IP Library Granted Patent US 8,420,777
Granted Patent B2
US 8,420,777 · App. 12/033,210 · Granted Apr 16, 2013

Compounds that inhibit Hsp90 protein-protein interactions with IAP proteins

Inventors: Dario C. Altieri (Worcester, MA); Janet Plescia (Meriden, CT); Whitney Salz (Acton, MA)
Assignee: University of Massachusetts
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Quick Facts
Patent No.
US 8,420,777
App. No.
12/033,210
Granted
Apr 16, 2013
Kind
B2
Abstract

Disclosed herein are compounds that inhibit Hsp90 interactions with IAP proteins, such as Survivin, XIAP, cIAP1, or cIAP2, and methods for identifying and using such compounds.

Claims (46)

1. An isolated compound that consists of a D-amino acid peptide selected from the group consisting of:

(D-Leu)-(D-Phe)-(D-Ala)-(D-Cys)-(D-Gly)-(D-Ser)-

(D-Ser)-(D-His)-(D-Lys);

(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His);

and

(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys).

2. An isolated compound that comprises the formula X-A or A-X, wherein:

A consists of a D-amino acid sequence selected from the group consisting of:

(D-Leu)-(D-Phe)-(D-Ala)-(D-Cys)-(D-Gly)-(D-Ser)-

(D-Ser)-(D-His)-(D-Lys);

(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His); 

and

(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys); 

and

X consists of an internalization peptide sequence of a protein selected from the group consisting of: Tat, Antennapedia, VP22, Pep-1, and transportan, or a retro-inverso version of said internalization peptide sequence.

3. The compound of claim 2 , wherein the compound comprises a D-amino acid sequence selected from:

(D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-

(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-

(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Cys)-(D-Gly)-

(D-Ser)-(D-Ser)-(D-His);

(D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-

(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-

(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Leu)-(D-Phe)-

(D-Ala)-(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-

(D-Lys);

and

(D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-

(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-

(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Gly)-(D-Ser)-

(D-Ser)-(D-His)-(D-Lys).

4. A composition comprising the compound:

Biotin-X-(D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-

(D-Arg)-(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-

(D-Val)-(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Leu)-

(D-Phe)-(D-Ala)-(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-

(D-His)-(D-Lys)-CONH 2 ,

wherein X indicates a hexanoic acid spacer and CONH 2 indicates amidation of the carboxy terminus.

5. The compound of claim 1 , wherein the compound consists of the D-amino acid peptide (D-Leu)-(D-Phe)-(D-Ala)-(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys).

6. The compound of claim 3 , wherein the compound comprises the D-amino acid sequence (D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Leu)-(D-Phe)-(D-Ala)-(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys).

7. The compound of claim 1 , wherein the compound consists of the D-amino acid peptide (D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His).

8. The compound of claim 3 , wherein the compound comprises the D-amino acid sequence (D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His).

9. The compound of claim 1 , wherein the compound consists of the D-amino acid peptide (D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys).

10. The compound of claim 3 , wherein the compound comprises the D-amino acid sequence (D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys).

11. The compound of claim 6 , wherein the compound consists of the D-amino acid peptide (D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Leu)-(D-Phe)-(D-Ala)-(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys).

12. The compound of claim 8 , wherein the compound consists of the D-amino acid peptide (D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Cys)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His).

13. The compound of claim 10 , wherein the compound consists of the D-amino acid peptide (D-Lys)-(D-Lys)-(D-Trp)-(D-Lys)-(D-Met)-(D-Arg)-(D-Arg)-(D-Asn)-(D-Gln)-(D-Phe)-(D-Trp)-(D-Val)-(D-Lys)-(D-Val)-(D-Gln)-(D-Arg)-(D-Gly)-(D-Ser)-(D-Ser)-(D-His)-(D-Lys).

Assignments (3)
CONFIRMATORY LICENSE Recorded Apr 30, 2013
From: UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 030315/0800 →
CONFIRMATORY LICENSE Recorded May 6, 2009
From: UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 022642/0808 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2008
From: ALTIERI, DARIO C.; PLESCIA, JANET; SALZ, WHITNEY
To: UNIVERSITY OF MASSACHUSETTS
Reel/Frame 020553/0005 →
Continuity (3)
Division 11187230 · Jul 22, 2005
Provisional Application 60590584 · Jul 23, 2004
Related Publication 20080171693A1 · Jul 17, 2008