US2010168034A1PendingUtilityA1

Peptide having cell membrane penetrating activity

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Assignee: UNIV EWHA IND COLLABORATIONPriority: Feb 20, 2006Filed: Feb 20, 2007Published: Jul 1, 2010
Est. expiryFeb 20, 2026(expired)· nominal 20-yr term from priority
Inventors:Kyunglim LeeMoonhee KimMiyoung KimYoungjoo Kwon
A61P 43/00C07K 14/435C07K 7/06A61K 47/64A61K 47/65C07K 14/47C07K 14/46C07K 16/18C07K 7/08A61K 48/0008C07K 7/00
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Claims

Abstract

The present invention provides a peptide having cell membrane penetrating activity, a transmembrane carrier comprising the peptide having cell membrane penetrating activity as an effective component, a transmembrane complex consisting of the peptide having cell membrane penetrating activity combined with a target substance, a transfection kit comprising the peptide having cell membrane penetrating activity and the target substance, use of the peptide having cell membrane penetrating activity for the manufacture of a transmembrane complex, use of the transmembrane complex for the manufacture of a medicament, and a method for delivering a target substance into cell interior which comprises administrating to a subject with a transmembrane complex consisting of the peptide having cell membrane penetrating activity combined with a target substance to induce transduction of the transmembrane complex into cell interior. The peptide having cell membrane penetrating activity of the present invention has a prominent penetrating efficiency as compared with the activities of prior TAT-derived peptides and so the peptide has applications on intracellular delivery in various research fields as well as on therapeutics of specific diseases where targeting of drugs is required at high efficiency. Accordingly, the peptide having cell membrane penetrating activity, the transmembrane complex consisting of the peptide combined with a target substance and the method for delivering a target substance into cell interior using the transmembrane complex of the present invention are very useful as drug delivery systems.

Claims

exact text as granted — not AI-modified
1 . A peptide having cell membrane penetrating activity, composed of the following amino acid sequence:
 R1-R2-R3-R4-R5-R6-R7-R8-R9-R10   In the above formula,   R1 may be deleted or one amino acid selected from M, A, Q, C, F, L or W,   R2 may be deleted or one amino acid selected from I or A,   R3 may be one amino acid selected from I or A,   R4 may be one amino acid selected from Y, A, F, S or R,   R5 may be one amino acid selected from R, A or K,   R6 may be one amino acid selected from D, A, I or R,   R7 may be deleted or one amino acid selected from L, K, A, E or R,   R8 may be deleted or one amino acid selected from I, K or A,   R9 may be deleted or one amino acid selected from A, S, E, Y or T,   R10 may be deleted or one amino acid selected from A, H, K or E, and   if R10 is K or H, the amino acid(s) selected from K, KK, R, RR or HH may be added thereto.   
     
     
         2 . The peptide having cell membrane penetrating activity according to  claim 1 , wherein the amino acid sequence is SEQ ID No.: 1 
     
     
         3 . The peptide having cell membrane penetrating activity according to  claim 1 , wherein the amino acid sequence is one selected from SEQ ID No.: 2, SEQ ID No.: 3, SEQ ID No.: 4, SEQ ID No.: 5, SEQ ID No.: 6, SEQ ID No.: 7 or SEQ ID No.: 13. 
     
     
         4 . The peptide having cell membrane penetrating activity according to  claim 1 , wherein the amino acid sequence is one selected from SEQ ID No.: 20, SEQ ID No.: 21, SEQ ID No.: 22, SEQ ID No.: 23, SEQ ID No.: 24, SEQ ID No.: 25, SEQ ID No.: 26, SEQ ID No.: 27, SEQ ID No.: 28, SEQ ID No.: 29, SEQ ID No.: 30, SEQ ID No.: 31, SEQ ID No.: 32, SEQ ID No.: 33, SEQ ID No.: 34, SEQ ID No.: 35, SEQ ID No.: 36, SEQ ID No.: 37, SEQ ID No.: 38, SEQ ID No.: 39, SEQ ID No.: 40, SEQ ID No.: 41, SEQ ID No.: 42, SEQ ID No.: 43, SEQ ID No.: 44, SEQ ID No.: 45, SEQ ID No.: 46, SEQ ID No.: 47, SEQ ID No.: 48, SEQ ID No.: 49, SEQ ID No.: 50, SEQ ID No.: 51, SEQ ID No.: 52, SEQ ID No.: 53 or SEQ ID No.: 54. 
     
     
         5 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 22. 
     
     
         6 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 26. 
     
     
         7 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 27. 
     
     
         8 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 31. 
     
     
         9 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 32. 
     
     
         10 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 33. 
     
     
         11 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 34. 
     
     
         12 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 35. 
     
     
         13 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 36. 
     
     
         14 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 37. 
     
     
         15 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 38. 
     
     
         16 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 39. 
     
     
         17 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 40. 
     
     
         18 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 41. 
     
     
         19 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 42. 
     
     
         20 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 43. 
     
     
         21 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 44. 
     
     
         22 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 45. 
     
     
         23 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 46. 
     
     
         24 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 47. 
     
     
         25 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 48. 
     
     
         26 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 49. 
     
     
         27 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 50. 
     
     
         28 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 51. 
     
     
         29 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 52. 
     
     
         30 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 53. 
     
     
         31 . The peptide having cell membrane penetrating activity according to  claim 4 , wherein the amino acid sequence is SEQ ID No.: 54. 
     
     
         32 . A transmembrane carrier comprising the peptide having cell membrane penetrating activity according to  claim 1  as an effective component. 
     
     
         33 . A transmembrane complex consisting of the peptide having cell membrane penetrating activity according to  claim 1  combined with a target substance. 
     
     
         34 . The transmembrane complex of  claim 33 , wherein the target substance is one or more selected from nucleic acid, drug, chemical compound, carbohydrate, lipid, glycolipid, enzyme, regulating factor, growth factor or antibody. 
     
     
         35 . A transfection kit comprising the peptide having cell membrane penetrating activity according to  claim 1  and a target substance. 
     
     
         36 . The transfection kit of  claim 35 , wherein the transfection kit further comprises a binding factor combining the peptide with the target substance. 
     
     
         37 . Use of the peptide having cell membrane penetrating activity according to  claim 1  for the manufacture of a transmembrane complex. 
     
     
         38 . A method for preparing a transmembrane complex by combining a target substance with the peptide having cell membrane penetrating activity according to  claim 1 . 
     
     
         39 . Use of a transmembrane complex consisting of the peptide having cell membrane penetrating activity according to  claim 1  combined with a target substance for the manufacture of a medicament. 
     
     
         40 . A method for manufacturing a medicament which comprises mixing a transmembrane complex consisting of the peptide having cell membrane penetrating activity according to  claim 1  combined with a target substance, with a pharmaceutically acceptable carrier. 
     
     
         41 . A method for delivering a target substance into cell interior which comprises administrating to a subject with a transmembrane complex consisting of the peptide having cell membrane penetrating activity according to  claim 1  combined with a target substance to induce transduction of the transmembrane complex into cell interior. 
     
     
         42 . A nucleic acid cording one amino acid sequence selected from SEQ ID No.: 1, 2, 22, 26, 27, or 31-54. 
     
     
         43 . The nucleic acid of  claim 42 , wherein the nucleic acid is one selected from SEQ ID No.: 17, 18, or 55-81 respectively.

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