University of Southampton

Ali Tavassoli

Catrin Sohrabi

Martin Fischlechner

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.

Methods for generating and screening compartmentalised peptide libraries

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&#x3b1; with HIF-1&#x3b2; and HIF-2&#x3b1; with HIF-1&#x3b2; 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-1&#x3b1; with HIF-1&#x3b2; and HIF-2&#x3b1; with HIF-1&#x3b2; and inhibits the activity of HIF-1 and HIF-2 by binding to HIF-1&#x3b1; or HIF-1&#x3b2; and/or HIF-2&#x3b1; or HIF-1&#x3b2;.

HIF-1 and HIF-2 inhibitors

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&#x3b1; with HIF-1&#x3b2; and HIF-2&#x3b1; with HIF-1&#x3b2; 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-1&#x3b1; with HIF-1&#x3b2; and HIF-2&#x3b1; with HIF-1&#x3b2; and inhibits the activity of HIF-1 and HIF-2 by binding to HIF-1&#x3b1; or HIF-1&#x3b2; and/or HIF-2&#x3b1; or HIF-1&#x3b2;.

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Southampton, United Kingdom

Ali Tavassoli