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    PROBE AND METHOD FOR DETECTING MEMBRANE-ASSOCIATED MOLECULES IN LIVING CELLS
    2.
    发明公开
    PROBE AND METHOD FOR DETECTING MEMBRANE-ASSOCIATED MOLECULES IN LIVING CELLS 审中-公开

    公开(公告)号：EP4184168A1

    公开(公告)日：2023-05-24

    申请号：EP21209717.4

    申请日：2021-11-22

    申请人： Ustav organicke chemie a biochemie AV CR, v.v.i.

    发明人： Lazar, Josef ,  Bondar, Alexey

    IPC分类号： G01N33/542 ,  G01N33/566 ,  G01N33/58 ,  C07K14/47

    摘要： The invention pertains to a protein-based probe for detecting the presence of one of two distinct states of a target membrane-associated molecule by means of polarization microscopy, wherein the probe contains or consists of
    a) an anchoring moiety containing or consisting of at least one lipidated peptide and/or at least one transmembrane α-helical peptide,
    b) a peptide linker moiety having the length of at least 5 amino acids, wherein at least 50% of the amino acids forming the linker are selected from glycine, serine, and threonine,
    c) a fluorescent moiety, and
    d) an affinity binding moiety capable of binding the target membrane-associated molecule, wherein the moieties are arranged in the order a-b-c-d or d-c-b-a in the direction from the N-terminus to the C-terminus.
    Methods of detecting presence or absence of the target molecule, of detecting activated or inactive forms of the target molecule, and of detecting the activation of the target molecule are also described.

    LIPOPHOSPHONOXINS OF SECOND GENERATION, AND THEIR USE
    9.
    发明公开
    LIPOPHOSPHONOXINS OF SECOND GENERATION, AND THEIR USE 有权

    公开(公告)号：EP3448865A1

    公开(公告)日：2019-03-06

    申请号：EP17721044.0

    申请日：2017-04-19

    申请人： Ustav organicke chemie a biochemie AV CR, v.v.i. ,  Mikrobiologicky Ustav AV CR, v.v.i. ,  Trios, Spol. S R.O.

    发明人： REJMAN, Dominik ,  POHL, Radek ,  ZBORNIKOVA, Eva ,  KRASNY, Libor ,  LATAL, Tomas ,  KOLAR, Milan

    IPC分类号： C07F9/6558 ,  A61K31/675 ,  A61P31/04

    CPC分类号： C07F9/65586

    摘要： Lipophosphonoxins of general Formula I are described here, wherein R1 is C8-C22, preferably C10-C18 and more preferably C12-C16 alkyl, or hexadecyloxypropyl, tetradecyloxypropyl, tetradecyloxyethyl or hexadecyloxyethyl, R2 is uracil, thymine, or cytosine, R3 is selected from a group which contains compounds of general formulas II and III, wherein R4 is H, CH2OH or CH2NH2, R5 is H, OH or NH2, R6 is H, OH or NH2, R7 is H, CH2OH or CH2NH2, wherein at least one of the groups R5 and R6 must be NH2 or one of the groups R4 and R7 must be CH2NH2. R8 is H, CH2OH or CH2NH2, R9 is H, OH or NH2, R10 is H, OH or NH2, R11 is H, OH or NH2, R12 is H, CH2OH or CH2NH2, wherein at least one of the groups R9, R10 and R11 must be NH2 or one of the groups R8 a R12 must be CH2NH2. R13 is NH2 or NH-CH(NH2)NH, R14 is NH2 or NH-CH(NH2)NH, R15 is NH2 or NH-CH(NH2)NH, R16 is NH2 or NH-CH(NH2)NH. Further, diastereomers and mixtures of diastereomers of compounds of general formula I and the corresponding pharmaceutically acceptable salts and/or hydrates are described. The compounds of general formula I are useful as antibacterial agents or active ingredients in disinfectants, and/or of selective in vitro culture media.