公开(公告)号：US11644469B2

公开(公告)日：2023-05-09

申请号：US17194522

申请日：2021-03-08

Applicant: UNIVERSITY OF SOUTHAMPTON

Inventor： Ali Tavassoli

IPC: A61K38/18 ,  A61K38/08 ,  A61P35/00 ,  C07K14/47 ,  C07K7/06 ,  C07K7/02 ,  G01N33/68

CPC classification number: G01N33/6845 ,  A61K38/08 ,  A61K38/18 ,  A61P35/00 ,  C07K7/02 ,  C07K7/06 ,  C07K14/4702 ,  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-1α with HIF-1β and HIF-2α with HIF-1β 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 X1, 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-1α with HIF-1β and HIF-2α with HIF-1β and inhibits the activity of HIF-1 and HIF-2 by binding to HIF-1α or HIF-1β and/or HIF-2α or HIF-1β.

公开(公告)号：US10962549B2

公开(公告)日：2021-03-30

申请号：US16072803

申请日：2017-01-27

Applicant: University of Southampton

Inventor： Ali Tavassoli

IPC: A61K38/18 ,  A61K38/08 ,  A61P35/00 ,  C07K14/47 ,  C07K7/06 ,  C07K7/02 ,  G01N33/68

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-1α with HIF-1β and HIF-2α with HIF-1β 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 X1, 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-1α with HIF-1β and HIF-2α with HIF-1β and inhibits the activity of HIF-1 and HIF-2 by binding to HIF-1α or HIF-1β and/or HIF-2α or HIF-1β.

公开(公告)号：US20190322998A1

公开(公告)日：2019-10-24

申请号：US15499841

申请日：2017-04-27

Applicant: University of Southampton

Inventor： Ali Tavassoli

IPC: C12N15/10

Abstract: Disclosed herein are methods of synthesising a double stranded polynucleotide, the methods including providing a set of self-templating oligonucleotides wherein the set of self-templating oligonucleotides encodes a double stranded polynucleotide sequence of interest; annealing the oligonucleotides together so that they form the double stranded polynucleotide sequence with the oligonucleotides in the correct order and adjacent oligonucleotides in the same strand close enough to each other that a covalent bond could form between the 5′ end of one oligonucleotide and the 3′ end of an adjacent oligonucleotide; and covalently bonding the backbones of adjacent oligonucleotides in the same strand to each other so that a covalent bond is formed between the 5′end of an oligonucleotide to the 3′end of the adjacent oligonucleotide to provide the double stranded polynucleotide of interest, wherein the covalent bonds between adjacent oligonucleotides can be read-through accurately by a DNA polymerase or an RNA polymerase.

公开(公告)号：US20190033318A1

公开(公告)日：2019-01-31

申请号：US16072803

申请日：2017-01-27

Applicant: University of Southampton

Inventor： Ali Tavassoli

IPC: G01N33/68 ,  C07K14/47 ,  A61K38/08 ,  C07K7/02 ,  A61P35/00 ,  A61K38/18 ,  C07K7/06

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-1α with HIF-1β and HIF-2α with HIF-1β 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 X1, 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-1α with HIF-1β and HIF-2α with HIF-1β and inhibits the activity of HIF-1 and HIF-2 by binding to HIF-1α or HIF-1β and/or HIF-2α or HIF-1β.