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Anti-arthritic effects of the novel dipeptidyl peptidase IV inhibitors TMC-2A and TSL-225.

作者信息

Tanaka S, Murakami T, Nonaka N, Ohnuki T, Yamada M, Sugita T

机构信息

Discovery Research Laboratory, Osaka, Japan.

出版信息

Immunopharmacology. 1998 Jul;40(1):21-6. doi: 10.1016/s0162-3109(98)00014-9.

DOI:10.1016/s0162-3109(98)00014-9
PMID:9776475
Abstract

We evaluated the immunopharmacological effects of two novel dipeptidyl peptidase IV (DP IV) inhibitors, TMC-2A [(2S,2S',2S'')-2-[2'-[2''-amino-3''-(-indol-3'''-yl)-1''-oxopropyl]-1',2 ',3',4'-tetrahydro-6',8'-dihydroxy-7'-methoxyisoquinol-3-yl-car bonylamino]-4-hydroxymethyl-5-hydroxypentanoic acid] and TSL-225 (tryptophyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid). TMC-2A, produced by Aspergillus sp. A374, inhibited rat kidney DP IV uncompetitively, with a Ki value of 5.3 microM. In vivo, TMC-2A suppressed alkyldiamine (N,N-dioctadecyl-N',N-bis(2-hydroxyethyl)propanediamine)-induced arthritis. We developed a chemically modified inhibitor, TSL-225, with potency similar to that of TMC-2A. TSL-225 inhibited DP IV uncompetitively, with a Ki value of 3.6 microM. TSL-225 was also effective against adjuvant-induced arthritis. These results suggest that TMC-2A and its derivatives may have therapeutic potential for the treatment of inflammatory diseases such as rheumatoid arthritis.

摘要

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