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    PEPTIDES BINDING TO HYPOXIA INDUCIBLE FACTORS AND THEIR USE
    1.
    发明申请
    PEPTIDES BINDING TO HYPOXIA INDUCIBLE FACTORS AND THEIR USE 审中-公开

    公开(公告)号：WO2022180410A1

    公开(公告)日：2022-09-01

    申请号：PCT/GB2022/050523

    申请日：2022-02-25

    Applicant: UNIVERSITY OF SOUTHAMPTON

    Inventor： TAVASSOLI, Ali

    IPC: C07K5/083

    Abstract: The present invention provides a series of tripeptides according to the compound of formula (I) that inhibit the interaction of both HIF-1α and HIF-2α with HIf-1 β by binding to the PAS-B domain of the α subunit of HIF. The tripeptides and methods disclosed herein are useful in treating diseases or conditions that involve the response to hypoxia.

    HIF-1 AND HIF-2 INHIBITORS
    3.
    发明申请
    HIF-1 AND HIF-2 INHIBITORS 审中-公开
    HIF-1和HIF-2抑制剂

    公开(公告)号：WO2017129997A1

    公开(公告)日：2017-08-03

    申请号：PCT/GB2017/050220

    申请日：2017-01-27

    Applicant: UNIVERSITY OF SOUTHAMPTON

    Inventor： TAVASSOLI, Ali

    IPC: C07K7/06 ,  C07K14/47 ,  G01N33/68

    CPC classification number: C07K7/06 ,  C07K14/4702 ,  G01N33/6845 ,  G01N2500/02

    Abstract: The present invention relates to inhibitors of HIF-1 and HIF-2 and uses thereof. The present invention further relates to the inhibitors for use in treatment of diseases. An isolated polypeptide is provided, that prevents dimerization of HIF-1 α with HIF-1 β and HIF-2α with HIF-1 β and/or inhibits the activity of HIF-1 and HIF-2, wherein the polypeptide comprises the amino acid sequence C-X1-X2-X3-Z-X4 (SEQ ID NO 1) and wherein XI, X2, X3 and X4 are any amino acid and wherein Z is leucine, valine of isoleucine or a non-natural derivative or leucine, valine or isoleucine. The isolated polypeptide prevents dimerization of HIF-1 α with HIF-1 β and HIF-2α with HIF-1 β and inhibits the activity of HIF-1 and HIF-2 by binding to HIF-1 α or HIF-1 β and/or HIF-2α or HIF-Ιβ.

    Abstract translation: 本发明涉及HIF-1和HIF-2的抑制剂及其用途。 本发明进一步涉及用于治疗疾病的抑制剂。 提供了分离的多肽，其防止HIF-1α与HIF-1β和HIF-2α与HIF-1β的二聚化和/或抑制HIF-1和HIF-2的活性，其中多肽包含氨基酸 序列C-X1-X2-X3-Z-X4（SEQ ID NO1），并且其中X1，X2，X3和X4是任何氨基酸，并且其中Z是亮氨酸，异亮氨酸的缬氨酸或非天然衍生物或亮氨酸，缬氨酸 或异亮氨酸。 分离的多肽阻止HIF-1α与HIF-1β和HIF-2α与HIF-1β二聚化，并通过与HIF-1α或HIF-1β和/或HIF-1β结合而抑制HIF-1和HIF- 或HIF-2α或HIF-1β。

    PEPTIDE
    4.
    发明申请
    PEPTIDE 审中-公开

    公开(公告)号：WO2021123789A1

    公开(公告)日：2021-06-24

    申请号：PCT/GB2020/053263

    申请日：2020-12-17

    Applicant: UNIVERSITY OF SOUTHAMPTON

    Inventor： TAVASSOLI, Ali

    IPC: C12N15/10 ,  C12N15/1093

    Abstract: The invention provides a non-toxic method for producing cyclic peptides within a mammalian cell, comprising the steps of a) introducing a vector into the mammalian cell, wherein the vector comprises a construct encoding a C-terminus intein domain, a polypeptide sequence to be cyclised, an N-terminus intein domain, and a degradation tag, wherein the degradation tag is attached to at least one intein domain, and b) expressing the construct to produce an intermediate comprising an active intein and the polypeptide sequence, wherein the active intein, once formed, undergoes splicing and cyclises the polypeptide and wherein the degradation tag degrades the active intein. The invention further provides a cyclic peptide library produced according to this method, and the incorporation of the non-toxic cyclic peptide-producing construct of the above method into a genetic construct, a vector, or a mammalian cell.

    METHODS FOR GENERATING AND SCREENING COMPARTMENTALISED PEPTIDE LIBRARIES
    5.
    发明申请
    METHODS FOR GENERATING AND SCREENING COMPARTMENTALISED PEPTIDE LIBRARIES 审中-公开

    公开(公告)号：WO2018154021A1

    公开(公告)日：2018-08-30

    申请号：PCT/EP2018/054443

    申请日：2018-02-22

    Applicant: UNIVERSITY OF SOUTHAMPTON

    Inventor： TAVASSOLI, Ali ,  SOHRABI, Catrin ,  FISCHLECHNER, Martin

    IPC: G01N33/50 ,  C07K7/64 ,  C07K14/00

    Abstract: A method for co-compartmentalising a cyclic polypeptide with a polynucleotide encoding the cyclic polypeptide, comprising the steps of a) forming a compartment containing a polynucleotide encoding the cyclic polypeptide, b) expressing a polypeptide from the polynucleotide, and c) cyclising the polypeptide. Co-compartmentalised cyclic polypeptides and encoding polynucleotides. Libraries of co-compartmentalised cyclic polypeptide and encoding polynucleotide. Methods for screening libraries of co-compartmentalised cyclic polypeptide and encoding polynucleotide. Incorporation of non-canonical nucleic acids into such libraries.

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