Thrombospondin-1 Mimetic Agonist Peptides Induce Selective Death in Tumor Cells: Design, Synthesis, and Structure-Activity Relationship Studies

被引：19

作者：

Denefle, Thomas ^{[1
,2
,3
]}

Boullet, Heloise ^{[1
,2
]}

Herbi, Linda ^{[4
,5
,6
]}

Newton, Clara ^{[1
,2
,3
]}

Martinez-Torres, Ana-Carolina ^{[4
,5
,6
]}

Guez, Alexandre ^{[1
,2
]}

Pramil, Elodie ^{[1
,2
,4
,5
,6
]}

Quiney, Claire ^{[4
,5
,6
]}

Pourcelot, Marilyne ^{[1
,2
,3
]}

Levasseur, Mikail D. ^{[1
,2
,3
]}

Larde, Eva ^{[1
,2
,3
]}

Moumne, Roba ^{[1
,2
]}

Ogi, Francois-Xavier ^{[8
]}

Grondin, Pascal ^{[9
]}

Merle-Beral, Helene ^{[4
,5
,7
]}

Lequin, Olivier ^{[1
,2
]}

Susin, Santos A. ^{[4
,5
,6
]}

Karoyan, Philippe ^{[1
,2
,3
]}

机构：

[1] UPMC Univ Paris 06, Sorbonne Univ, Ecole Normale Super, CNRS,Lab Biomol, F-75005 Paris, France

[2] UPMC Univ Paris 06, PSL Res Univ, Ecole Normale Super, Dept Chim,CNRS,Lab Biomol, F-75005 Paris, France

[3] UPMC Univ Paris 06, Lab BioMol, Site GSK,25-27 Ave Quebec, F-91140 Les Ulis, France

[4] INSERM, Ctr Rech Cordeliers, Cell Death & Drug Resistance Lymphoproliferat Dis, UMRS 1138, Paris, France

[5] UPMC Univ Paris 06, Sorbonne Univ, UMRS 1138, Paris, France

[6] Univ Paris 05, Sorbonne Paris Cite, UMRS 1138, Paris, France

[7] GH Pitie Salpetriere, AP HP, Serv Hematol Biol, F-75013 Paris, France

[8] NanoTemper Technol GmbH, Floessergasse 4, D-81369 Munich, Germany

[9] GSK, 25 Ave Quebec, F-91140 Les Ulis, France

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 59卷 / 18期

关键词：

C-TERMINAL DOMAIN; CHRONIC LYMPHOCYTIC-LEUKEMIA; INTEGRIN-ASSOCIATED PROTEIN; BINDING DOMAIN; CD47; RECEPTOR; CANCER; AMINOMETHYLATION; IDENTIFICATION; DERIVATIVES;

D O I：

10.1021/acs.jmedchem.6b00781

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thrombospondin-1 (TSP-1) is a glycoprotein considered as a key actor within the tumor microenvironment. Its binding to CD47, a cell surface receptor, triggers programmed cell death. Previous studies allowed the identification of 4N1K decapeptide derived from the TSP-1/CD47 binding epitope. Here, we demonstrate that this peptide is able to induce selective apoptosis,of various cancer cell lines while sparing normal cells. A structure activity relationship study led to the design of the first serum stable TSP-1 mimetic agonist peptide able to trigger selective programmed cell death (PCD) of at least lung, breast, and colorectal cancer cells. Altogether, these results will be of valuable interest for further investigation in the design of potent CD47 agonist peptides, opening new perspectives for the development of original anticancer therapies.

引用

页码：8412 / 8421

页数：10

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