Epidermal growth factor receptor inhibitors
AssigneeFilamon Ltd
InventorsTimothy MANN, Jun ZENG, Kieran SCOTT
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Abstract
The present disclosure generally relates to epidermal growth factor receptor (EGFR) inhibitors and methods of treating EGFR-dependent or associated diseases, disorders or conditions, such as cancer.
Claims32
A cyclic peptide comprising the sequence of the formula:
- Xaa1-Xaa2-Xaa3-Xaa4-Xaa5
- in which:
- Xaa1 is F or 1NapA;
- Xaa2 is L or I;
- Xaa3 is S or T;
- Xaa4 is F or 2NapA;
- and
- Xaa5 is R or K.
(canceled)
(canceled)
A method of promoting internalisation and/or lysosomal degradation of EGFR in a cell, said method including the step of contacting the cell with an effective amount of a cyclic peptide comprising the sequence of the formula:
- Xaa1-Xaa2-Xaa3-Xaa4-Xaa5
- in which:
- Xaa1 is F or 1NapA;
- Xaa2 is L or I;
- Xaa3 is S or T;
- Xaa4 is F or 2NapA;
- and
- Xaa5 is R or K;
- or a pharmaceutically acceptable salt, solvate or prodrug thereof, to thereby promote internalisation and/or lysosomal degradation of EGFR in the cell.
17-20. (canceled)
A method of identifying, designing or producing an agent capable of interacting with or binding to a ligand binding domain of EGFR, said method including the steps of:
- (a) contacting a cell expressing EGFR with a candidate agent, wherein the candidate agent is a derivative, variant or analogue of:
- (i) cyclo-((2-Nal)-Leu-Ser-(2-Nal)-Arg);
- or (ii) a cyclic peptide of the formula:
- Xaa1-Xaa2-Xaa3-Xaa4-Xaa5
- in which:
- Xaa1 is F or 1NapA;
- Xaa2 is L or I;
- Xaa3 is S or T:
- Xaa4 is F or 2NapA;
- and
- Xaa5 is R or K;
- or a pharmaceutically acceptable salt, solvate or prodrug thereof;
- and
- (b) determining whether the candidate agent inhibits the binding of an EGFR ligand to EGFR of the cell.
22-29. (canceled)
Dependencies are inferred from the claim text.