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

Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.

Abstract: A method of inhibiting a binding event between a target protein and a binding protein, comprising administering to a cell in vitro an effective amount of a non-naturally occurring bifunctional inhibitor molecule including (a) protein binding moiety, and (b) an effector region, wherein the protein binding moiety binds to a blocking protein, and wherein the effector region binds to the target protein in order to bind the target protein and the blocking protein and prevent access of the binding protein to the target protein. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.

Abstract: Described herein are peptide compositions of a prominin-1, which have regenerative activity. As such the peptides are useful when regeneration is needed, for example, to enhance angiogenesis, increase VEGF binding to endothelial cells, promote vasodilation, enhance cell migration, enhance cell proliferation, stimulate neuronal growth, prevent neurodegeneration, and/or promote neuroregeneration.

Abstract: Provided herein is a new class of cyclic lactadherin peptides (cLac) that mimic the natural phosphatidylserine (PS)-binding activity of the parent lactadherin protein. These cLacs are useful as small molecule indicators of early stage of apoptosis and of treatment efficacy evaluation.

Abstract: The present application provides, among other things, compounds, compositions and methods for treating various diseases including cancer.

Abstract: Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer), a lipid metabolism disorder, a billary disorder, cardiovascular disease, obesity or an endocrine disorder) by administering at least one agonist of guanalyte cyclase receptor either alone or in combination with a compound typically used to treat the disorder and or with an inhibitor of cGMP-dependent phosphodieasterases.

Abstract: An agent for treating heart failure, which improves left ventricular diastolic function itself without depending on the diuretic effect or vasodilation effect; controls the pathological condition of diastolic functional failure; and prevents the recurrence, and can prevent dyspnea and death from the pathological condition, is provided. By directly acting on a heart, 4-[(2-{(2R)-2-[(1E,3S)-4-(4-fluorophenyl)-3-hydroxy-1-buten-1-yl]-5-oxo-1-pyrrolidinyl}ethyl)thio]butanoic acid improves left ventricular diastolic function, and can effectively treat diastolic functional failure among heart failure types. Accordingly, by present invention, a new agent for treating heart failure that can relieve diastolic functional failure, for which no effective therapeutic method has been established, can be provided.

Abstract: Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [125I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.

Abstract: A cyclic organic compound which comprises 16 amino acids or 17 amino acids and has no carboxyl group C-terminally and/or no amino group N-terminally. Optionally, one of the amino acids is a nonnatural amino acid. The ring closure is formed between a side chain of one amino acid and the C-terminus of another amino acid, or the ring closure is effected with the aid of a nonnatural amino acid. A process for producing and using the compound for regulating vectorial ion channels, for treating diseases associated with the lung function and for treating oedemas is provided.

Abstract: The present invention provides a novel macrocyclic compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: The invention provides bipartite inhibitors of bacterial RNA polymerase that contain: (i) a first moiety that binds to the salinamide binding site of a bacterial RNA polymerase; (ii) a second moiety comprising a nucleoside analog; and (iii) a linker connecting said first and second moieties.

Abstract: The invention provides methods for treating a patient with constipation-predominant irritable bowel syndrome by administering a therapeutically effective dose of linaclotide.

Abstract: The present invention relates to methods of treating dry eye using ?-turn peptidomimetic cyclic compounds or derivatives thereof. The ?-turn peptidomimetic cyclic compounds can be used alone, in combination and/or in conjunction with one or more other compounds, molecules or drugs that treat dry eye.

Abstract: The invention provides RGD-containing cyclic peptidomimetics; conjugates of said peptidomimetics and a moiety of a payload selected from fluorescent probes, photosensitizers, chelating agents, or cytotoxic agents; and pharmaceutical compositions comprising these conjugates. The conjugates of the invention are useful both for diagnostic purposes and treatment of various diseases, disorders and conditions. More specifically, conjugates comprising fluorescent probes can be used for diagnostic purposes, e.g., visualization of organs and tissues, and diagnosis of tumors; conjugates comprising photosensitizers can be used for photodynamic therapy of both tumors and nonneoplastic tissues; conjugates comprising chelating agents can be used in radioimaging or radiotherapy; and conjugates comprising cytotoxic agents can be used for targeted chemotherapy.

Abstract: Polypeptides comprising variant vascular endothelial growth factor sequences are provided. The polypeptides are useful in cancer imaging, cancer diagnosis, monitoring and treatment as well as treatment of diseases characterized by excessive neovascularization.

Abstract: The CD40L/Mac-1 interaction is selectively targeted by small peptide inhibitors and/or antibodies and such peptides are used for the specific treatment of inflammation and atherogenesis. In particular, pharmaceutical compositions comprising a polypeptide having the amino acid sequence EQLKKSKTL and antibodies specifically binding to an epitope are disclosed.

Abstract: The present invention relates to substances and compositions thereof useful in the control of cancer stem cell persistence and concomitant tumor recurrence and/or control of tumor growth. In particular, the invention relates to substances and compositions useful in the treatment of cancers and/or tumors linked to cancer stem cells, preferably brain cancers and/or tumors, in a subject.

Abstract: Compounds of formula (IV) and pharmaceutical compositions comprising the same are described, wherein X1 and X2, R3, L, Ar1, p and Z have the values disclosed herein.

Abstract: The present disclosure provides novel solid CB-183,315 formulations which have improved chemical stability. The chemical stability of the solid CB-183,315 is dependent on the process by which the composition is made. Solid preparations of CB-183,315 can be prepared by the following method: (a) forming an aqueous solution of CB-183,315 and at least one sugar that (e.g., sucrose, trehalose or dextran) at a pH of 2-7, preferably pH 6 and (b) converting the aqueous solution to the solid preparation of CB-183,315 (e.g., via lyophilization or spray drying).

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, and A-B are defined herein, which are non-immunosuppresive, cyclophilin-binding, mPTP blockers and are therefore useful for the prevention or treatment of diseases or disorders such as HCV infection, stroke, multiple sclerosis, HBV infection, HPV infection, asthma, cancer, muscular dystrophy, sepsis, ischemia/reperfusion injury, and heart failure.

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

Abstract: The present invention relates to the treatment of vascular disease in a diabetic patient using a drug-eluting implantable medical device that releases everolimus from three distinctly loaded drug reservoir layers wherein at least one of the layers comprises at least 200 ?g/cm2 of everolimus and further wherein the everolimus is the only therapeutic agent in the layers or the layers or any combination thereof further comprise an anti-inflammatory agent or an RGD peptide or both.

Abstract: The present invention relates to a sustained-release drug composition consisting essentially of microparticles of a peptide as the active substance and a biocompatible water-soluble polymer, in particular peptide as meianocortin receptor ligand. The present invention relates also to an injection formulation comprising the sustained-release drug composition suspended in an injection medium.

Abstract: Embodiments of the present invention provide for novel peptides of use for detection and/or inhibition of anti-?1-adrenergic receptor antibodies. Certain embodiments concern uses of cyclic and/or linear peptides. In other embodiments, the present invention relates to novel peptides of use in diagnostic and/or pharmaceutical compositions. Some embodiments concern diagnosing and/or treating cardiac conditions. Cardiac conditions of the instant invention can concern infectious heart disease, non-infectious heart disease, ischemic heart disease, non-ischemic heart disease, inflammatory heart disease, myocarditis, cardiac dilatation, idiopathic cardiomyopathy, idiopathic dilated cardiomyopathy, immune-cardiomyopathy, heart failure, and any cardiac arrhythmia condition.

Abstract: ?-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis.

Abstract: The invention features targeted cytotoxic compounds and methods relating to their therapeutic use for the treatment of neoplasia and other conditions.

Abstract: A method and formulation for preparing spray dried vancomycin. In various embodiment, the formulation includes vancomycin HC1 (10-20%) and one or more of the following PEG (0-5%), mannitol (0-5%), ethanol (0-10%), and a citrate buffer. Spray dried vancomycin has favorable reconstitution times and water content.

Abstract: Disclosed are compounds and methods relating to a chemical transformation for the conjugation of unprotected peptide biomolecules via a SNAr process between highly fluorinated aryl moieties and thiols (“fluoroaryl-thiol-click”).

Abstract: Novel urotensin ll receptor (UT) agonists and antagonists are described herein. More specifically, novel derivatives of urotensin ll-related peptide (URP) are described herein.

Abstract: The present invention provides extracts of material fermented with Paenibacillus sp., preferably the one called here Paenibacillus elgii ourofinensis with antimicrobial activity and/or growth promoter in animals intended for slaughter for human consumption. The invention provides new peptides derived from the fractions of the fermentation of Paenibacillus elgii ourofinensis extract, said new peptides having antimicrobial activity and promoting the growth of organisms, for example, plants and animals. The invention is also related to the use of the extract of this new strain, Paenibacillus elgii ourofinensis, as a growth promoter and as an antimicrobial agent in the treatment and prophylaxis of animals intended for human consumption.

Abstract: The present invention relates to a biodegradable, inhalable microparticle formulation comprising a compound of formula I obtained by fermentation of a microorganism of the Streptomyces species (PM0626271/MTCC5447), as described in PCT application publication WO2011027290, and a biodegradable lipid for drug delivery wherein the ratio of drug (compound of formula I) to lipid is 1:15 to 1:25. The present invention also relates to the process for preparation of the formulation and to the method of treatment of pulmonary tuberculosis, multi drug resistant tuberculosis (MDRTB), methicillin resistant Staphylococcus aureus (MRSA) pneumonias and methicillin sensitive Staphylococcus aureus (MSSA) pneumonias by administering therapeutically effective amount of the formulation to a mammal in need thereof.

Abstract: The present invention provides a titratable transdermal drug delivery system comprising an effective dose of an antithrombotic agent, such as tirofiban, or a pharmaceutically acceptable salt thereof. The dosage of the drug delivered is proportional to the size of the patch applied and achieves 60-85% platelet inhibition. The system enables and individualized treatment for patients. Also provided are methods for the treatment of various disorders where platelet inhibition is desired.

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.

Abstract: The invention relates to a pharmaceutical composition comprising a HDAC inhibitor, a pharmaceutically acceptable acid or a salt thereof or a mixture thereof and a steroid or a pharmaceutically acceptable salt thereof as well use of said pharmaceutical composition for the treatment of cancer as a pretreatment prior to other treatments. Said HDAC inhibitor or steroid may alternatively be administrated separately prior to additional treatments.

Abstract: Provided herein are inventive enopeptin compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Further provided are methods of preparation, use, and treatment.

Abstract: The invention relates to novel pharmaceutically-useful peptides, in particular cyclic peptides that are agonists of the AngII type 2 receptor (AT2 receptor). The invention further relates to the use of such peptides as medicaments, to pharmaceutical compositions containing them, and to their production.

Abstract: The present invention is related to new peptide antagonists of ?v?3 receptor, designed on the basis of the crystal structure of integrin ?v?3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the ?v?3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for ?v?3-targeted therapy and imaging.

Abstract: The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives.

Abstract: The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein, using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.

Abstract: Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Abstract: The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against Clostridium difficile.

Abstract: A nasal delivery device for and method of delivering a substance, preferably comprising oxytocin, non-peptide agonists thereof and antagonists thereof, preferably as one of a liquid, as a suspension or solution, or a powder to the nasal airway of a subject, preferably the posterior region of the nasal airway, and preferably the upper posterior region of the nasal airway which includes the olfactory bulb and the trigeminal nerve, and preferably in the treatment of neurological conditions and disorders.

Abstract: Compositions and methods for treating wounds are provided. The compositions include cyclic analogues of histatin (5).

Abstract: The present invention describes the use of translation inhibitors for the treatment of cancer and other disorders. Described herein are translation-inhibiting compounds, and methods of using those compounds for the treatment of cancer and other disorders. In some aspects the compounds inhibit translation elongation at the ribosome. In some aspects the compounds are used alone or in combination with known therapies.

Abstract: Cross-linked proteins and peptides, and methods of making and uses of such cross-linked proteins and peptides. The cross-linked proteins and peptides have rigid, distance-matching bismethylene aryl cross-linking moieties. Compositions comprising the cross-linked proteins and peptides can be used as pharmaceutical delivery formulations. The cross-linked proteins and peptides can have improved properties, such as cell permeability, as compared to the parent protein or peptide.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.