IP Library › Granted Patent US 11,407,815
Granted Patent B2
US 11,407,815 · App. 16/560,521 · Granted Aug 9, 2022

Stabilized fibronectin based scaffold molecules

Inventor: Dasa Lipovsek (Pepperell, MA)
Assignee: BRISTOL-MYERS SQUIBB COMPANY
C07K14/78A61K47/6435C40B40/08C07K2318/20C40B40/10
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Quick Facts
Patent No.
US 11,407,815
App. No.
16/560,521
Granted
Aug 9, 2022
Kind
B2
Abstract

Provided herein are proteins comprising a fibronectin based scaffold (FBS) domain, e.g., 10 Fn3 molecules, that bind specifically to a target, and wherein the FBS domain is linked at its C-terminus to a region consisting of PmXn, wherein P is proline, X is any amino acid and wherein n is 0 or an integer that is at least 1 and m is an integer that is at least 1, and wherein the PmXn moiety provides an enhanced property to the FBS domain, e.g., enhanced stability, relative to the protein that is not linked to the PmXn moiety.

Claims (16)

1. A nucleic acid encoding a fibronectin based scaffold (FBS) protein comprising a 10 Fn3 domain, wherein the 10 Fn3 comprises an amino acid sequence that is at least 70% identical to SEQ ID NO: 1, and wherein (i) the C-terminal amino acid at the position corresponding to position 94 of SEQ ID NO: 1 is covalently linked through a peptide bond to a moiety consisting of the amino acid sequence PmXn, wherein P is proline, X is any amino acid, m is an integer that is at least 1 and n is 0 or an integer that is at least 1, and (ii) the PmXn moiety provides an enhanced property to the FBS protein relative to the FBS protein that is not linked to the PmXn moiety.

2. The nucleic acid of claim 1 , wherein the moiety consists of P (m is 1 and n is 0).

3. (Previously Presented The nucleic acid of claim 1 , wherein the moiety consists of PP (m is 2 and n is 0).

4. The nucleic acid of claim 1 , wherein the moiety consists of PmXn, wherein n is 1-150.

5. The nucleic acid of claim 1 , wherein the moiety consists of PmXn, wherein n is 1-10.

6. The nucleic acid of claim 1 , wherein the moiety consists of PmXn, wherein n is 1-5.

7. The nucleic acid of claim 1 , wherein the moiety consists of PI, PC, PID, PIE, PIDK (SEQ ID NO: 61), PIEK (SEQ ID NO: 63), PIDKP (SEQ ID NO: 65), PIEKP (SEQ ID NO: 67), PIDKPS (SEQ ID NO: 69), PIEKPS (SEQ ID NO: 71), PIDKPC (SEQ ID NO: 73), PIEKPC (SEQ ID NO: 75), PIDKPSQ (SEQ ID NO: 77), PIEKPSQ (SEQ ID NO: 79), PIDKPCQ (SEQ ID NO: 81), PIEKPCQ (SEQ ID NO: 83), PHHHHHH (SEQ ID NO: 85) or PCHHHHHH (SEQ ID NO: 87).

8. The nucleic acid of claim 1 , wherein the FBS protein comprises the amino acid sequence LEVVAA(X)uLLISW(X)vYRITY(X)wFTV(X)xATISGL(X)yYTITVY A(X)ZISINYRT (SEQ ID NO: 16), wherein (X)u, (X)v, (X)w, (X)x, (X)y and (X)z consist of the wild-type amino acid sequence (SEQ ID NO: 1) or comprise at least one amino acid difference with the corresponding wild-type sequence.

9. The nucleic acid of claim 1 , wherein PmXn is P or PC.

10. The nucleic acid of claim 1 , wherein at least one X of PmXn is a cysteine.

11. The nucleic acid of claim 10 , wherein the cysteine is conjugated to a heterologous moiety.

12. The nucleic acid of claim 1 , wherein the enhanced property conferred by the PmXn moiety is enhanced stability.

13. The nucleic acid of claim 10 , wherein the PmXn moiety is PmCXn or PmXn 1 CXn 2 , wherein C is cysteine and n 1 and n 2 are independently 0 or an integer that is at least 1.

14. The nucleic acid of claim 13 , wherein the cysteine is conjugated to a heterologous moiety.

15. A vector comprising the nucleic acid of claim 1 .

16. A host cell comprising the nucleic acid of claim 1 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 9, 2020
From: LIPOVSEK, DASA
To: BRISTOL-MYERS SQUIBB COMPANY
Reel/Frame 051469/0415 →
Continuity (4)
Continuation 15127183
Provisional Application 62084270 · Nov 25, 2014
Provisional Application 61955975 · Mar 20, 2014
Related Publication 20200062824A1 · Feb 27, 2020
Cited By (2)
US 12,529,165 US 12,534,511