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Synthesis and activity of dipeptides, linked to targeting ligands, as specific NK cell enhancers.

Abstract：

:Water soluble analogues of the lipophilic immunostimulant, octadecyl D-alanyl-L-glutamine, BCH-527, were synthesized and evaluated for the ability to stimulate natural killer (NK) cells. One of these compounds in which the octadecyl chain of BCH-527 was replaced with a shorter chain alcohol, 6-(D-alanyl-L-glutaminylamino)hexan-1-ol, 9, displayed an in vitro stimulation of NK cells comparable to that of interleukin 2 (IL 2). However, when the hydroxyl of 9 was linked to L-fucose to yield 1-beta-[6-(D-alanyl-L-glutaminylamino)hex-1-yl]-L- fucopyranose (BCH-2537, 1), the observed stimulation of NK cells was greater than that observed with IL 2. Further evaluation of these compounds revealed that the improved in vitro activity of BCH-2537 was more pronounced in vivo. That is, while both compounds significantly increased splenic NK cells, only BCH-2537 significantly increased the activity of these cells in vivo. In terms of a structure-activity relationship, NK cell activity was sensitive to minor structural modifications. It was influenced by conservative substitutions within the dipeptide, the length of the hydrocarbon chain, and the functionality at the end of the chain. No other compound enhanced NK cell activity to the extent exhibited by BCH-2537, although a few were equipotent to 9.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Abbott SD,Gagnon L,Lagraoui M,Kadhim S,Attardo G,Zacharie B,Penney CL

doi

10.1021/jm970734v

subject

Has Abstract

pub_date

1998-05-21 00:00:00

pages

1909-26

issue

11

eissn

0022-2623

issn

1520-4804

pii

jm970734v

journal_volume

41

pub_type

杂志文章

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