Abstract: Provided are a peptide compound prepared by additional synthesis in a drug having an effect of inhibiting restenosis, a composition for inhibiting restenosis and promoting re-endothelialization including the peptide compound, and a stent having a surface coated by using the composition, in order to overcome a restenosis problem in the stent.

Abstract: Deubiquitinating enzyme (DUB) probes are provided that resemble native diubiquitin (diUB) with a similar linkage size and that may contain a Michael acceptor for trapping the DUB active-site cysteine. For example, both K63- and K48-linked diubiquitin probes are generated using a facile chemical ligation method, utilizing the linker compound 3-(2-(bromomethyl)-1,3-dioxolan-2-yl)prop-2-en-1-amine. The diUb probes are capable of labelling DUBs from different families and may be employed to reveal intrinsic linkage specificities of DUBs.

Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

Abstract: A method of treating Hodgkin's disease in a subject. The method involves administering to the subject an effective amount of a water-soluble composition which includes a cocrystal composition containing doxorubicin and a theanine enantiomer.

Abstract: Provided are a peptide compound prepared by additional synthesis in a drug having an effect of inhibiting restenosis, a composition for inhibiting restenosis and promoting re-endothelialization including the peptide compound, and a stent having a surface coated by using the composition, in order to overcome a restenosis problem in the stent.

Abstract: The present invention relates to a method or composition for treating diabetes mellitus, comprising administering a subject with a pharmaceutical composition comprising a therapeutically effective amount of an active compound from Antrodia camphorate, such as antroquinonols, and a pharmaceutically acceptable carrier. In addition, the prevent invention provides a new process for the total synthesis of antroquinonol. Also provided are the new compounds produced during the process for preparing of antroquinonol.

Abstract: Provided are a peptide compound prepared by additional synthesis in a drug having an effect of inhibiting restenosis, a composition for inhibiting restenosis and promoting re-endothelialization including the peptide compound, and a stent having a surface coated by using the composition, in order to overcome a restenosis problem in the stent.

Abstract: The invention provides methods to assess protein stability and to obtain sizing information. In one aspect, the screen comprises a 94 detergent panel and a series of MWCO filtered microplates. A protein of interest is bound to an affinity matrix and aliquoted into a 96-well microplate. Wells containing the immobilized protein are washed in the new detergent and then eluted in the new detergent into a collection plate. Protein not stable in the new detergent is precipitated on the resin and not present in the elutions. Half of the elution is passed through a high (i.e., 300 kDa) MWCO microplate and the other half through a low (i.e., 100 kDa) MWCO microplate. Elutions from the microplates are spotted on a nitrocellulose membrane, visualized by Western analysis (or by some other method), and quantified. The high MWCO provides stability readout and the ratio of low/high kDa provides sizing information.

Abstract: Aldehyde- and ketone-functionalized proteins are promising new substrates for the development of chemically modified biotherapeutics and protein-based materials. Their reactive carbonyl groups are typically conjugated with a-effect nucleophiles, such as substituted hydrazines and alkoxyamines, to generate hydrazones and oximes, respectively. However, the resulting C?N linkages are susceptible to hydrolysis under physiologically relevant conditions, which limits their utility in biological systems. Here we introduce a Pictet-Spengler ligation that is based on the classic Pictet-Spengler reaction of aldehydes and tryptamine nucleophiles. The ligation exploits the bioorthogonal reaction of aldehydes and alkoxyamines to form an intermediate oxyiminium ion; this intermediate undergoes intramolecular C—C bond formation with an indole nucleophile to form an oxacarboline product that is hydrolytically stable.

Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

Abstract: A method of making a water-soluble doxorubicin-theanine cocrystal composition. The method includes the steps of providing a quantity of doxorubicin, adding a quantity of a theanine enantiomer to the quantity of doxorubicin to form a mixture of the quantity of doxorubicin and the enantiomer of theanine, wetting the mixture, and grinding the mixture for a length of time sufficient to produce a dried crystalline mass.

Abstract: The present invention relates to peptidomimetics for reactivating p53. Methods of using the peptidomimetics are also disclosed.

Abstract: Disclosed is a family of intranasal spray dispensers for administering uniform low doses of desmopressin so as to achieve safe antidiuresis in human patients. The dispensers of the invention may be used in the treatment of nocturia, primary nocturnal enuresis, incontinence, urinary frequency, diabetes insipidus, or any disease or syndrome where desmopressin therapy is useful or where safe temporary suppression of urine production may lead to beneficial health effects or increased convenience in voiding control.

Abstract: Disclosed are two PTH analog ligands, SP-PTH-AAK and Aib-SP-PTH-AAK, that have long-acting activity at the PTH receptor, as demonstrated both in vitro and in vivo. These polypeptides are thus particularly useful in the treatment of diseases, such as hypoparathyroidism, in which long-acting activity is desired. The method of making the analog polypeptides is also disclosed.

Abstract: Polypeptides that bind to DC-SIGN and/or its homologues and methods for using such peptides for the treatment of various disorders are described. DC-SIGN and its homologues are receptors that bind IgG antibodies or Fc fragments and mediate intravenous immunoglobulin (IVIG)-related reversal of inflammation associated with various immune disorders.

Abstract: Antiviral protease inhibitors, including peptidyl aldehydes, peptidyl ?-ketoamides, peptidyl bisulfate salts, and peptidyl heterocycles, are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.

Abstract: Therapeutic compositions for treatment of protein serine/threonine phosphatase-related diseases are obtained by engineering amino acid sequences that disrupt interaction between the protein serine/threonine phosphatase and a protein inhibitor and are provided herein. Calcineurin and PPI are examples of protein serine/threonine phosphatases. RCAN1 is an inhibitor of calcineurin and is overexpressed in patients with serious diseases, such as Down syndrome and Alzheimer's disease. Molecules that bind RCAN1 at regions that interact with calcineurin selectively modulate functions of calcineurin to treat these diseases. Methods of treating a subject for a protein serine/threonine phosphatase-related disease by administering a molecule having an amino acid sequence selected from the group of SEQ ID NOs: 1-19 are further provided.

Abstract: There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing said compounds.

Abstract: The invention relates to curcumin derivatives having the formula I: wherein: Z represents: H3CO A represents —CH2—CH2— or —CH?CH—; L represents —C(O)—(NH)n1—R—(NH)n2—C(O)—; R represents a saturated or unsaturated, branched or unbranched hydrocarbyl chain having a minimum of 3 carbon atoms in the chain; wherein the maximum number of carbon atoms in the chain is 24; and wherein the carbon atoms of the chain can be replaced by at least one heteroatom, wherein the heteroatoms are independently —O— or —NH2—, with the proviso that each heteroatom is separated from each other heteroatom by at least two carbon atoms; n1 and n2 independently represent 0 or 1; and Y represents an antibody that binds specifically to a target antigen of a tumor cell. The invention further relates to methods of method of inhibiting the growth of tumors in a human by administering an effective amount of the curcumin derivative, and to methods of producing the curcumin derivative.

Abstract: The present application relates to novel fluorinated epoxyketone-based compounds, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions mediated by proteasome inhibition, in particular, the present application includes compounds of Formula I, and compositions and uses thereof.