Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
AssigneeYale University
InventorsCraig M. Crews, Hyun Seop Tae, Ashley R. Schneekloth, Taavi Neklesa, Thomas Sundberg
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Abstract
The present invention includes compounds that are useful in perturbing or disrupting the function of a transmembrane or intracellular protein, whereby binding of a compound to the transmembrane or intracellular protein induces proteasomal degradation of the transmembrane or intracellular protein. The present invention further includes a method of inducing proteasomal degradation of a transmembrane or intracellular protein. The present invention further includes a method of identifying or validating a protein of interest as a therapeutic target for treatment of a disease state or condition.
Claims5
A compound of formula:
- HYD-LR,
- wherein HYD is a hydrophobic group selected from the group consisting of HTL-13, HTL-34 and HTL-35:
- wherein LR is a linker group having a reactive moiety selected from the group consisting of:
- and
- wherein the reactive moiety is capable of forming a covalent link between the HYD group and a target protein of interest.
Dependencies are inferred from the claim text.