Abstract: Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

Abstract: The present invention relates to new bi-functional and polyfunctional bis-dioxolanes and bis-dioxanes. The present inventors have established that the bis-dioxolanes and bis-dioxanes of the invention are highly advantageous as building blocks, cross-linking and/or coupling agents in polymer engineering. They can be derived from biomass sources in a highly efficient manner. The production of the present bis-dioxolanes and bis-dioxanes from biomass has the particular advantage that it facilitates the introduction of desired functionality in a highly flexible manner. Hence, the present invention provides novel bi- or polyfunctional bis-dioxolanes and bis-dioxanes, their production from renewable (biomass) sources, as well as their use in the engineering of polymers.

Abstract: Provided herein are methods and compositions for the sequencing of long nucleic acids, such as DNA. The methods and compositions are suited for the spatial labeling and sequencing of long nucleic acid molecules.

Abstract: The invention provides pharmaceutical compositions and method of using the compositions, wherein the compositions comprise liposomes or micelles that contain one or more targeting peptides and/or anticancer drugs. In various embodiments, the components of the liposomes can include a) a phospholipid and optionally a lipid that is not a phospholipid; b) a pegylated lipid; c) a peptide-ethylene glycol (EG)-lipid conjugate wherein the peptide is a targeting ligand, and d) one or more drug-conjugated lipid, encapsulated drugs, or a combination thereof. The peptide-EG-lipid conjugate can be, for example, a compound of Formula (I) or Formula (II). The ethylene glycol (EG) segments of the peptide-EG-lipid conjugate can be, for example, EG6 to about EG36; and the EG segment can be conjugated to one or more lysine moieties.

Abstract: The present disclosure relates to the use of a recombinant LAG-3 or derivatives thereof in order to boost a monocyte-mediated immune response, in particular to elicit an increase in the number of monocytes in blood. This finds use in the development of novel therapeutic agents for the treatment of an infectious disease or cancer.

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: Provided herein are methods and compositions for improving muscle performance and increasing endurance. Agonists of AMP-activated protein kinase (AMPK) and agonists of peroxisome proliferator-activated receptor delta (PPAR?) can be used in such treatments.

Abstract: This invention provides a pharmaceutical preparation for DDS containing a pharmaceutical agent fixed by bonding to a monomolecular layer that is covalently bonded to a magnetic particle surface, (a) by reacting an alkoxysilane compound with the magnetic microparticle surface by dispersing a magnetic microparticle in a liquid mixture including an epoxy-containing alkoxysilane compound, a silanol condensation catalyst, and a non-aqueous organic solvent; (b) by washing the microparticle surface with an organic solvent to remove remaining surplus alkoxysilane compound for producing an epoxy-containing monomolecular layer that is covalently bonded to the microparticle surface; and (c) by fixing an imino-containing pharmaceutical agent such as a protein, amino acid, enzyme, antibody, antibiotic, antimicrobial, or contrast medium by reaction with the epoxy group.

Abstract: A pressure gauge may be coupled to a supply line which carries liquid from a bottle to either one or more mixing vessels and/or one or more reactors in a combinatorial processing tool. A control device may monitor the pressure measured by the pressure gauge, and the control device may be configured to change the pressure supplied to the bottle based on a comparison of the measured pressure to a predetermined pressure value. The control device may adjust the pressure provided to the bottle using a pressure regulator coupled to the pressure source. By changing the pressure provided to the bottle, the control device may maintain a relatively constant flow rate of fluids from the liquid source into one or more mixing vessels and/or the one or more reactors.

Abstract: Embodiments described herein generally relate to the separation of carbon nanotubes by reversible gelation.

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: Disclosed are two myocardial peptides, whose amino acid sequences are Trp-Ser-Asn-Val-Leu-Arg-Gly-Met-Gly-Gly-Ala-Phe and Lys-Gly-Ala-Trp-Ser-Asn-Val-Leu-Arg-Gly-Met-Gly-Gly-Ala-Phe respectively, wherein the latter can be obtained by extracting from myocardial peptides solution. The myocardial peptides can be used in the produce of a medicament for preventing and/or treating myocardial ischemia.

Abstract: A precision volumetric liquid dispensing instrument is disclosed that includes two pressure sensors and a fluid passageway with a defined volume portion in communication with the two sensors for receiving and distributing liquid in relatively small volumes. One of the pressure sensors is positioned to measure pressure at one portion of the defined volume portion of the fluid passageway and the other of the gas pressure sensors is positioned to measure gas pressure at a different portion of the defined volume portion of the passageway. At least one valve is in communication with the passageway for moving fluids into or out of the defined volume portion of the fluid passageway, and a processor carries out a step selected from the group consisting of (i) calculating the volume of the liquid based upon the measured pressure and (ii) metering a liquid into the defined volume portion of the fluid passageway until the measured pressure indicates that a desired volume of fluid is in the fluid passageway.

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 provides modified collagen and related therapeutic and diagnostic methods.

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

Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.

Abstract: The invention describes peptide ligands specific for human plasma Kallikrein.

Abstract: Nanoparticles can include a core linked to a polymerizable moiety that can be polymerized, cross-linked or cured. The polymerizable nanoparticles can be included in a composition for a polymerization, cross-linking or curing reaction in an amount and disposition sufficient for inhibiting or preventing volume shrinkage during polymerization, cross-linking or curing reaction. Also, the nanoparticles can be included with monomers, dendrimers, oligomers or polymers in the compositions that can be reacted to form a polymerized, cross-linked or cured product.

Abstract: The invention relates to multimeric forms of antimicrobial peptides, for example, defensin peptides. The multimeric forms of defensin peptides possesses antimicrobial activity and may be formulated into antimicrobial compositions, pharmaceutical compositions, eyedrop composition, contact lens solution compositions for coating medical devices and the like. The invention also relates to the use of these multimeric forms of peptides, e.g. multimeric forms of defensin peptides for inhibiting and/or reducing the growth of microorganisms in general, including in a host. The invention further relates to a method of preparing multimers of peptides derived from defensins, for example hBD3.

Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided.

Abstract: ?-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa7, Xaa8, Xaa13 and Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties 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: The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D-mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.

Abstract: Apparatus and methods utilizing infrared energy for heating reactions associated with peptide synthesis, such as activation, deprotection, coupling, and cleavage. Thorough agitation of the contents of reaction vessels during heating and real-time monitoring and adjustment of temperature and/or reaction duration are also described. Existing peptide synthesizers may be retrofitted to include an infrared energy source.

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: The invention provides a cross-linked poly-?-lysine polymer. The poly-?-lysine and cross linker are linked by amide bonds and may the cross linker has at least two functional groups capable of reacting with an alpha carbon amine of poly-?-lysine. The polymer is suitably insoluble in water and other solvents and is provided in particulate form. The invention provides a particulate support comprising the cross-linked poly-?-lysine polymer and the polymer may provide the particle itself or be coated on a particle for example silica. The polymer is useful in a wide range of applications including wound treatment, as a medical diagnostic comprising a particulate support and a functional material bound or retained by the support and solid phase synthesis of peptides, oligonucleotides, oligosaccharides, immobilisation of species, cell culturing and in chromatographic separation.

Abstract: The present invention relates to a hydrophilic crosslinked polymer, preferably in the form of porous particles, and to the preparation and use thereof. The polymer according to the invention is produced by polymerisation from chain-forming hydrophilic vinyl ethers and crosslinking, preferably heterocyclic divinyl ethers.

Abstract: Heteroclitic analogs of Class I epitopes are prepared by providing conservative or semi-conservative amino acid substitutions at positions 3 and/or 5 and/or 7 of these epitopes. The analogs are useful in eliciting immune responses with respect to the corresponding wildtype epitopes.

Abstract: The present invention provides a solid support for Fmoc-solid phase synthesis of peptides. In particular, the solid supports of the invention may be utilized to produce peptide acids.

Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided.

Abstract: Peptides of general formula (I): R1—Wn—Xm-AA1-AA2-AA3-AA4-AA5-AA6-Yp—Zq—R2 their stereoisomers, mixtures thereof and/or their cosmetically or pharmaceutically acceptable salts, a preparation process, cosmetic or pharmaceutical compositions which contain them and their use in the treatment and/or care of conditions, disorders and/or diseases which improve or are prevented by PGC-1? modulation.

Abstract: The invention provides a universal linker capable of synthesizing nucleic acid having a phosphate group at the 3? terminal, a universal support carrying the linker, and a synthesis method of nucleic acid using the universal support. The linker for solid phase synthesis of nucleic acid contains a compound represented by at least one of the following formulae wherein each symbol is as defined in the specification.

Abstract: [Technical Promblem] To provide a method for manufacturing that enables to obtain a targeted glycopeptide harboring a sialyl sugar chain in high yield without decomposing sialic acid at a non-reducing terminal of sugar chain when the glycopeptide is synthesized by a Boc solid phase synthesis method. [Solution to Problem] The present invention is characterized in that the Boc-sialylglycosylated amino acid derivative used in Boc solid phase synthesis method is one where the carboxyl group of the sialic acid at the sugar chain non-reducing terminal is protected with a phenacyl group.

Abstract: The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.

Abstract: The present invention relates to methods and compositions for pretargeting delivery of therapeutic agents. In preferred embodiments, the pretargeting method comprises: a) administering a bispecific antibody with a first binding site for a disease-associated antigen and a hapten on a targetable construct; b) administering a targetable construct comprising at least one therapeutic agent. In preferred embodiments, the bispecific antibody is made by the dock-and-lock (DNL) technique. In a more preferred embodiment, the targetable construct comprises one or more SN-38 moieties.

Abstract: Polypeptides labelled with a donor and acceptor pair of dyes selected from a dibenzorhodamine dye and a diamino-benzophenoxazine dye are peptide conjugates which are useful for intracellular and bead-based assays with fluorescence detection. Peptide conjugates with a caspase-recognition site undergo cleavage into peptide fragments which may be detected, located, and quantitated by the changes in fluorescence. Intracellular cleavage of peptide conjugates is correlated with apoptosis.

Abstract: A method for preparing a peptide or peptides containing a dicarba bridge, comprising: (i) providing a reactable peptide having at least two complementary metathesisable groups or two or more reactable peptides having at least two complementary metathesisable groups between them; (ii) subjecting the reactable peptide or reactable peptides to metathesis to form a reactable peptide or peptides having at least one unsaturated dicarba bridge; and (iii) adding one or more further amino acids to one or both ends of at least one of the reactable peptides.

Abstract: A bifunctional linker and method of use is provided that has a spacer molecule with a functional group on one end configured to couple to the surface of a substrate and a function group on the other end that is configured couple to a biomolecule and methods of use. The preferred bifunctional linker has a poly(ethylene glycol) spacer ranging from 3 to 20 ethylene glycol units that has a silane functional group to react with a substrate and an azide functional group that can couple to a biomolecule that includes an alkyne group. The preferred linker can produce an azide-derivatized glass surface in one step and the azide functional group of the spacer can in sequence conjugate with a biomolecule using click chemistry, which can be conducted at low temperature and in aqueous solution.

Abstract: A new method of synthesizing GLP-1 peptide is devised.

Abstract: A method for preparing exenatide by solid-phase synthesis, including: 1) mixing an Fmoc-Rink amide AM resin with a deprotecting agent to obtain a Rink amide AM resin; 2) condensing an Fmoc-Ser(tBu)-OH with the Rink amide AM resin to obtain an Fmoc-Ser(tBu)-Rink amide AM resin; 3) repeating the Fmoc deprotection and the condensation between an amino acid and a polypeptide on the resin, and condensing an amino acid with a polypeptide on the resin from the C-terminal to the N-terminal, to form a polypeptide resin; and 4) separating the polypeptide and the resin on the polypeptide resin.

Abstract: The present invention relates to novel phalloidin derivatives and their fluorescent dye conjugates. These new compounds may be used in studies of actin dynamics in living systems. The present invention also relates to methods for preparing such compounds. The synthesis routes combine solid-phase and solution phase peptide synthesis, and has great advantage for efficient preparation of a diverse library of the phalloidin derivatives, especially for the synthesis of phalloidin.

Abstract: The present invention relates to a controlled metathesis-driven polymerization process which is particularly useful for the synthesis of biological polymers such as peptides and polymers. The invention also provides metathesisable supports, groups and linkers for use in the process.

Abstract: The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.

Abstract: The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

Abstract: An apparatus is provided for the semi-automated parallel synthesis of multiple peptides. The apparatus includes an array of nozzles, each positioned above or adjacent a separate reaction container, two or more liquid reservoirs, each reservoir coupled to the liquid dispenser(s), and base chamber(s) connected to the reaction containers for removing liquid there from. The addition and removal of liquids may be controlled by programmable electromagnetic valves. The apparatus may also be used for other parallel solid phase reactions. A method is also provided for synthesizing multiple polypeptides or other macromolecules, for example by using the above apparatus, wherein multiple common steps are performed automatically while reactants are added manually.

Abstract: The invention relates to a method for obtaining thymosins and/or the pharmaceutically acceptable salts thereof by means of solid-phase synthesis on polymeric supports, which comprises the steps of linearly synthesizing the thymus-derived peptides in solid phase, incorporating at least one Thr or Ser in the sequence, in pseudoproline dipeptide form, obtaining the thymosins by treating the peptidyl resin with trifluoroacetic acid, and purifying the thymosins by RP-HPLC. The present invention also protects the isolated and/or purified compound obtained by means of said method and also the use thereof in the preparation of a medicinal product.

Abstract: The present invention discloses a process for preparing ubiquinated peptide conjugates comprising a ubiquitin peptide residue UR attached at its C-terminus to a substrate peptide via a native isopeptide bond, this process comprising combining Native Chemical Ligation (NCL) and solid phase peptide synthesis (SPPS). Further are disclosed ubiquinated peptide conjugates containing a native isopeptide bond, as well as various uses thereof.

Abstract: A process for manufacturing a cyclic peptide which comprises providing a cyclic peptide bonded to a Merrifield-type resin and cleaving the cyclic peptide from the Merrifield type resin by transesterification.

Abstract: Water soluble reagents and methods for the formation of an amide bond between a phosphinothioester and an azide in an aqueous medium. The phosphinothioester is generated using a water-soluble phosphinothiol reagent. This reaction allows formation of an amide bond between a wide variety of chemical species including amino acids, peptides or protein fragments in an aqueous solution. Of particular interest, this reaction allows for the formation of an amide bond in a physiological setting. In a specific embodiment, this invention provides reagents and methods for peptide ligation in an aqueous medium. The reaction eliminates the need for a cysteine residue and is traceless leaving no residual atoms in the ligated peptide product.

Abstract: The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the modulation of unwanted immune responses, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use.