Compositions and methods for increasing drug efficiency
OwnerMichael Newman, Angelo Castellino +5inventors
InventorsMichael Newman, Angelo Castellino, Joel Desharnais, Zijian Guo, Qing Li, Carlo Ballatore, Chengzao Sun
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Abstract
In one embodiment, provided herein are compositions and methods for increasing drug efficiency. In certain embodiments, the compositions contain conjugates having the formula: D-L-S wherein D is a drug moiety; L, which may or may not be present, is a non-releasing linker moiety; and S is a substrate for a protein or lipid kinase that is overexpressed, overactive or exhibits undesired activity in a target system.
Claims145
A conjugate, comprising a drug and a substrate for a protein kinase or a lipid kinase non-releasably linked thereto, optionally via a non-releasable linker, or a pharmaceutically acceptable derivative thereof.
A peptide comprising an amino acid sequence:
- Gly-Arg-Pro-Arg-Thr-Ser-Ser-
- (SEQ ID NO. 5)
- Phe-Ala-Glu-Gly;
- Gly-Arg-Pro-Arg-Thr-Ser-DSer-
- (SEQ ID NO. 1406)
- Phe-Ala-Glu-Gly;
- Gly-Arg-Pro-Arg-Ala-Ala-Ala-Phe-
- (SEQ ID NO. 1407)
- Ala-Glu-Gly;
- Arg-Ser-Arg-Thr-Ser-Ser-Phe-Ala-
- (SEQ ID NO. 1408)
- Glu-Gly;
- Gly-Arg-Ser-Arg-Thr-Ser-Ser-Phe-
- (SEQ ID NO. 1409)
- Ala-Glu-Gly;
- Arg-Pro-Arg-Thr-Ser-Ser-Phe;
- (SEQ ID NO. 6)
- Arg-Ser-Arg-Thr-Ser-Ser-Phe
- (SEQ ID NO. 1410)
- and
- Arg-Pro-Arg-Lys-Glu-Ser-Tyr,
- (SEQ ID NO. 1411)
- wherein the peptide is free from resin.
A peptide comprising an amino acid sequence:
- Tyr-Ile-Tyr-Gly-Ser-Phe-Lys;
- (SEQ ID NO. 668)
- Glu-Tyr-Ile-Tyr-Gly-Ser-Phe-Lys:
- (SEQ ID NO. 1412)
- Tyr-Ile-Tyr-Gly-Ser-Phe-Arg;
- (SEQ ID NO. 1413)
- Tyr-Ile-DTyr-Gly-Ser-Phe-Arg;
- (SEQ ID NO. 1414)
- Tyr-Ile-Phe-Gly-Ser-Phe-Arg
- (SEQ ID NO. 1415)
- Glu-Tyr-Ile-Tyr-Gly-Ser-Phe-Lys;
- (SEQ ID NO. 1416)
- Glu-Tyr-Ile-Tyr-Gly-Ser-Phe-Arg;
- (SEQ ID NO. 1417)
- Tyr-Ile-Tyr-Gly-Ser-Phe-Ser;
- (SEQ ID NO. 1418)
- Tyr-Ile-Tyr-Gly-Ser-Phe-His
- (SEQ ID NO. 1419)
- and
- Gly-Ile-Lys-Trp-His-His-Tyr.
- (SEQ ID NO. 1420)
- wherein the peptide is free from resin, with the proviso that when the peptide is Tyr-Ile-Tyr-Gly-Ser-Phe-Lys (SEQ ID NO. 668), then the N terminus is capped with a capping group.
Dependencies are inferred from the claim text.