Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis

Yim Victor; Noisier Anais F. M.; Hung Kuo-yuanBartsch Joerg W.Schlomann UweBrimble Margaret A.

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Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis

机译：Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis

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The metalloproteinase ADAM8 serves as a pivotal catalyst in the development of inflammatory diseases and cancer metastasis. The cyclic peptide cyclo(RLsKDK) has been shown to inhibit the enzymatic activity of ADAM8 with high specificity and potency. Herein we report a structure-activity relationship (SAR) study of cyclo(RLsKDK) that involves the synthesis and biological evaluation of the lead compound and structural analogues thereof. This study provides insight into the ligand-receptor interactions that govern the binding of cyclo(RLsKDK) to the ADAM8 disintegrin domain and represents a stepping stone for the development of new treatments for inflammatory diseases and cancer metastasis. (C) 2016 Elsevier Ltd. All rights reserved.

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《Bioorganic and medicinal chemistry》 |2016年第18期|4032-4037|共6页
作者
Yim Victor; Noisier Anais F. M.; Hung Kuo-yuanBartsch Joerg W.Schlomann UweBrimble Margaret A.;
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作者单位

Univ Marburg, Univ Hosp, Dept Neurosurg, Baldingerstr, D-35053 Marburg, Germany;

Univ Auckland, Sch Biol Sci, 3a Symonds St, Auckland Cent 1010, New Zealand;

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正文语种英语
中图分类药学;
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ADAM8 inhibitors; Cancer metastasis; Cyclic peptides; Peptidomimetics; SAR study;

Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis

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