Abstract: Compounds and compositions comprising fragments and synthetic analogs of human thrombospondin are provided together with methods for their use as thrombospondin-like agents.

Abstract: The present invention pertains to modified bradykinin antagonist peptides of the formula X-A.sup.0 -B.sup.1 -C.sup.2 -D.sup.3 -E.sup.4 -F.sup.5 -G.sup.6 -H.sup.7 -J.sup.8 -K.sup.9, where at least one of F.sup.5, H.sup.7 and J.sup.8 is an indane substituted amino acids.

Abstract: The peptide HITWDQLWNVMN (SEQ ID NO: 4) and related peptides and peptidomimetics bind to endothelial leukocyte adhesion molecule 1 and block the binding of leukocytes to this important receptor and so can be used to ameliorate the detrimental effects of certain disease conditions.

Abstract: A cyclosporin of the formula ##STR1## wherein A is a residue of the formula ##STR2## wherein R is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or C.sub.1-3 alkylthio; halo-substituted-C.sub.1-3 alkyl, -C.sub.1-3 alkoxy or -C.sub.1-3 alkylthio; hydroxy-substituted-C.sub.1-3 alkyl, -C.sub.2-3 alkoxy or -C.sub.2-3 alkylthio; or amino or mono- or di-(C.sub.1-2 alkyl)-amino,X is oxygen or sulphur,--x--y-- is --CH.dbd.CH-- (trans) or --CH.sub.2 --CH.sub.2 --,B is -.alpha.Abu-, -Val-, -Thr- or -Nva- andQ is -(D)Ala-; -(D)Ser-; -[O-(2-hydroxyethyl)(D)Ser]-; or -[O-acyl(D)Ser]- or -[O-(2-acyloxy ethyl)(D)Ser]-in which the acyl residue is physiologically hydrolysable and acceptable, are useful in the topical treatment of asthma.

Abstract: Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 .alpha.-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein the substituents have various significances, are disclosed. They can be prepared by isolation or derivation from an appropriate microorganism strain such as S 42508/F (NRRL 15761).They have interesting pharmacological, e.g. antifungal, chemotherapeutic drug resistance reversing and to some extent immunosuppressant and antiinflammatory properties.

Abstract: This invention relates to compounds of the formula: ##STR1## wherein: A' is absent, Asn, Gln, Ala or Abu;A is absent or a D- or L-amino acid chosen from Arg, HArg, (Me.sub.2)Arg, (Et.sub.2)Arg, Abu, Ala, Gly, His, Lys, or an .alpha.-R' substituted derivative thereof, Dtc, Tpr and Pro;B is a D- or L-amino acid chosen from Arg, HArg, NArg, (Me.sub.2)Arg, (Et.sub.2)Arg and Lys or an .alpha.-R' substituted derivative thereof;Q is absent or a D or L amino acid chosen from Tyr, (Alk)Tyr, Phe, (4'W)Phe, HPhe, Phg, Pro, Trp, His, Ser, (Alk)Ser, Thr, (Alk)Thr, (Alk)Cys, (Alk)Pen, Ala, Val, Nva, Met, Leu, Ile, Nle and Nal, or an .alpha.-R' substituted derivative thereof;M is absent or Gly or a D- or L-amino acid chosen from Glu, Phe, Pro, Lys and Ser or, provided n is 1, B-Gly-Glu-Q;W is halogen or Alk;R' is Alk or PhCH.sub.2 ; ##STR2## wherein Z.sub.1 and Z.sub.2 are linked via a covalent bond between L.sup.1 and L.sup.2 ; or Z.sub.1 and Z.sub.

Abstract: Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking adhesion of leukocytes to the selectins for the purpose of inhibiting inflammation as well as in diagnostic methods employing labeled peptides and peptide mimetics that bind selectins for the purpose of determining the site of inflammation in mammals which inflammation is mediated by the presence of one or more selectins.

Abstract: A composition designed for the sustained and controlled release of medicamentous peptide substances having the formula (I):Ac-D-Nal-D-pClPhe-R.sup.3 -Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH.sub.2wherein R.sup.3 is D-Pal or D-Trp. The composition is obtained in the form of microspheres of a biodegradable polymeric material incorporating a water-insoluble salt of the peptide of formula (I).

Abstract: Disclosed is a peptide compound represented by the following formula (I):R.sup.1 -R.sup.2 -R.sup.3 -R.sup.4 -R.sup.5 -R.sup.6 -R.sup.7 -R.sup.8 -R.sup.9 -R.sup.10 -R.sup.11 -R.sup.12 -Phe-R.sup.14 -R.sup.15 -R.sup.16 -R.sup.17 -R.sup.18 -Ile-R.sup.20 -Z SEQ. ID NO. 64, (I)wherein R.sup.1-12, R.sup.14-18, and R.sup.20 are as defined in the specification.

Abstract: Analogues of cholecystokinin-8, which are receptor selective, vary from the normal hormone by alteration of at least one of the two, three or six position amino acids of the natural sequence.

Abstract: Peptides having high binding activity for human interleukin-1 and represented by the following formulaH-X.sup.1 -Cys-A-B-A-B-A-Ser-X.sup.2 -Ywherein each A represents an amino acid residue selected from the group consisting of Val, Leu, Ile and Nle, independent of any other selection for A; B represents an amino acid residue selected from the group consisting of Arg, Lys, Gln, His and Ser, independent of any other selection for B; X.sup.1 and X.sup.2 each is a single bond or a peptide segment comprising 1-10 amino acid residues selected from Gly, Ala, Val, Arg, Asn, Ser, Phe, Pro, Leu, Glu, Asp, Lys, Thr, His, Tyr, Nle and Ile and Y represents a hydroxyl group or an amino group; and their salts.

Abstract: Disclosed are (1) a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof:His-Ser-Asp-Gly-Ile-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-NH-CHX-CO-A la-Val-Lys-Lys-Tyr-Y SEQ ID NO: 13 (I)wherein X is hydrogen atom; or a lower alkyl group which may be substituted with a member selected from the group consisting of hydroxy group, substituted or unsubstituted amino group, carboxyl group, carbamoyl group, and substituted or unsubstituted aromatic group; and Y is one of amino acids or peptides consisting of 1 to 16 amino acid residues counted from the N-terminal side of Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys SEQ ID NO: 20, and (2) a pharmaceutical composition comprising a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof, which has remarkable c-AMP activity and is useful as a nerve activating agent.

Abstract: The present invention provides polypeptides of the formula XX.sup.1 TrpX.sup.2 X.sup.3 X.sup.4 X.sup.5 X.sup.6 X.sup.7 NH.sub.2, methods of treatment using the polypeptides, pharmaceutical compositions comprising such polypeptides, and processes for their preparation. The polypeptides possess antagonist properties against bombesin and bombesin-like peptides and are useful in the treatment of malignant disease. M, X, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, and X.sup.7 are as defined in the specification.

Abstract: Bombesin is an amphibian peptide that has a structure closely related to that of several mammalian peptides, including Gastrin Releasing Peptide (GRP) and Neuromedins B and C. Bombesin, GRP and related peptides exert their in vivo effects by binding to specific receptors present on cells of the gastrointestinal tract, the central nervous system, and tumors. The invention relates to novel bombesin derivatives which act as bombesin receptor antagonists by blocking the binding of bombesin, GRP or related peptides to cellular receptors. By blocking the binding of bombesin, GRP and related peptides to cellular receptors on cancer cells, these antagonists inhibit the growth of tumor cells that respond to the growth-promoting action of bombesin. These antagonists are expected to block the binding of bombesin, GRP or related peptides to similar receptors on cells in the gastrointestinal tract or the central nervous system.

Abstract: A peptide represented by the formula: ##STR1## wherein R.sub.1 represents an oil-soluble group; R.sub.2 and R.sub.5 represent a hydrogen atom or a lower alkyl group; R.sub.3 represents an aliphatic group which may have O or S; R.sub.4 represents a heterocyclic-substituted lower alkyl group; R.sub.6 represents a hydrogen atom, a lower alkyl group or an aromatic cyclic group; X represents a group having an aromatic ring; n represents an integer of 0 or more and m represents an integer of 2 or more, or a salt thereof exhibits a marked endothelin receptor-antagonistic action, and the peptide [I] is pharmaceutically useful as a therapeutic agent for hypertension, cardiovascular disease and renal disease, for instance.

Abstract: The invention relates to preparation of selected peptides of the HIV gag protein and derivatives thereof which comprise the peptide sequence NPGLLETSEGCRQ, and which inhibit HIV.

Abstract: The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.

Abstract: The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.

Abstract: Peptide derivatives with inhibitory activity on the enzyme systems involved in the oxidative burst of human phagocytic cells comprise six and seven amino acid peptide sequences from human cytochrome b.sub.558. The derivatives may be used in medicaments for the treatment of inflammatory diseases.

Abstract: A method for treating acute or chronic inflammatory or autoimmune disorders using polypeptides with fibronectin or related activity is provided. The method involves (administering an amount of) one or more polypeptides corresponding to isolated amino acid residue sequences of the 33 kD carboxy terminal heparin-binding region located on the A chain of fibronectin to effectively suppress inflammation and impairment of tissue function in a patient.