US 2022/0177531 A1 · Selective and Noncovalent Inhibitors of Oncogenic RAS Mutants

Abstract

Provided are proteins or peptides, which may be referred to as monobodies. Fusion proteins and proteolysis targeting chimeras (PROTACs) comprising the proteins or peptides are also provided. Also provided are compositions of the proteins or peptides of the present disclosure, as well as compositions of fusion proteins and compositions of PROTACs. Methods of treating an individual in need of treatment are also provided. The methods may be to treat an individual suffering from or suspected of having KRAS(G12V), KRAS(G12S), KRAS(G12A) and/or KRAS(G12C)-associated cancers. A method may be for inhibiting ERK activation and/or proliferation of KRAS(G12V), KRAS(G12S), KRAS(G12A) and/or KRAS(G12C)-associated cancers.

Claims20

Dependent claims

A protein or peptide comprising:

i) the following sequence:
VSSVPTKLEVVAATPTSLLISWDAPAVTVFFYVITYGETGHGVGAFQAFKVPGSKST ATISGLKPGVDYTITVYARGYSKQGPYKPSPISINYRT (12VC1) (SEQ ID NO:1) or a truncated variant thereof;
or
ii) a variant with at least 80% homology to SEQ ID NO:1.

1 more element

A protein or peptide comprising the following sequence or a truncated variant thereof, or having the following sequence or truncated variant thereof:

XXXVPTXLEVVAATXXSLLISWDAPAVTVXFYVIXYGETGHGVGAFXAFXVXXXXS TATISGLXPGVDYTITVYARXXSKQGXYXPSPISINYRT (SEQ ID NO:26),
wherein each X is a canonical or non-canonical amino acid.

Dependencies are inferred from the claim text.

Facts

Application

17/543,464Filed 6 Dec 2021

Priority

5 Dec 2020

Published

9 Jun 2022

Term ends

Not estimatedThe source records don’t support an estimate.

Classification15 codes

C07K 14/4702
Not used: regulators; Modulating activity
A61P 35/00
Antineoplastic agents
C07K 14/78
From animals; from humans: connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
C07K 14/82
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof: translation products from oncogenes

Selective and Noncovalent Inhibitors of Oncogenic RAS Mutants

Life of this patent

Selective and Noncovalent Inhibitors of Oncogenic RAS Mutants

Life of this patent

Abstract

Claims20