Pan-HER antagonists and methods of use
AssigneeMolecular Logix, Inc.
InventorsPhilip Pienkos, Daniel Monticello
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Abstract
The present invention features human epidermal receptor (HER) antagonists. These antagonists are polypeptide variants of ligands of HER. The HER ligand polypeptide variants of the invention possess Pan-HER antagonistic properties and can inhibit at least one HER-mediated biological activity of one or more HER subtypes, such as inhibition of the receptor's kinase activation activity and subsequently, cell proliferation. Such polypeptide variants, and nucleic acids encoding these polypeptide variants can be used therapeutically in situations in which inhibition of HER activity is indicated.
Claims38
A human epidermal receptor (HER)-ligand polypeptide variant comprising a HER ligand polypeptide in which the amino acid position that corresponds to amino acid Gly 39 of human wild-type epidermal growth factor (EGF) is substituted with another amino acid, wherein the HER ligand polypeptide further comprises at least one substituted domain, and wherein the variant has at least one Pan-HER antagonist activity.
A human epidermal receptor (HER)-ligand polypeptide variant having at least one Pan-HER antagonist activity wherein the variant comprises a mutation that disrupts binding via Domain I and/or III.
Dependencies are inferred from the claim text.