Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.

Abstract: Tryptophan derivatives substituted by a hydrophobic group, e.g. carbobenzoxy, at the N-terminus, and a hydrophilic group, e.g. --COOH, --SO.sub.3 H or --PO.sub.3 H, at the C-terminus, were found to be cell-permeable blockers of protein tyrosine kinases (PTKs). These PTK blockers are useful in basic research and in the treatment of neoplastic diseases.

Abstract: A method for screening or detection of a non-enzyme catalytic polypeptide or protein for the conversion of a substrate S to a product P is provided, in which a preparation containing the potential catalyst is contacted with the substrate S immobilized to a support and the immobilized product P obtained is detected, preferably by immunoassay. The method is preferably used for the screening of hybridoma supernatants for catalytic monoclonal antibodies that catalyze acyl transfer reactions, e.g., hydrolysis or aminolysis, condensation reactions and resolution of enantiomers.

Abstract: Pharmaceutical preparations for controlling proliferation of ectodermally-derived tissues comprising the specific negative growth factor activin A or an agonist thereof, and their use in methods of treatment of proliferative conditions and wound repair.

Abstract: The invention relates to an expression vector, the nucleic acid sequence of which comprises a promoter that is capable of controlling, when the vector is in a bacterial host and the temperature is lowered to below about 20.degree. C., the production of recombinant peptide or protein encoded by a gene contained within the vector. The invention also relates to host cells containing the vectors and to a method of producing a recombinant protein.

Abstract: The present invention is directed to conotoxin peptides having 25-35 amino acids, six cysteines which form three disulfide bonds between the first and fourth, second and fifth, and third and sixth cysteines, respectively. The invention is directed to .delta.-conotoxin GmVIA having the formula Val-Lys-Pro-Cys-Arg-Lys-Glu-Gly-Gln-Leu-Cys-Asp-Pro-Ile-Phe-Gln-Asn-Cys-Cy s-Arg-Gly-Trp-Asn-Cys-Val-Leu-Phe-Cys-Val (SEQ ID NO:1). This peptide activates sodium channels. The invention is further directed to .mu.O-conotoxin peptides of the generic formula Ala-Cys-Xaa.sub.1 -Lys-Lys-Trp-Glu-Tyr-Cys-Ile-Val-Pro-Ile-Xaa.sub.2 -Gly-Phe-Xaa.sub.3 -Tyr-Cys-Cys-Pro-Gly-Leu-Ile-Cys-Gly-Pro-Phe-Val-Cys-Val, wherein Xaa.sub.1 is Arg or Ser, Xaa.sub.2 is Ile or Leu and Xaa.sub.3 is Ile or Val (SEQ ID NO:2). These peptides block sodium charmels. Examples of .mu.

Abstract: The invention provides a dry, disposable, polymeric product having sustained-release anti-microbial activity, the product consisting essentially of a polymeric material selected from the group consisting of fibers, fabrics, sheets, films and other stable woven, non-woven and knitted materials prepared from natural, man-made and synthetic polymers and an amine salt anti-microbial agent, the anti-microbial agent being incorporated in the polymeric material without an intermediary adhesive, carrier or linking agent and being releasable therefrom in anti-microbially effective amounts for a period of at least three days upon the product being brought into contact with a moist surface.

Abstract: A method for preparing mimics of a wide variety of drugs and other biologically active molecules using molecular imprinting techniques, and the mimics produced thereby, is disclosed. Specifically, the mimic is designed by: (i) polymerization of functional monomers around a known drug or biologically active molecule (the template) that exhibits a desired activity; (ii) removal of the template molecule; and then (iii) polymerization of a second class of monomers in the void left by the template, to provide a new organic molecule which exhibits one or more desired properties which are similar to that of the template.

Abstract: The invention provides a method for the rapid detection of biotoxic contaants in a test material comprising combining a sample of the test material with activated spores essentially devoid of detectable enzymatic activity, which activity becomes manifest and increases measurably following germination of the spores and with at least one germinant capable of triggering germination of the spores and a substrate which is catalytically convertible to a product by the enzymatic activity, incubating the mixture for a period of less than one hour to accelarate germination of the spores, increase of the enzyme activity, and a catalytic conversion of the substrate, and detecting the formation of the product of the catalytic conversion of the substrate and the enzyme, the level of the product being maximal in the absence of any biotoxic contaminants, and decreasing in direct proportion to the toxicity of contaminants in the test sample.

Abstract: Genetically engineered human acetylcholinesterase and antibodies that def the protein are described. These composition may be used in pharmaceutical preparations for treatment and prophylaxis of organo-phosphorous compound poisoning or post-operative apnea. Also described are human cholinesterase DNA probes which may be employed for diagnosing progressing ovarian carcinomas and hemocytopoietic disorders.

Abstract: A method for the biological control of pollen in plants, including the thinning of fruits, reducing seeds in citrus plants and reducing the incidence of shotberries in grapes, by applying an effective amount of activated or inactivated RNase or mixtures of these to the flowers of the plants.

Abstract: A colonic delivery system for delivering a drug to the colon is provided. The system comprises a drug in combination with a matrix, wherein the matrix comprises a saccharide-containing polymer. According to the invention, the matrix is resistant to chemical and enzymatic degradation in the stomach and small intestine. The matrix is degraded in the colon by bacterial enzymatic action, and the drug is released. The system is useful for targeting drugs to the colon in order to treat colonic disease. The system is also useful for enteric administration of drugs such as proteins and peptides which are otherwise degraded in the stomach and small intestine.

Abstract: A monomeric diacid derivative includes at least two fatty acids coupled by hydrolytically or enzymatically degradable bond. In a biological environment, the bond degrades forming naturally occurring fatty acid products thereby allowing elimination.

Abstract: A monomeric diacid derivative includes at least two fatty acids coupled by a hydrolytically or enzymatically degradable bond. In a biological environment, the bond degrades forming naturally occurring fatty acid products thereby allowing elimination.

Abstract: Pharmaceutical compositions comprising compounds of the formula: R.sup.2 C{CH.sub.2 O(CH.sub.2).sub.n CO[NR.sup.3 CHR(CH.sub.2).sub.m CO].sub.q NOHR.sup.1 }.sub.3, wherein R is hydrogen, alkyl optionally substituted by OR.sup.5, SR.sup.5, NR.sup.5 R.sup.6, COR.sup.6, COOR.sup.6, CONR.sup.5 R.sup.6, --NHC(NR.sup.5 R.sup.6).dbd.NR.sup.7, aryl, aralkyl or heteroaryl; R.sup.1, R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen, alkyl, aralkyl, aryl, COOR.sup.4, CONHR.sup.4 and CONR.sup.4 R.sup.4 ; R.sup.2 may additionally be alkyl substituted by alkoxy, alkenyloxy or by a group --O--(CH.sub.2).sub.p --COOX or --O--(CH.sub.2).sub.p --CONHX, wherein p is an integer from 1 to 10 and X is alkyl, aralkyl, aryl or heteroaryl; R.sup.4, R.sup.5 and R.sup.6 are hydrogen, alkyl, aralkyl, aryl or heteroaryl; n is 1 or 2, m is 0, 1 or 2 and q is 0 or 1, and when m is 0, the moiety --NR.sup.

Abstract: Pharmaceutical preparations for the treatment of hyperproliferative epidermal conditions comprising the specific negative growth factor activin A, and their use in methods of treatment of hyperproliferative epidermal conditions.

Abstract: The invention relates to novel (3S,4S)-7-hydroxy-.DELTA..sup.6 -tetrahydrocannabinol homologes and derivatives, essentially free of the (3R,4R) form and to pharmaceutical compositions which have a potent analgetic, antiemetic and antiglaucoma effect, which compositions contain an effective dosage of a compound of this type. The novel pharmaceutical compositions are practically devoid of the undesired side effects of the (3R,4R) type compounds, such as cannabimimetic psychotropic effects. The pharmaceutical compositions are of special utility in cases of acute and of chronic pain. The invention also relates to a process for the production of the above defined novel compounds.

Abstract: A biological control agent comprising the mycoparasite Trichoderma harzia T-315 (ATCC No. 20671), which is characterized by fungicidal activity against fungi of the genera Pythium, Phizoctonia, Sclerotium and Fusarium. This strain is useful for controlling damping-off, root-rot, crown-rot and neck-rot in seedling crops. This strain is also resistant to chemical pesticides and soil-sterilants and useful for integrated biological and chemical control of soil-borne pathogens.

Abstract: The present method and apparatus produces undistorted x-ray images of sources emitting x-rays and especially of certain areas emitting x-rays. Stigmatic monochromatic x-ray images, and x-ray spectra with a spatial resolution along the lines of the spectrum are produced. The device comprises, in combination, an x-ray diffraction crystal capable of simultaneous reflection, and an x-ray point intensity measuring system, the arrangement being such that the reflection plane of the crystal makes an angle with the plane of the intensity measurement system of 90 degrees of angle minus the Bragg angle for a forbidden reflection of the crystal, and where the x-ray radiation incident on the crystal makes a Bragg angle with the plane of the forbidden reflection, the azimuthal arrangement allowing simultaneous reflection.