Abstract: The present invention is to provide a method for producing a peptide containing an N-alkylamino acid, which comprises the following Steps (1) to (3). Step (1): a step of mixing an N-terminal protected amino acid or an N-terminal protected peptide with a carboxylic acid halide or a halogenated alkyl formate; Step (2): a step of mixing an amino acid or a peptide in which the N-terminal and the C-terminal are not protected with a trialkylsilylating agent; and Step (3): a step of mixing the product obtained in Step (1) with the product obtained in Step (2).

Abstract: Described are methods and uses of TRPV3 agonists for the treatment of conditions associated with TRPV3 pathophysiology such as acne, psoriasis, dermatitis, would healing, the inhibition of hair growth, anxiety or depression. Peptides comprising all or part of the C-terminal portion of soricidin are shown to activate TRPV3 cation channel activity and/or promote wound healing in keratinocytes.

Abstract: The present invention provides a linker for preparing antibody-drug conjugates and antibody-drug conjugates prepared by the linker, as well as use of the antibody-drug conjugates in a medicament for treating tumor. The linker is capable of coupling simultaneously with the thiol group or amino group on the antibody or functional fragment of the antibody, especially it is capable of coupling with 2, 3 or 4 thiol groups on the antibody or functional fragment of the antibody. A coupled product is uniform and structurally stable.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.

Abstract: Provided are amino acid based polymerizable compounds and their applications in ophthalmic devices. The amino acid based polymerizable compounds are of formula I: wherein R, R1, and R2 are as described herein.

Abstract: This document provides butyrylcholinesterases having an enhanced ability to hydrolyze acyl ghrelin as well as nucleic acids encoding such butyrylcholinesterases. This document also provides methods and materials for treating obesity and/or aggression. For example, methods for administering a nucleic acid encoding a wild-type or mutant butyrylcholinesterase having the ability to hydrolyze acyl ghrelin to a mammal under conditions wherein the level of acyl ghrelin within the mammal is reduced, under conditions wherein the rate of body weight gain of the mammal is reduced, under conditions wherein the mammal's level of aggression is reduced, and/or under conditions wherein the mammal's rate of developing stress-induced tissue damage are provided.

Abstract: Disclosed herein are chimeric antigen receptor (CAR) polypeptides that can be used with adoptive cell transfer to target and kill IL13Ra2-expressing cancers. Also disclosed are immune effector cells, such as T cells or Natural Killer (NK) cells, that are engineered to express these CARs. Therefore, also disclosed are methods of providing an anti-tumor immunity in a subject with an IL13Ra2-expressing cancer that involves adoptive transfer of the disclosed immune effector cells engineered to express the disclosed CARs.

Abstract: Disclosed is a vaccine containing an MTV transition protein. A further version of the invention is a vaccine comprising MTV polypeptides coupled to a carrier protein. MTV may be treated by providing an MTV vaccine with an MTV transition protein; and, administering said vaccine.

Abstract: There is disclosed an improved ADC (antibody drug conjugate) type composition having at least two different drug payloads conjugated to a single targeting protein. More specifically, the present disclosure attaches a first drug conjugate to a dual Cysteine residue on a targeting protein and a second drug conjugate with a different drug to a Lys residue on the targeting protein.

Abstract: A method for producing a protein composition containing a protein (A), a radical scavenger (RS), and at least one hydrogen-bond-formable compound (HC) selected from the group consisting of amino acids, peptides, and proteins other than the protein (A). The method including a sterilization step of radiosterilizing an unsterilized protein composition, wherein the unsterilized protein composition contains the protein (A), the radical scavenger (RS), and the hydrogen-bond-formable compound (HC), the protein (A) contains at least one functional group selected from the group consisting of sulfide, amide, hydroxyl, amino, and carboxyl groups, the hydrogen-bond-formable compound (HC) contains at least one functional group selected from the group consisting of sulfide, amide, hydroxyl, amino, and carboxyl groups, the at least one functional group in the protein (A) is capable of binding to the at least one functional group in the hydrogen-bond-formable compound (HC) via a hydrogen bond.

Abstract: Systems and methods for making an antenna reflector. The methods comprise: obtaining a Carbon Nano-Tube (“CNT”) material; cutting the CNT material into a plurality of wedge shaped pieces; and bonding together the wedge shaped pieces using a resin film adhesive to form the antenna reflector with a three dimensional contoured surface.

Abstract: The invention relates to neurodegenerative disorders, and in particular to novel peptides, peptidomimetics, compositions, therapies and methods for treating such conditions, for example Alzheimer's disease.

Abstract: The present invention provides a multivalent compound for targeted molecular imaging and/or targeted drug delivery, wherein two components or targeting molecules each interacts with one or more biomarkers on a cell. The present invention further provides a multifunctional chelator to combine the targeting molecules. The present invention also provides an in vitro high-throughput screening assay to determine the length of the spacer molecules. The present invention also relates to compounds/probes, kits and methods for use in targeted molecular imaging and/or targeted drug delivery.

Abstract: Provided are compounds described by the Formula I: wherein: R1 is a linear or branched, saturated or unsaturated aliphatic group having from 5 to 22 carbon atoms; R2 is selected from the group consisting of the functional groups: —NH2; and salts thereof; n is from 0 to 4; and R3 is a linear or branched, saturated or unsaturated aliphatic group having from 1 to 6 carbon atoms. Also provided are compositions comprising, and methods of use of, the compounds of the present invention.

Abstract: The invention generally relates to targeted compounds for the site-specific coupling of chemical moieties. The present invention features a targeted compound for the coupling of chemical moieties comprising at least one targeting domain capable of binding a target, and at least one linking moiety of up to 80 amino acids, preferably alanine, proline, and serine, and at least one coupling site consisting of cysteine or a cysteine-rich peptide motif (CXC, CXXC, or CXXXC), and wherein said linking moiety connects the targeting domain and a coupling site and/or wherein a linking moiety connects two coupling sites. The invention further features fusion proteins with ubiquitin muteins (Affilin @) as targeting domain. The invention also relates to the use of the targeted compounds for medical applications, in treatment or diagnosis of diseases.

Abstract: The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

Abstract: The present invention provides a pharmaceutical composition comprising a binary conjugate, DC009, which is a conjugate of a thrombolytic peptide (Pro-Ala-Lys) and a tetrahydroisoquinoline compound having two C1-4 alkyl groups via a lysine linking arm, and a pharmaceutical acceptable carrier. The composition has a pH less than 6.5, preferably has a pH about pH 2-5.5 The composition may comprise a pharmaceutical acceptable excipient such as mannitol, sorbitol, sucrose, lactose, or trehalose.

Abstract: Provided is an antibody-drug conjugate (ADC) using one or more cysteine or derivatives thereof as linkers to couple one or more drugs at the limited binding sites of an antibody, making it possible to produce an ADC product with high drug payload, or to choose a drug with less toxicity, thereby obtaining an ADC product with wide therapeutic window. In addition, since a plurality of drugs may be coupled to one binding site, the ADC products obtained by the method of the present disclosure have better uniformity in the case of same DAR value. Moreover, the amount of antibody required for production may be greatly reduced, thereby lowering the cost. Compared with the antibody-drug conjugates coupled only one drug, the antibody-drug conjugates produced by the method of the present disclosure have the same inhibition or killing effect on tumor cells while using fewer drugs for coupling to the same site.

Abstract: The present application discloses a crystal of oxidized glutathione dication salt and a method of producing the same.

Abstract: Provided herein is a combination comprising an HDAC inhibitor and an IMiD for increasing interferon regulated gene expression or decreasing c-MYC gene expression in a cancer cell or tumor in a subject in need thereof. Increasing interferon regulated gene expression may result in increased recognition of tumors by innate or adaptive immune system and an increase in programmed cell death (apoptosis) gene expression, increasing apoptosis in cancer cells and tumors. The cells can be multiple myeloma cells or diffuse large B-cell lymphoma cells. Also provided are methods for treating myelodysplastic syndromes/acute myeloid leukemia (MDS/AML) or pathogen infections in a subject in need thereof comprising administering to the subject an effective amount of HDAC inhibitor and an IMiD. The HDAC inhibitor can be an HDAC6-selective inhibitor.

Abstract: In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.

Abstract: The present invention relates to a crystal of glutathione trisulfide dihydrate and a method for producing the same. According to the present invention, for example, the crystal can be provided by concentrating an aqueous solution in which glutathione trisulfide is dissolved and collecting the precipitated crystal of glutathione trisulfide dihydrate. In addition, the present invention relates to a simple method for producing polysulfide in an aqueous solvent using thiosulfate without using hydrogen sulfide, by stirring an aqueous solution in which a compound having a thiol group or a disulfide bond and thiosulfate are dissolved or by leaving the aqueous solution to stand.

Abstract: Methods of delivering therapeutic agents by administering compositions including a bacterial collagen-binding polypeptide segment linked to the therapeutic agent to subjects in need of treatment with the therapeutic agent are provided. In these methods, the therapeutic agent is not a PTH/PTHrP receptor agonist or antagonist, basic fibroblast growth factor (bFGF) or epidermal growth factor (EGF). The bacterial collagen-binding polypeptide segment delivers the agent to sites of partially untwisted or under-twisted collagen. Methods of treating collagenopathies using a composition including a collagen-binding polypeptide and a PTH/PTHrP receptor agonist are also provided. In addition, methods of treating hyperparathyroidism, and hair loss using compositions comprising a collagen binding polypeptide and a PTH/PTHrP receptor agonist are provided. Finally, methods of reducing hair regrowth by administering a composition including a collagen binding polypeptide and a PTH/PTHrP receptor antagonist are provided.

Abstract: The peptides have the general following formula: X-Pro*-Pro*-Xaa-Y in which: •Xaa is selected from Leucine (Leu, L), Arginine (Arg, R), Lysine (Lys, K), Alanine (Ala, A), Serine (Ser, S), and Aspartic acid (Asp, D); •At the N terminal end of the peptide, X is selected from H, —CO—R1 and —SO2—R1; •At the C terminal end of the peptide, Y is selected from OH, OR1, NH2, NHR1 and NR1R2; •R1 and R2 are, independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly-cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulfured, and which skeletum can comprise an heteroatom, in particular an O, S and/or N atom; •Pro* correspond to a Proline, an analogue or derivative thereof; •if X is H then Y is selected from OR1, NH2, NHR1 and NR1R2, and if Y is OH then X is —CO— or —SO2—R1; and the peptide hypoxanthine-Pro-Pro-Arg being excluded.

Abstract: A method of treating cancer in a subject in need thereof, comprising administering to the subject a first amount of a compound of the HAT inhibitor of the following formula: wherein R is chosen from coenzyme A, (CH2)2NHCO(CH2)2NHCOR2; (CH2)2NHCOR3; (CH2)2NHCO(CH2)2NHCOR4; R1 is H, NH2, NH, N, and R1 can optionally cyclize with at least one other X2 to form a C3-8 membered ring containing C, O, S, or N; R2 is chosen from alkyl, cycloalkyl, aryl, heteroaryl; R3 is chosen from an alkyl, cycloalkyl, aryl, heteroaryl; R4 is chosen from CH(OH)C(CH3)2CH2)OCOR2; X1 is chosen from H or can cyclize with one other X2 or R1 to form a C3-8 membered ring containing C, O, S, or N; and X2 is chosen from C, N, NH, and can optionally cyclize with at least one other X2 or R1 to form a C3-8 membered ring containing C, O, S, or N; or a pharmaceutically acceptable salt or hydrate thereof, thereby treating the cancer.

Abstract: The invention is concerned with the compounds of formula I: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Abstract: This invention relates to quaternary amine linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.

Abstract: Some embodiments of the invention involve methods for introduction of various functional groups onto polypeptides, peptides and proteins by alkylation of thioether (a.k.a. sulfide) groups by ring opening reactions, creating new compositions of matter that may be useful for medical therapeutic or diagnostic applications. The thioether groups may either be present in the polypeptides, or may be added to polypeptides by chemical modification, such as by alkylation of thiol (sulfhydryl) groups.

Abstract: Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a ?-elimination mechanism.

Abstract: Methods for treating a bioprosthetic tissue are described herein. The methods comprise contacting the bioprosthetic tissue with at least one nucleophile and/or at least one electrophile in the presence of a catalytic system comprising at least one or a combination of a fluoride-based salt, a cesium-based salt, a potassium-based salt, a rubidium-based salt, or a carbonate-based salt. The methods may be used to alter functional groups on biological tissue which represent actual and potential calcium binding sites and also processes for cross-linking bioprosthetic tissue. Both processes may be used in conjunction with known fixative techniques, such as glutaraldehyde fixation, or may be used to replace known fixative techniques.

Abstract: The invention is directed to the use of at least one peptide of formula: X—(Xaa1)n-Pro*-(Xaa2)m-Y (I) With: —n=0, 1 or 2; —m=0 or 1 and if m=0 then n?0-Xaai is: —An hydrophobic amino acid; —A polar amino acid; —or Glycine (Gly, G); When n=2 the two amino acids Xaa1 can be the same or different; —Xaa2 is: —An hydrophobic amino acid; —A basic amino acid Glycine (Gly, G) or Serine (Ser, S); —At the N terminal end of the peptide, X is selected from H, —CO—R1 and —SO2—R1; —At the C terminal end of the peptide, Y is selected from OH, OR1, NH2, NHR1 or NR1R2, R1 and R2 being independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group; Excluding the peptides where X=H and Y=OH, for a non therapeutical cosmetic pro-pigmenting treatment of skin.

Abstract: Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.

Abstract: The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).

Abstract: The disclosure provides crystalline Sovaprevir forms. The crystalline forms of Sovaprevir comprise a Form A polymorph, a Form B polymorph, a Form C polymorph, a Form D polymorph, and a Form E polymorph. The Form A, B, C, D, and E polymorphs exhibit X-ray powder diffraction patterns having peak locations in accordance with FIGS. 1, 4, 7, 10, and 13, respectively.

Abstract: The present invention relates to a chromogenic method for simultaneously determining the activity of multiple coagulation proteases or for simultaneously determining the inhibition of multiple coagulation proteases in a single test reaction. For this purpose, use is made of two chromogenic substrates which have different absorption maxima and whose color signals can be separated spectrally.

Abstract: The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.

Abstract: The present invention provides a production method of peptide, which includes the following step (1). (1) removing N-terminal Fmoc group of N-Fmoc C-protected amino acid or N-Fmoc C-protected peptide wherein a C-terminal carboxy group is protected by an anchor group derived from an anchor soluble in halogenated solvents or ether solvents, insoluble in polar solvents and having a molecular weight of not less than 300, with a non-nucleophilic organic base in a halogenated solvent or ether solvent to give a C-protected amino acid or C-protected peptide, neutralizing with an acid, adding N-Fmoc amino acid or N-Fmoc peptide, a condensing agent and a condensation accelerator to the reaction solution after neutralization, and condensing the N-terminal of the C-protected amino acid or C-protected peptide with N-Fmoc amino acid or N-Fmoc peptide to give an N-Fmoc C-protected peptide.

Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:

Abstract: A peptide which can adopt a 310-helical conformation in which the side chains of two amino acid residues in the peptide backbone are linked by a group comprising an aromatic 5-membered ring.

Abstract: The present invention relates to a method for detecting at least one direct factor Xa inhibitor in a sample other than citrate plasma, comprising the step of mixing a sample containing a factor Xa inhibitor with a composition containing factor Xa under conditions which allow the factor Xa to release a detectable substance from a chromogenic substrate.

Abstract: The present invention relates to a composition for improving or promoting hair growth, which contains, as an active ingredient, a photosensitizer-peptide conjugate, and to a method for screening for the hair growth promoter using the active ingredients. ALA, which is the photosensitizer of the present invention, is preferably activated by LED radiation, and more preferably activated by radiation having a long wavelength of 650 to 675 nm. The peptide of the present invention is a peptide in which 3 to 7 amino acid residues are incorporated (most preferably, glycine-histidine-lysine), and may cooperate with the photosensitizer to enable very superior hair growth improving or promoting effects using light radiation. Further, the composition of the present invention may exhibit further superior effects when natural extracts (for example, Cimicifuga heracleifolia extracts, Scutellaria baicalensis extracts or Codonopsis lanceolata extracts) are added.

Abstract: A composition of dipeptides or tripeptides or ester derivatives may be used as a nutritional supplement and to modulate expression of genes associated with healthy maintenance and regulation of muscular and neurological tissue. The compositions include dipeptides and/or tripeptides of branched chain amino acids and optionally include adjuvants, anti-aging compounds and may be provided in a dissolvable powder or liquid form.

Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula Ia or Ib: The peptoid oligomers are prepared as modulators of androgen receptor (AR), and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals, including humans, associated with unwanted or aberrant AR activity. The present peptoid oligomers are particularly valuable for the treatment of subjects with cancer.

Abstract: The present invention provides a method of radio fluorination of biological targeting molecules (BTMs) with the radioisotope 18F. Also provided are novel conjugates useful in the 18F-radio fluorination method, and the use of such conjugates and automated synthesizer apparatus including cassettes for carrying out the method.

Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: A topical composition for application to aging skin, including an effective amount of S-acyl glutathione derivative of formula (I) wherein R1 consists of an unsaturated or saturated C16 acyl group and R2 is a hydrogen, aliphatic or aromatic acyl group; and a dermatologically acceptable carrier. Preferred compositions include about 1.0% to about 3.0% by weight of S-palmitoyl glutathione.

Abstract: The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.

Abstract: Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range.

Abstract: Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.

Abstract: An isolated peptide is disclosed. The peptide comprises a titanium oxide binding amino acid sequence connected to a heterologous biologically active amino acid sequence via a beta sheet breaker linker, wherein: (i) the titanium oxide binding amino acid sequence is selected to bind coordinatively with titanium oxide; (ii) the titanium oxide binding amino acid sequence is selected to induce a beta sheet structure; and (ii) the titanium oxide binding amino acid sequence binds to titanium oxide with a higher affinity than said biologically active amino acid sequence binds to the titanium oxide under physiological conditions. Use of the peptides and titanium devices comprising same are also disclosed.