US 10,500,288 B2 · Cytotoxic HEXIM1 peptides and uses thereof

Abstract

Disclosed are isolated cytotoxic peptides having similar sequences as the basic region (BR) of Hexamethylene Bisacetamide Inducible Protein 1 (HEXIM1). Preferred embodiments include QLGKKKHRRRPSKKKRHW (SEQ ID No: 3). QLGRRRHRRRPSRRRRHW (SEQ ID No: 4) and QLGKKILAARPSKKKRHW (SEQ ID No: 5). Also encompassed are isolated nucleic acid molecules encoding for the claimed peptides, vectors comprising the isolated nucleic acids, compositions comprising peptides conjugated to cell-targeting or penetrating peptides or antibodies, nucleic acid molecules or vectors expressing conjugates thereof; methods of treating or preventing diseases or conditions, including cancers and obesity as well as a method of eliminating undifferentiated stem cells.

Claims9

Dependent claims

A recombinant peptide comprising a cytotoxic peptide and an internalizing peptide, wherein the cytotoxic peptide is conjugated to the internalizing peptide, and wherein the cytotoxic peptide is represented by the consensus sequence Q1-L2-G3-X4-X5-X6-X7-X8-X9-R10-P11-S12-X13-X14-X15-R16-H17-W18 (SEQ ID NO:

36),
wherein,
i) each of X4, X5, and X6 is any amino acid;
ii) X7 is histidine or leucine;
iii) X8 and X9 are independently K or R or H or A;
and
iv) X13, X14 and X15 are independently K or R or H;
and, wherein the internalizing peptide is a cancer cell-targeting peptide selected from the group consisting of arginine-glycine-aspartic acid (RGD), asparagine-glycine-arginine (NGR), TCP-1 phage peptide (TCP-1) and any one of the peptides of SEQ ID Nos:
8-11, 64-789 and 795-798.

6 more elements

Dependencies are inferred from the claim text.

Facts

Application

15/555,482Filed 3 Mar 2016

Priority

SG 10201501642V4 Mar 2015

Published

US 2018/0243441 A130 Aug 2018

Granted

10 Dec 2019

Term ends

Not estimatedThe source records don’t support an estimate.

Classification17 codes

A61K 47/6931
The form being a nanoparticle, e.g. an immuno-nanoparticle: the material constituting the nanoparticle being a polymer
A61K 38/04
Medicinal preparations containing peptides: peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
A61K 47/66
The modifying agent being a protein, peptide or polyamino acid: the modifying agent being a pre-targeting system involving a peptide or protein…
A61K 47/6851
The modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site: the antibody targeting a determinant of a…

Cytotoxic HEXIM1 peptides and uses thereof

Life of this patent

Cytotoxic HEXIM1 peptides and uses thereof

Life of this patent

Abstract

Claims9