Abstract: SorCS2 related lipidated cyclic peptides, cyclic peptides, lipidated linear peptides, linear peptides which may be of use in medicine, and related aspects.

Abstract: The invention regards a method for 18F-labeling of a peptide.

Abstract: SorCS2 related lipidated cyclic peptides, cyclic peptides, lipidated linear peptides, linear peptides which may be of use in medicine, and related aspects.

Abstract: The present invention relates to virally expressed peptides which bind to PDZ domains and thereby block PDZ domain mediated protein-protein interactions and expression vectors encoding these peptides. The virally expressed peptides comprise an oligomerization domain, capable of forming higher order constructs, such as trimers or tetramers, and a peptide ligand capable of binding to a PDZ domain. The invention furthermore relates to therapeutic use of said peptides and expression vectors encoding these peptides.

Abstract: The present invention relates novel cyclic peptides which can act as inhibitors of protein-protein interactions, specifically by inhibiting the PDZ2 domain of PSD-95, as well as their use in treatment of excitotoxic-related diseases and neuropathic pain.

Abstract: The present invention relates to a conjugated molecule comprising a peptide displaying at least 0.1% activity of native glucagon-like peptide 1 (GLP-1) at the GLP-1 receptor, and an N-methyl-D-aspartate receptor (NMDAR) antagonist, the peptide being covalently bonded to the NMDAR antagonist either directly or through a chemical linker, the conjugated molecule for use in therapy, pharmaceutical composition comprising the conjugated molecule, a method of reducing body weight of a mammal comprising administering the conjugated molecule to the mammal, and a non-therapeutic method of reducing body weight of a mammal comprising orally administering the conjugated molecule to the mammal.

Abstract: The present invention relates to virally expressed peptides with high affinity for the PDZ domains, such as the PDZ domain of PICK1. The invention furthermore relates to the therapeutic use of these peptides in prevention and/or treatment of diseases and/or disorders associated with maladaptive plasticity and/or transmission.

Abstract: The present invention relates to peptides and peptide analogues with high affinity for the PDZ domains of PICK1. The peptide or peptide analogue interacts with PICK1, blocking the native protein-protein interactions between PICK1 and its natural ligands. The invention furthermore relates to the therapeutic use of these peptides and peptide analogues in prevention and/or treatment of diseases and disorders associated with maladaptive plasticity, drug addiction and neuropathic pain.

Abstract: The present invention is directed to the provision of small molecule inhibitors of the PSD-95/NMDA receptor interaction, employing an undecapeptide corresponding to the C-terminal of the NMDA as a template for finding lead candidates. A compound (NMDAR/PSD-95 inhibitor) of the invention includes a peptide or peptide analog comprising at least four peptide bonded residues having the sequence YTXV or YSXV, wherein Y is selected from among E, Q, and A, or an analog thereof, and X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analog thereof, wherein an amino-terminal residue of the peptide is N-alkylated.

Abstract: The present invention provides fatty acid derived compounds capable of binding to the PDZ domains of PSD-95 and their medical use as inhibitors of protein-protein interaction mediated by PSD-95.

Abstract: The present invention is directed to the provision of small molecule inhibitors of the PSD-95/NMDA receptor interaction, employing an undecapeptide corresponding to the C-terminal of the NMDA as a template for finding lead candidates. A compound (NMDAR/PSD-95 inhibitor) of the invention includes a peptide or peptide analogue comprising at least four peptide bonded residues having the sequence YTXV or YSXV, wherein Y is selected from among E, Q, and A, or an analogue thereof, and X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analogue thereof, wherein an amino-terminal residue of the peptide is N-alkylated.

Abstract: The present invention is directed to the provision of small molecule inhibitors of the PSD-95/NMDA receptor interaction, employing an undecapeptide corresponding to the C-terminal of the NMDA as a template for finding lead candidates. A compound (NMDAR/PSD-95 inhibitor) of the invention includes a peptide or peptide analogue comprising at least four peptide bonded residues having the sequence YTXV or YSXV, wherein Y is selected from among E, Q, and A, or an analogue thereof and X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analogue thereof, wherein an amino-terminal residue of the peptide is N-alkylated.

Abstract: The invention provides novel potent inhibitors of the ternary protein complex of nNOS, PSD-95, and the NMDA receptor and pharmaceutical compositions comprising the inhibitors for prophylaxis and/or treatment of excitotoxic-related disease and chronic pain conditions in a subject. The inhibitors are dimeric PSD-95 inhibitors comprising a first peptide or peptide analogue linked to a second peptide or peptide analogue by a linker, wherein the first and the second peptide or peptide analogue comprise at least four amide-bonded residues having a sequence YTXV (SEQ ID NO: 5) or YSXV (SEQ ID NO: 6), wherein a. Y is selected from among E, Q, and A, or an analogue thereof, and b. X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analogue thereof, and wherein a Cell Penetrating Peptide (CPP) is linked to the linker or to an amino acid side chain of the first and second peptide or peptide analogue. The linker can be a PEG or NPEG linker.

Abstract: The invention provides novel potent inhibitors of the ternary protein complex of nNOS, PSD-95, and the NMDA receptor and pharmaceutical compositions comprising the inhibitors for prophylaxis and/or treatment of excitotoxic-related disease and chronic pain conditions in a subject. The inhibitors are dimeric PSD-95 inhibitors comprising a first peptide or peptide analogue linked to a second peptide or peptide analogue by a linker, wherein the first and the second peptide or peptide analogue comprise at least four amide-bonded residues having a sequence YTXV or YSXV, wherein a. Y is selected from among E, Q, and A, or an analogue thereof, and b. X is selected from among A, Q, D, N,N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analogue thereof, and wherein a Cell Penetrating Peptide (CPP) is linked to the linker or to an amino acid side chain of the first and second peptide or peptide analogue. The linker can be a PEG or NPEG linker.

Abstract: The present invention is directed to the provision of small molecule inhibitors of the PSD-95/NMDA receptor interaction, employing an undecapeptide corresponding to the C-terminal of the NMDA as a template for finding lead candidates. A compound (NMDAR/PSD-95 inhibitor) of the invention includes a peptide or peptide analogue comprising at least four peptide bonded residues having the sequence YTXV or YSXV, wherein Y is selected from among E, Q, and A, or an analogue thereof and X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analogue thereof, wherein an amino-terminal residue of the peptide is N-alkylated.

Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1-C5) alkyl group, (C2-C5) alkenyl, or a (C2-C5) alkynyl, (C1-C5) alkoxy, (C2-C5) alkenyloxy, or (C2-C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1-C5) alkyl, (C2-C5) alkenyl, or (C2-C5) alkynyl, or a cyclo

Abstract: The subject invention provides ginkgolide C derivatives compounds having the structure: wherein R is H or -A-Ar, where A is an alkyl group; and Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, —CH2CO2R4, and —CH2CONR5R6; where R4 is an alkyl group; and R5 and R6 are each, independently, hydrogen or a branched or unbranched alkyl group; wherein R1 is H or —COR7, where R7 is alkyl, aryl or amino; wherein R2 is present or absent, and when present is H, —COR8 or —CO—Z—R8; where R8 is alkyl, aryl or amino; and Z is oxygen; wherein R3 is present or absent, and when present is —COR9; where R9 is alkyl or aryl; wherein only one of R2 or R3 is present in the compound; wherein only two of R, R1, R2 and R3 are H; and wherein each of a and b designates a single covalent bond which is present or absent, where bond a is present when R3 is absent and bond b is present when R2

Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1-C5) alkyl group, (C2-C5) alkenyl, or a (C2-C5) alkynyl, (C1-C5) alkoxy, (C2-C5) alkenyloxy, or (C2-C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1-C5) alkyl, (C2-C5) alkenyl, or (C2-C5) alkynyl, or a cycl

Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1–C5) alkyl group, (C2–C5) alkenyl, or a (C2–C5) alkynyl, (C1–C5) alkoxy, (C2–C5) alkenyloxy, or (C2–C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1–C5) alkyl, (C2–C5) alkenyl, or (C2–C5) alkynyl, or a cyclo

Abstract: The subject invention provides ginkgolide C derivatives compounds having the structure: wherein R is H or -A-Ar, where A is an alkyl group; and Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, —CH2CO2R4, and —CH2CONR5R6; where R4 is an alkyl group; and R5 and R6 are each, independently, hydrogen or a branched or unbranched alkyl group; wherein R1 is H or —COR7, where R7 is alkyl, aryl or amino; wherein R2 is present or absent, and when present is H, —COR8 or —CO-Z-R8; where R8 is alkyl, aryl or amino; and Z is oxygen; wherein R3 is present or absent, and when present is —COR9; where R9 is alkyl or aryl; wherein only one of R2 or R3 is present in the compound; wherein only two of R, R1, R2 and R3 are H; and wherein each of a and b designates a single covalent bond which is present or absent, where bond a is present when R3 is absent and bond b is prese