA.sub.j, AA.sub.k and AA.sub.l = alpha-, beta- and omega-amino acid residues; (AA.sub.i).sub.i (AA.sub.j).sub.j =peptide chains having the same or different amino acid residues; (AA.sub.k).sub.k =peptide chains having the same or different amino acid residues; (AA.sub.l).sub.

Abstract: A novel peptide that exhibits a natriuretic action and a vasodepressor activity, and hence, that is applicable as a diagnostic reagent. The novel peptide is manufactured by the procedure of genetic engineering as well as by the methods of purification from chicken brains or by chemical synthesis.

Abstract: A novel peptide that exhibits a natriuretic action and a vasodepressor activity, and hence, that is applicable for a diagnostic reagent. The novel peptide is manufactured by tile procedure of genetic engineering as well as by the methods of purification from frog brains or by chemical synthesis.

Abstract: The invention relates to, novel peptide derivatives with the formula: R.sub.1 -A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -R.sub.2 or its salt, wherein R.sub.1 =H or a protective group, A.sub.1 =H, Ile, Leu or Val, A.sub.2 =Glu, Asp, Ser, Thr; A.sub.3 =Gly or Glyc; A.sub.4 =Arg or Lys; R.sub.2 =4-nitroaniline with the proviso that A.sub.3 is Gly when A.sub.4 is Lys and that A.sub.3 is Glyc when A.sub.4 is Arg. The invention also discloses the process for the preparation of the peptide derivatives, the method for the determination of the bacterial endotoxins by the use of the invented peptide derivatives and the use of these derivatives for determination of bacterial endotoxins.

Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.

Abstract: A new class of opioid receptor analogs is described based on an alanine substitution in the three position in the enkephalin analog DPDPE. The alanine-substituted analogs show increased selectivity for the delta type of opioid receptors over the mu type of receptors.