Abstract: There is provided in the present application a pharmaceutically acceptable salt of a polypeptide and a pharmaceutical composition comprising the same, wherein the polypeptide comprises the amino acid sequence YEKLLDTEI (SEQ ID NO:1) or a functional variant thereof.

Abstract: A sample is dissolved in a reagent 4 containing an organic solvent in a conversion vessel 11. A gas is supplied from a first gas supply part into the conversion vessel 11 via a reagent introduction tube 17, and thus the interior of the conversion vessel 11 is pressurized. A gas is supplied from a second gas supply part into the reagent 4 in the conversion vessel 11 via a reagent discharge tube 18, and thus gas bubbles 41 are formed in the reagent 4.

Abstract: The present invention provides a method for preparing S-Bz-MAG3 as a precursor of contrast media. Thioglycolic acid and benzoyl chloride are taken for the thiol protection reaction. Next, N,N?-dicyclohexylcarbodiimide and N-hydroxysuccinimide are converted to corresponding ester compounds. The corresponding ester compounds then react with triglycine by amide bonding reaction. The product of the reaction is recrystallized using acetone, filtered, and finally flushed using flushing agent to give the final product. This is a bifunctional chelator and can be bridged with 99mTc and 186/188Re effectively and applied to nuclear medicine imaging and tumor radiotherapy. By taking advantage of fewer synthesis steps and ease of operations, complicated separation and purification reactions can be reduced and thus achieving highly productivity of S-Bz-MAG3.

Abstract: The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates) and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in PREVNAR®, SYNFLORIX® and/or PREVNAR 13®. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumoccocal infections using said novel immunogenic compositions.

Abstract: The present invention discloses recyclable polymeric catalyst of Formula I, for chlorination of organic acids and alcohols using chlorinating agents such as carbonyl chloride, oxalyl chloride or thionyl chloride, wherein, ‘m’ on the pendent groups on polystyrene backbone can have values from 1 to 5 and R is the alkyl group ranging from C1 to C5.

Abstract: An improved method for coupling carboxylic acids and amines is disclosed that includes the steps of combining a hyper-acid sensitive linker connecting an amine and a resin, a carboxylic acid, a carbodiimide, an activator additive, and a base, and carrying out the activation and coupling at a temperature greater than 30° C.

Abstract: The invention relates to a process for the preparation of a ketone of a general formula 1 with X being Cl or Br, in particular with X being Cl, with Y being F, Cl, Br, I or H, in particular with Y being F, comprising the steps of: activation of a carboxylic acid by using a peptide coupling agent, coupling of the activated carboxylic acid with a malonic acid derivative providing a ?-ketoester precursor and converting the ?-ketoester precursor to the ketone of the general formula 1.

Abstract: This invention relates pro-coagulant serpin molecules engineered by modification of the P4, P2, P1 and/or P1? residues within the reactive center loop (RCL) to display increased specificity for anticoagulant proteases. These modified serpin molecules may be useful in therapy, for example as pro-coagulants for the treatment of bleeding.

Abstract: The present invention relates to binding fusion protein compositions comprising targeting moieties linked to extended recombinant polypeptide (XTEN), binding fusion protein-drug conjugate compositions, and XTEN-drug conjugate compositions, isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of using such compositions in treatment of diseases, disorders, and conditions.

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

Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production. Macrocycles of the invention include triazole moieties that crosslink amino acid side chains. The cross links can stabilize a secondary structure of a peptidomimetic macrocycle, such as an ?-helix.

Abstract: Described is a method of fabricating biologically active, unnatural polypeptides. The method includes the steps of selecting a biologically active polypeptide or biologically active fragment thereof having an amino acid sequence comprising ?-amino acid residues, and fabricating a synthetic polypeptide that has an amino acid sequence that corresponds to the sequence of the biologically active polypeptide, but wherein about 14% to about 50% of the ?-amino acid residues found in the biologically active polypeptide or fragment of step (a) are replaced with ?-amino acid residues, and the ?-amino acid residues are distributed in a repeating pattern.

Abstract: A test kit for the quantitative determination of narcotic drugs comprising (A) series of sealed vessels, each vessel containing a deuterium free isotopologue of a narcotic drug in exactly defined concentrations and quantities, wherein the isotopologue differs from vessel to vessel and—wherein the quantities of the isotopologue differ from vessel to vessel or are the same for all vessels; and/or (B) series of sealed vessels, each vessel containing in exactly defined concentrations and quantities the same isotopologue in quantities which differ from vessel to vessel; wherein the free isotopologues are selected from narcotic drugs; prodrugs, salts, solvates, hydrates and polymorphs and contain at least three stable isotopes selected from the group consisting of 13C, 15N and 18O in the molecule with a degree of labeling of at least 95 mol-%; the use of the test kit and a method for quantitatively determining narcotic drugs.

Abstract: Some embodiments include a method in which a mixture of polynucleotide structures comprises a set of surface shapes. Surface shapes of some polynucleotide structures are complementary to surface shapes of other polynucleotide structures. The complementary surface shapes lock together along interfaces between adjacent polynucleotide structures to incorporate the polynucleotide structures into a polynucleotide mask. The polynucleotide mask is used during fabrication of features associated with a semiconductor substrate. Some embodiments include a method in which a semiconductor substrate comprises registration regions configured to adhere individual polynucleotide structures to specific locations of the semiconductor substrate. The adhered polynucleotide structures are incorporated into a polynucleotide mask which is used during fabrication of features associated with the semiconductor substrate.

Abstract: Disclosed are a carrier for use for separation purpose and a method for separation of a compound which enable a chemical reaction to be performed in a liquid phase, enable a compound of interest to be separated from the liquid phase after the completion of the reaction readily, enable the separated compound to be evaluated by structural analysis or the like while the compound being bound to the carrier, and enable the compound to be separated from the carrier readily. A carrier for separation which has a reaction site capable of reacting with other compound on a benzene ring, and a long-chain group having a specified carbon atom(s) at each of the ortho-position and the para-position of the reaction site through an oxygen atom.

Abstract: Disclosed herein are methods and compositions for correction and/or mutation of genes associated with Parkinson's Disease as well as clones and animals derived therefrom.

Abstract: The present invention relates to a method for preparing a cyclic peptide with antiparasite activity and anticancer activity. The invention also relates to this peptide as an antiparasite agent, for example in the treatment of toxoplasmosis and as an anticancer agent. The invention also relates to the use of this cyclic peptide for treating organs ex vivo before transplantation.

Abstract: The present invention relates to methods of preparing ?-turn cyclic peptidomimetic compounds and intermediates thereof. Particularly, the present invention relates to a process for the synthesis of ?-turn cyclic peptidomimetic compounds of formula I: where R1, R2, R3, R4, R5, R6, R7, L2, X, Y and n are as defined in the specification. The present invention provides a more efficient route for preparing ?-turn cyclic peptidomimetic compounds and intermediates thereof.

Abstract: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

Abstract: The invention mainly relates to a method for manufacturing a polypeptide of formula: X1—X?—X2??(III) X1 and X2 each representing a peptide fragment, and X? representing an amino acid residue comprising a thiol function, said method comprising at least one step of ligation reaction between a polypeptide of formula: X1—N(CH2CH2SH)2??(I) and a polypeptide of formula: H—X?—X2.??(II) The invention also relates to the polypeptides of formula (I) themselves and the method for obtaining them, as well as resin supports suitable for obtaining them.

Abstract: The present invention relates to analytical methods such as molecular weight determination of polypeptide, in particular Glatiramer acetate. The present invention further relates to an improved process for preparation of polypeptides or pharmaceutically acceptable salts thereof, particularly Glatiramer acetate also known as Copolymer-1. The present invention further relates to characterization of Glatiramer acetate by peptide mapping.

Abstract: The invention provides certain embodiments relating to methods and compositions for incorporating non-natural amino acids into a polypeptide or protein by utilizing a mutant or modified aminoacyl-tRNA synthetase to charge the non-natural amino acid to a the corresponding tRNA. In certain embodiments, the tRNA is also modified such that the complex forms strict Watson-Crick base-pairing with a codon that normally forms wobble base-pairing with unmodified tRNA/aminoacyl-tRNA synthetase pairs.

Abstract: The present invention relates to a process for the enzymatic production of a dipeptide composition from a cyanophycin (CGP) or CGP-like polymer preparation by degrading the polymer preparation with an CGPase, a CGPase particularly adapted for said process, and the use of cyanophycin (CGP) or CGP-like polymers or fragments thereof, notably a dipeptide composition obtained by the process as defined above, as pharmaceutical composition, medicament, or as food or feed substitute.

Abstract: Improved methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product which contains an aziridinyl ring. Subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product.

Abstract: The present invention relates to an improved process for the preparation of Micafungin.

Abstract: The present invention relates to a chimeric inhibitor protein of a protease comprising an inhibiting polypeptidic sequence and at least one polypeptidic sequence of a substrate-enzyme interaction site specific for a protease. Other objects of the invention are to provide a purified and isolated DNA sequence encoding the chimeric inhibitor protein of a protease, an expression vector characterized in that it comprises said purified and isolated DNA sequence, a eukaryotic or prokaryotic host cell transformed with this expression vector and a method of producing a chimeric inhibitor protein.

Abstract: This invention relates to a method of hydrolysis of the peptide bond between R1 and B in a specific designed amino acid sequence R1BXJZR3R2, where R1 represents a polypeptide of interest, R2 represents a sequence capable of specific binding to another component or molecule or another domain which needs to be cleaved, R3 represents an optional short peptide sequence, B represents a residue capable of accepting an acyl group, J represents a residue capable of metal ion binding, and X and Z represent amino acid residues, wherein the said method is based on a novel molecular mechanism of peptide bond hydrolysis, occurring in a specific complex of this metal ion with the BXJZ sequence. This method can be used to remove BXJZR3R2 domains in recombinant polypeptides, such as sequences capable of specific binding to another component or molecule to yield pure, unmodified R1 polypeptides of interest.

Abstract: A method for stabilizing an alpha helix of a polypeptide includes steps of: (1) connecting an unnatural amino acid to an amino terminus of the polypeptide and end-capping via an acetylation; (2) processing a product of the step (1) with a thiolene reaction and obtaining a polypeptide compound having a modification of thioether side chains; (3) oxidizing the polypeptide compound having the modification of the thioether side chains, and obtaining a polypeptide compound having a modification of R-configured sulfoxide side chains or S-configured sulfoxide side chains; (4) separating and purifying a product of the step (3), and obtaining the modification of the R-configured sulfoxide side chains. CD diagrams show that, via chiral sulfoxide side chains, the method has good performance on stabilizing the alpha helix of the polypeptide and good tolerance to a polypeptide sequence.

Abstract: Methods for building peptide chains containing sulfonyl modified amines at the N-terminus, or, within amino acid side chains, of a growing peptide in a solid-phase peptide synthesis are described. Further, compositions having a sulfonyl modified amine attached to the N-terminus, or within an amino acid side chain, of a polypeptide containing three or more amino acid residues are described.

Abstract: The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.

Abstract: This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.

Abstract: The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.

Abstract: Methods to synthesize self-assembling peptides embedded with complex organic electronic subunits are provided.

Abstract: Described is a method of fabricating biologically active, unnatural polypeptides. The method includes the steps of selecting a biologically active polypeptide or biologically active fragment thereof having an amino acid sequence comprising ?-amino acid residues, and fabricating a synthetic polypeptide that has an amino acid sequence that corresponds to the sequence of the biologically active polypeptide, but wherein about 14% to about 50% of the ?-amino acid residues found in the biologically active polypeptide or fragment of step (a) are replaced with ?-amino acid residues, and the ?-amino acid residues are distributed in a repeating pattern.

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one aromatic amine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one alkylated amine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

Abstract: A nanoparticle-polypeptide complex comprising a bioactive polypeptide in association with a nanoparticle, wherein the bioactive polypeptide is modified by the addition of a chemical moiety that facilitates cellular uptake of the protein. The polypeptide can be a protein or a peptide. In some embodiments, the amino acid sequence of the protein or peptide is derived from the amino acid sequence of a tumor suppressor gene product.

Abstract: A method of selectively introducing a substituent into a protein proximal to a binding site on the protein for a homing peptide, comprising: (a) contacting the protein with a compound comprising a homing peptide having the ability to bind to the binding site of the protein; and (b) allowing a moiety on the protein proximal to the binding site to react with the compound comprising the homing peptide, thereby to transfer the substituent G onto the protein.

Abstract: A chemoselective chemical ligation method is disclosed. The method joins two peptide segments efficiently to produce a larger peptide or protein, by generating a natural peptide bond (Xaa-Ser and Xaa-Thr) at the ligation site (Xaa represents any 5 amino acid). The method requires two steps (FIG. 1 (a)): a) reacting the starting peptide(s) to form an acetal intermediate with an acetal group at the ligation site; b) converting said acetal intermediate to a desired peptide or protein with said natural peptide bond.

Abstract: The present invention is characterized by a D-Aptamer-Like Peptide (D-Aptide) or retro-inverso Aptide which specifically binds to a target comprising: (a) a structure stabilizing region comprising parallel, antiparallel or parallel and antiparallel D-amino acid strands with interstrand noncovalent bonds; and (b) a target binding region I and a target binding region II comprising randomly selected n and m D-amino acids, respectively, and coupled to both ends of the structure stabilizing region. The D-Aptide or retro-inverso Aptide has the sequence of the same or opposite direction to L-Aptide, wherein the stability to proteases is improved while maintaining the affinity to a target compared with L-Aptide. The D-Aptide of the present invention has substantially the same target affinity and a remarkably improved stability compared with L-Aptide which is different from a general technical knowledge.

Abstract: An instrument and method for accelerating the solid phase synthesis of peptides are disclosed. The method includes the steps of deprotecting a protected first amino acid linked to a solid phase resin by admixing the protected linked acid with a deprotecting solution in a microwave transparent vessel while irradiating the admixed acid and solution with microwaves, activating a second amino acid, coupling the second amino acid to the first acid while irradiating the composition in the same vessel with microwaves, and cleaving the linked peptide from the solid phase resin by admixing the linked peptide with a cleaving composition in the same vessel while irradiating the composition with microwaves.

Abstract: Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.

Abstract: A method is provided for the synthesis of glycopeptides using a sugar assisted ligation strategy, wherein an N-terminal peptide portion in the form of a thioester is coopled with a C-terminal peptide portion bearing a carbohydrate moiety comprising a thiol group.

Abstract: Prostaglandin-F2 alpha (PGF2?) receptor (FP) modulators of formula I, as well as the use of PGF2? receptor modulators for the treatment of conditions associated with FP activity such as preterm labor and colorectal cancer, are disclosed.

Abstract: Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.

Abstract: A method for selectively acylating an amino group in a peptide or protein which has two or more reactive nucleophilic functional groups is described.

Abstract: Peptide ligands for transporting therapeutic agents across the intestinal epithelial barrier that ordinarily are inadequately absorbed and must be delivered by alternative means, which contain an isolated amino acid sequence wherein at least one pair of amino acids are of an opposite charge and the pair members are separated by a spacer of 1-12 amino acid residues including at least one hydrophobic amino acid, and wherein the length of the amino acid sequence is greater than 5 and less than 20 amino acids. Pharmaceutical compositions for gastro-intestinal delivery and methods for the gastrointestinal delivery of poorly absorbed therapeutic agents are also disclosed.

Abstract: The present invention discloses a design for a molecular delivery vehicle capable of delivering a molecular payload to a target cell and its intracellular compartments. Also disclosed are highly pH-sensitive nanoconstruct that takes advantage of the requirement of cationic charge for internalization of CPPs to mask the non-specific internalization, compositions containing nanoconstruct, and methods for forming the same.

Abstract: The invention relates to a method for producing C-terminal amidated dibasic or polybasic peptides, consisting in reacting two peptides in the presence of trypsin biologically active enzymes and, if necessary, in purifying the thus obtainable compounds of formula (I) by means of protein chemistry.

Abstract: Embodiments of the invention are directed to a one-bead-two-compound method for the creation of encoded cyclic peptoid libraries. This scheme is useful for the creation of cyclic peptoid microarrays since only the cyclic peptoid, not the linear encoding molecule, contains an attachment residue and thus can be spotted onto an activated substrate.

Abstract: A novel method for synthesizing a Hirulog peptide is devised.