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US 11,628,221 B2Granted
Peptide linker and combination for prodrugs activated by prostate-specific antigen
AssigneeRutgers, The State University of New Jersey
InventorsLongqin Hu, Herve Aloysius
Life of this patent
Estimating the term…
Abstract
The present disclosure is directed to a series of target-selective chemotherapeutic ester prodrugs comprising PSA-cleavable peptides that promote the delivery of free doxorubicin and other chemotherapeutic agents into the prostate and/or prostate tumors with greater efficiency.
Claims18
An ester prodrug according to Formula I:
- Formula I
- (SEQ ID NO:
- 5)
- A-B-A1a-Ser-Chg-Gln-NH-U-V-W-C(Me)2C(O)—O—C
- wherein:
- A is GABA, Glutaryl or Y;
- Y is an N-capping group;
- B is ←mGly, Ser, ←DSer-ψ[NH—CO—NH] or X;
- X is any amino acid residue;
- U is absent;
- V is O;
- W is CH2;
- Chg is cyclohexylglycine;
- and
- C is a chemotherapeutic agent or prostate disease drug.
12 more elements
A PSA-cleavable peptide according to Formula IV
- Formula IV
- (SEQ ID NO:
- 6)
- A-B-A1a-Ser-Chg-Gln-NH-U-V-W-C(Me)2C(O)—
- wherein:
- A is GABA, Glutaryl or Y;
- Y is an N-capping group;
- B is ←mGly, Ser, ←DSer-ψ[NH—CO—NH]— or X;
- X is any amino acid residue;
- U is absent;
- V is O;
- W is CH2;
- and
- Chg is cyclohexylglycine.
11 more elements
Dependencies are inferred from the claim text.