Abstract: The present invention relates to cyclic peptides mimetics of the C-terminal binding domain of TSP-1. The present invention also relates to the use of these cyclic peptides as agonists of CD47 and their ability to trigger programmed cell death (PCD). The present invention further relate to a pharmaceutical composition for use in the treatment of diseases associated with defects in PCD such as cancers and immunological disorders (including chronic inflammation) and comprising at least one cyclic peptide according to the invention.

Abstract: A construct composed of a Kinesin-derived Angiogenesis Inhibitor peptide and one or more carrier moieties and/or stabilizing moieties is provided as are methods for inhibiting angiogenesis and treating a disease or condition characterized by excessive vascularity.

Abstract: Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.

Abstract: The present invention relates to the use of a cyclic peptide comprising the tripeptide reproducing a binding site of fertilin beta to the oocyte integrin, for improving cellular energy metabolism. More particularly, the invention concerns the use of a cyclic peptide comprising the tripeptide FEEc for stimulating the energy metabolism of gametes or embryonic cells in the context of medically assisted procreation (MAP) protocols, in particular promoting the in vitro maturation of the oocyte, the fertilization rate and the birth rate.

Abstract: Provided are a newly developed norbornene-based amphiphilic compound, a method for preparing the same, and a method for extracting, solubilizing, stabilizing, crystallizing or analyzing a membrane protein using the same. In addition, the compound may effectively extract membrane proteins having various structures and characteristics, compared to a conventional compound, from cell membranes, and may be stably stored in an aqueous solution for a long period of time, and therefore may be used in their functional analysis and structural analysis. The structural and functional analyses of membrane proteins are the most noticeable field in biology and chemistry today due to a close relationship to the development of new drugs.

Abstract: The invention provides materials and methods for the treatment of obesity and excess weight, diabetes, and other associated metabolic disorders. In particular, the invention provides novel acylated glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.

Abstract: Methods for extracting metabolites from mushroom comprising dispersing a sample of the mushroom; contacting the sample with a first solvent system at a temperature of 80° C. or greater to extract at least a first portion of metabolites from the sample; and contacting the sample with a second solvent system at a temperature of 80° C. or greater to extract at least a second portion of metabolites from the sample, wherein the combined first portion of metabolites and the second portion of metabolites include primary and secondary metabolites from the mushroom. A high-throughput process for establishing a metabolic profile of a mushroom, such as Amanita mushroom, can comprise extracting metabolites from mushroom and analyzing the extracted metabolites by automatic peak recognition or peak integration. Assay for identifying and/or assessing candidate metabolites extracted from Amanita mushroom are also disclosed.

Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.

Abstract: The present disclosure provides a method of treating muscle myopathy, including muscle dystrophies and cardiomyopathies, by administering stable, long-lasting vasoactive intestinal peptide therapeutic agents. These agents include one or more clastin-like peptides and can be administered at a low-dose.

Abstract: Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction.

Abstract: Disclosed are Somatostatin receptor ligands comprising a peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and an active agent moiety covalently bonded to the cyclic peptide moiety through a nitrogen atom of a side chain functional group of an internal residue of the cyclic peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and a nanoparticle active agent moiety covalently bonded to the cyclic peptide moiety, pharmaceutical compositions and uses thereof.

Abstract: The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of CD137. The invention also includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by CD137.

Abstract: Polypeptides having the ability to specifically form connections of glucosyl units in alpha 1,3 on an acceptor having at least one hydroxyl moiety are presented. The polypeptides include i) the pattern I of sequence SEQ ID NO: 1, ii) the pattern II of sequence SEQ ID NO: 2, iii) the pattern III of sequence SEQ ID NO: 3, and iv) the pattern IV of sequence SEQ ID NO: 4, or derivates from one or several of said patterns, wherein the polypeptide furthermore has an aspartic residue (D) at position 5 of the pattern II (SEQ ID NO: 2), a glutamic acid residue (E) at position 6 of the pattern III (SEQ ID NO: 3) an an aspartic acid residue (D) at position 6 of the pattern IV (SEQ ID NO: 4). Methods for producing acceptors connected to glucosyl units in alpha 1,3 using the polypeptides are also provided.

Abstract: Peptidyl IL-2R? ligands and compounds comprising the IL-2R? ligands are disclosed. The IL-2R? ligands and compounds such as synthetic monomers, homodimers, or heteromers and recombinant fusion proteins comprising the IL-2R? ligands can be used as targeting or imaging agents, as diagnostics or to treat cancers and autoimmune diseases.

Abstract: Described herein is a process for the total synthesis of macrolactones and macrolactams of formula I including E- and Z-configuration thereof, in particular, nannocystins.

Abstract: Provided are compositions that include an effective amount of a peptide or polypeptide derived from a Bordetella ACT AC domain, optionally wherein the peptide or polypeptide is 80-100% identical to an amino acid sequence as set forth in SEQ ID NOs: 1-5 and 44-53. Also provided are methods of using the same for preventing and/or treating a diseases, disorders, and conditions associated with the presence and/or development of biofilm; and for reducing the incidence of nosocomial infections; for inhibiting biofilm development and/or for reducing or eliminating biofilm present on medical, dental, and industrial surfaces.

Abstract: The peptides of the invention are of formula (I) or (IV). The peptides of the invention are useful in the treatment of cancer.

Abstract: The invention provides compositions and methods for the treatment or prevention of pain. Compositions provided are resistant to overdose and abuse. Compositions provided comprise two or more different molecules, where each molecule comprises at least one GI enzyme-labile opioid agonist releasing subunit comprising an opioid agonist that is covalently linked to at least one GI enzyme inhibitor subunit.

Abstract: Provided herein are compounds comprising peptides that bind Bfl-1. Also provided are compositions containing these peptides and methods of using such peptides in the treatment of cancer that include administering to a subject one of the peptides.

Abstract: A multi-branched drug conjugate of formula (I) or a pharmaceutically acceptable salt thereof. In the formula, R is an organic center, POLY is a polymer, L is a multivalent linker, T is a targeting molecule, D is an active agent, and q is any integer between 3 and 8. The symbol “*” in L represents a junction point of the multivalent linker L and the targeting molecule T, “#” represents a junction point of the multivalent linker L and the active agent D, and “%” represents a junction point of the multivalent linker L and POLY. 1 is any integer between 2 and 20, and m and n are each an integer between 0 and 10. T is iRGD, cRGD, tLyp-1, Lyp-1, RPARPAR, Angiopep2, or GE11. D is a camptothecin drug.