This invention is in the field of medicinal pharmacology. In particular, the invention relates to protease activated receptor type 2 (PAR2) modulating compounds (e.g., mimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment of conditions involving PAR2 activity.

The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.

Provided herein in aspects is an antibacterial combination comprising a thiopeptide antibiotic and an iron inhibitor. Methods of treatment and/or prevention of bacterial infections using the combination are also provided as well as methods of sensitizing a gram-negative bacteria to a thiopeptide antibiotic and methods of screening a molecule for antimicrobial activity.

Doxorubicin derivatives for targeted activation by Legumain, its preparation method and use. The doxorubicin derivatives are obtained by condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: ##STR00001##
compounds A and B have the following structures, respectively: ##STR00002##
wherein R.sub.3 in compound B is Leu or absent; R.sub.4 is any one amino acid selected from the group consisting of Ala and Thr; R.sub.5 is any one amino acid selected from the group consisting of Ala, Thr and Asn; R.sub.6 is ##STR00003##
wherein n=1-20; or ##STR00004##
wherein R.sub.7 is substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be used to prepare an anti-tumor drug.

Disclosed are geminoid peptide-like compound according to Formula I:

R.sup.1—C(═O)—Z.sub.n—NR.sup.3-R.sup.2  (I)

in which R.sup.1 and R.sup.2 are each independently saturated, partly saturated or unsaturated, straight, branched or cyclic alkyl chains, wherein R.sup.1 has a number of C atoms of 11 or more, preferably 11 to 19, and R.sup.2 has a number of C atoms of 12 or more, preferably 12 to 20; R.sup.3 is hydrogen or C.sub.1-C.sub.6 alkyl; n is an integer from 1-15;
each Z independently is an amino acid residue, wherein Z.sub.n comprises an N-terminus attached to C(═O) and a C-terminus that is attached to NR.sup.3, for use as a medicament.

The present invention relates to a functional 3D neuronal model based on ultrashort self-assembling peptide scaffolds in accordance with the present invention, and to a method of preparing such a model. The models are suitable for in vitro drug testing, cellular replacement therapies as well as other applications.

Novel compounds and methods for the inhibition of biological barrier permeability and for the inhibition of peptide translocation across biological barriers are identified. Assays for determining modulators of biological barrier permeability and for peptide translocation across biological barriers are provided. Methods for treating diseases relating to aberrant biological barrier permeability and peptide translocation across biological barriers are provided. Such diseases include celiac disease, necrotizing enterocolitis, diabetes, cancer, inflammatory bowel diseases, asthma, COPD, excessive or undesirable immune response, gluten sensitivity, gluten allergy, food allergy, rheumatoid arthritis, multiple sclerosis, immune-mediated or type 1 diabetes mellitus, systemic lupus erythematosus, psoriasis, scleroderma and autoimmune thyroid diseases.

Neuropeptide S receptor agonists are provided. The NPS agonists include trimeric, tetrameric, pentameric or hexameric peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The peptidomimetic molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling.

The disclosure pertains to methods of treating or preventing a disease or condition associated with and/or induced by soluble A-beta oligomer such as Alzheimer's disease by administering to a subject in need thereof conformation specific and/or selective antibodies or binding fragments thereof and related products.

Provided are a new polypeptide for repairing mucosal damage or a skin wound, and the use thereof. The polypeptide is not homologous with known polypeptides, can be stably present in vivo and in vitro, and has the effect of regulating stem cell proliferation and differentiation to repair mucosal damage or a skin wound. The present invention further relates to the use of the new polypeptide in the repairing of mucosal damage or a skin wound by means of regulating stem cell proliferation and differentiation, and the use thereof in the prevention, alleviation or treatment of gastrointestinal diseases.