Abstract: The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other conditions.

Abstract: The invention provides a method for preventing or treating a disease caused by an extracellular microorganism, said method comprising systemically administering to a subject in need thereof a prophylactically or therapeutically effective amount of a salicylic acid (SAL) or a SAL analogue. The extracellular microorganism can be of the bacterial genus Staphylococcus, for example, Staphylococcus aureus. The extracellular microorganism can be a strain that is resistant to at least one antibiotic. The strain can be selected from the group consisting of methycillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate Staphylococcus aureus (VISA) and vancomycin-resistant Staphylococcus aureus (VRSA).

Abstract: The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.

Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.

Abstract: An activatable functionalised Nth generation dendrimer having: a core comprising a first monomer having at least two carboxylic acid functional groups; and N successive generations, where N=0 to 10, wherein each generation comprises: a second monomer having at least two alcohol functional groups, wherein at least one alcohol group is bonded to a carboxylic acid group of the first monomer of the prior generation, and an additional first monomer attached to a second alcohol function group of said second monomer of that generation; and the final generation having attached thereto at said second alcohol functional group of said second monomer, a moiety having a dicarboxylic acid functional group, activatable by treatment with a carboxylic acid activating reagent such that reactivity of the carboxylic acid functional group is increased. The dendrimer, when activated, may be used in applications such as polymer crosslinking and/or nanoshell production.

Abstract: Described herein are peptides, compositions, and related methods for treating upper gastrointestinal disorders and conditions (e.g., dyspepsia, gastroparesis, post-operative gastric ileus, a functional esophageal disorder, a functional gastroduodenal disorder, gastroesophageal reflux disease (GERD), or a duodenal or stomach ulcer) as well as other conditions and disorders that are described herein.

Abstract: The present application relates to novel derivatives of monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and also to the use of these derivatives for preparing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as, for example, cancerous disorders. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.

Abstract: The invention provides compounds of the formula Poly-([SP-LI]n-PL-L2) including a collection of 152 peptides useful to create the compounds, and their uses thereof for the treatment of a variety of mammalian diseases. The compound, a novel ligand-targeted multi-stereoisomer peptide polymer conjugate, comprises two or more stereoisomer peptides and a peptide-ligand conjugated via linkers to a biocompatible hydrophilic polymer, preferably HPMA. The increased stability and solubility of the compound carrying the stereoisomer peptides and a peptide-ligand provide ideal pharmaceutical properties including the delivery by the polymer of the peptides into the target cells. The compounds of the invention are useful therapeutics for the treatment of a variety of mammalian diseases.

Abstract: C-terminal endostatin polypeptides are disclosed herein. Polynucleotides encoding these polypeptide, host cells transformed with the polynucleotides, and methods of using these polypeptides and polynucleotides are disclosed. Uses of these polypeptide, polynucleotides and expression vectors include the treatment of fibrosis in a subject. Thus, methods are provided for treating fibrosis, including fibrosis of the skin and/or the lung.

Abstract: Enediyne compounds having a structure according to formula (I), where R0, R2, R3, R4, R5, R6, and R7 are defined herein, can be used in chemotherapeutic drugs, especially in conjugates, for the treatment of diseases such as cancer.

Abstract: A compound comprising a peptide moiety comprising, consisting essentially of, or consisting of, the peptide sequence of a tyrosine cluster YC of the BY-kinase of a Gram positive or Gram negative bacteria, or a fragment or an analogue thereof, and an adenine peptide analogue PNA(A), whereas the peptide moiety and the PNA are linked together. The compound is useful as an inhibitor of bacterial tyrosine kinase.

Abstract: The present application provides biligand and triligand protein-catalyzed capture (PCC) agents that specifically bind VEGF, as well as the use of these capture agents as detection, diagnosis, and treatment agents.

Abstract: Methods for concentrating microorganisms in a liquid sample or depleting microorganisms therefrom, utilizing polymeric compounds having affinity to microbial cells that are composed of a plurality of positively charged amino acid residues and two or more hydrophobic moieties are disclosed. Also disclosed are devices for concentrating and methods for detection and identification microorganisms in a liquid sample.

Abstract: The invention relates to compositions that comprise dendrimers useful in medical and veterinary applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the dendrimer through a linkage that releases the drug or a prodrug through controlled beta elimination.

Abstract: Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.

Abstract: The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof. The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.

Abstract: Provided are human serum albumin (HSA) compositions with improved properties over native HSA.

Abstract: A method of treating a disease characterized by aberrant cell migration and/or invasion includes administering to a subject an effective amount of the peptide of SEQ ID NO:3, an ?6 polypeptide, or an isolated polypeptide consisting essentially of the Link region of human CD44 as indicated in FIG. 17 to modulate a FAK signal transduction pathway for a sufficient period of time to treat the disease. A method of diagnosing a condition characterized by aberrant cell migration and/or invasion includes measuring the effect of these polypeptides on FAK signal transduction activity; wherein a change in FAK signal transduction activity is indicative of said aberrant cell migration or invasion. A method of diagnosing a condition characterized by aberrant cell migration and/or invasion includes imaging FAK signal transduction activity in the presence of these polypeptides.

Abstract: Peptides may be produced by using (A) a first amino acid or peptide, which is converted into its ionic liquid form through the formation of an ionic bond, as a substance serving as both a reaction solvent and a reaction starting material; and reacting the first amino acid or peptide with (B) an ester of second amino acid or peptide, in the absence of any peptide hydrolase or any condensation agent, in the presence of water in an amount of not more than 20% by mass relative to the total mass of the reaction system to form a peptide bond between the first amino acid or peptide and the second amino acid or peptide. By means of this process, it is possible to synthesize a peptide at a high concentration and at a high yield, and this method is excellent for producing peptides on an industrial scale.

Abstract: The present application describes a method of treating a bacterial infection comprising administering to a subject in need thereof a pharmaceutically acceptable amount of a defined macrocycle compound.