Title:
【発明の名称】ベタイドを製造するためのアミノ酸並びにベタイドライブラリーのスクリーニング方法及び製造方法
Document Type and Number:
Japanese Patent JPH10510814
Kind Code:
A
Abstract:
Compounds are provided termed "betides" which mimic peptides and which contain one or more residues of aminoglycine, C alpha -aminoalanine, aminosarcosine or the like wherein the side chain amino group has been acylated and optionally also alkylated. Generally, betides have the formula: XN-X1-X2-X3-Xm-X4-X5-X6-XC, where XN is an acyl or other N-terminal group or a peptide up to about 50 amino acids in length having such a group; XC is OH, NH2 or other C-terminal group or a peptide up to about 50 amino acids in length having such a group; and X1-X6 are each independently a betide amino acid or alpha -amino acid or des-X; and Xm is a peptide up to about 50 amino acids or des-X; provided however that at least one of X1-X6 is a betide amino acid residue having the formula: wherein Ro is H or CH3, R and R2 are H or lower alkyl, and R3 is an acyl group, an isocyanate group, an isothiocyanate group or a sulfonyl group. In methods for making betides, an aminoglycine residue can be subjected to side chain acylation, and optionally also alkylation, after it has been incorporated into a peptide intermediate. This method can be used as a valuable tool to synthesize and screen multiple substituents at one or more positions in a peptide, permitting simultaneous screening of betides which mimic peptides having a large number of natural or unnatural amino acid substituents at a particular position, and optionally both D- and L-isomers of those substituents.
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Inventors:
Revere Gene IF
Porter John S
Porter John S
Application Number:
JP51924396A
Publication Date:
October 20, 1998
Filing Date:
December 15, 1995
Export Citation:
Assignee:
The Solck Institute For Biological Studies
International Classes:
G01N33/48; C07C233/47; C07C233/56; C07C235/42; C07C271/22; C07C279/14; C07K1/04; C07K1/10; C07K7/06; C07K7/23; C07K14/575; C07K14/655; G01N33/68; A61K38/00; (IPC1-7): C07K1/10; C07K7/06; C07K7/23; C07K14/575; C07K14/655; G01N33/48; G01N33/68
Attorney, Agent or Firm:
Minoru Nakamura (6 outside)