US2020323943A1PendingUtilityA1

Malignant tumor target peptide

Assignee: AISTPriority: Aug 16, 2016Filed: Jun 25, 2020Published: Oct 15, 2020
Est. expiryAug 16, 2036(~10.1 yrs left)· nominal 20-yr term from priority
C08G 69/08C07K 7/06A61P 35/00A61K 38/06C07K 19/00A61K 49/0056C07K 5/08C12N 15/09A61K 49/06A61K 38/03C07K 5/10C07K 14/4721A61K 49/14A61K 45/00A61K 51/08C07K 14/00C07K 5/0821A61K 49/04A61K 47/64C07K 7/08A61K 49/085C07K 5/0812
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Claims

Abstract

The present invention provides a peptide comprising the amino acid sequence of any of the formulas (I)-(III) below: (I) an amino acid sequence of (X1) [D] P [D] (X2) [D] wherein X1 is W or F, X2 is S or T, and each amino acid symbol immediately followed by symbol [D] is a D form of the amino acid, (II) an amino acid sequence of P[D]T[D] (X) n F[D] wherein (X) n is any amino acid in the number of n selected independently of each other, n is an integer of 0-4, and the symbol [D] is as defined above, (III) an amino acid sequence that is a Retro-inverso of the amino acid sequence of any of the aforementioned (I) and the aforementioned (II); and a conjugate containing the peptide and a functional part.

Claims

exact text as granted — not AI-modified
1 . A peptide comprising the amino acid sequence of any of the following (i)-(vi):
 (i) an amino acid sequence of L[D] R[D] F[D] P[D] T[D]V[D] L[D],   (ii) an amino acid sequence of L[D] L[D] S[D] W[D] P[D]S[D] A[D],   (iii) an amino acid sequence of S[D] P[D] T[D] S[D] L[D]L[D] F[D],   (iv) an amino acid sequence of M[D] P[D] T[D] L[D] T[D]F[D] R[D],   (v) an amino acid sequence of any of (i)-(iv), in which 1 or several amino acids are inserted, substituted or deleted, or these are combined, and   (vi) an amino acid sequence that is a Retro-inverso of the amino acid sequence of any of (i)-(v),   wherein each amino acid symbol immediately followed by symbol [D] is a D form of the amino acid.   
     
     
         2 . The peptide according to  claim 1 , consisting of the amino acid sequence of any of the following (i)-(vi):
 (i) an amino acid sequence of L[D] R[D] F[D] P[D] T[D]V[D] L[D],   (ii) an amino acid sequence of L[D] L[D] S[D] W[D] P[D]S[D] A[D],   (iii) an amino acid sequence of S[D] P[D] T[D] S[D] L[D]L[D] F[D],   (iv) an amino acid sequence of M[D] P[D] T[D] L[D] T[D]F[D] R[D],   (v) an amino acid sequence of any of (i)-(iv), in which 1 or several amino acids are inserted, substituted or deleted, or these are combined, and   (vi) an amino acid sequence that is a Retro-inverso of the amino acid sequence of any of (i)-(v),   wherein each amino acid symbol immediately followed by symbol [D] is a D form of the amino acid.   
     
     
         3 . A conjugate comprising the peptide according to  claim 1  linked to one other component. 
     
     
         4 . The conjugate according to  claim 3 , wherein the one other component is an anticancer agent. 
     
     
         5 . The conjugate according to  claim 4 , wherein the anticancer agent is selected from the group consisting of an antimetabolite, an alkylating agent, an anticancer antibiotic, a microtubule inhibitor, a platinum preparation, a topoisomerase inhibitor, a molecular targeting agent, and an anti-angiogenic agent. 
     
     
         6 . The conjugate according to  claim 3 , wherein the one other component is a detectable substance. 
     
     
         7 . The conjugate according to  claim 6 , wherein the detectable substance enables detection of the conjugate in vivo by a means selected from the group consisting of X-ray photography, computed tomography (CT), nuclear magnetic resonance imaging (MRI), ultrasonography, scintigraphy, positron emission tomography (PET), endoscopy and laparoscopy. 
     
     
         8 . The conjugate according to  claim 6 , wherein the detectable substance is a radioisotope, an MRI enhancer, a radiopaque substance, a contrast agent or a fluorescent substance. 
     
     
         9 . The conjugate according to  claim 7 , wherein the detectable substance is a radioisotope, an MRI enhancer, a radiopaque substance, a contrast agent or a fluorescent substance. 
     
     
         10 . A composition comprising the peptide according to  claim 1  and a pharmacologically acceptable carrier.

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