Article (Scientific journals)
Thrombospondin-1 Mimetic Agonist Peptides Induce Selective Death in Tumor Cells: Design, Synthesis and Structure-Activity Relationship Studies
DENEFLE, Thomas; Boullet, Heloise; Lequin, Olivier et al.
2016In Journal of Medicinal Chemistry
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Keywords :
CD47; Cancer; Peptide
Abstract :
[en] 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.
Research center :
Sorbonne-Université, UPMC, Université Paris 06, Ecole Normale Supeŕieure, CNRS, Laboratoire des Biomolećules, 75005 Paris, France
Deṕartement de Chimie, Ecole Normale Supeŕieure,PSL Research University, UPMC Université Paris 06, CNRS, Laboratoiredes Biomolećules,75005 Paris, France
Cell Death and Drug Resistance in Lymphoproliferative Disorders Team, Centre de Recherche des Cordeliers, INSERM UMRS, 1138, Paris, France
Université Paris Descartes, Sorbonne Paris Cite,́ UMRS 1138, Paris, France
AP-HP, GH Pitie-́Salpet̂rier̀e, Service d’Heḿatologie Biologique, 75013 Paris, France
NanoTemper Technologies GmbH, Floessergasse 4, 81369 Munich, Germany
GSK, 25 Avenue du Queb́ec, 91140 Les Ulis ,France
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
DENEFLE, Thomas
Boullet, Heloise
Lequin, Olivier
Karoyan, Philippe
Herbi, Linda
Other collaborator :
Lardé, Eva ;  Université de Liège > Département des sciences biomédicales et précliniques > GIGA-R : Labo de recherche sur les métastases
Newton, Clara
Martinez-Torres, Ana Carolina
Grondin, Pascal
Language :
English
Title :
Thrombospondin-1 Mimetic Agonist Peptides Induce Selective Death in Tumor Cells: Design, Synthesis and Structure-Activity Relationship Studies
Publication date :
15 August 2016
Journal title :
Journal of Medicinal Chemistry
ISSN :
0022-2623
eISSN :
1520-4804
Publisher :
American Chemical Society, Washington, United States - District of Columbia
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 24 July 2019

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