Exploring the N‑Terminal Region of C‑X‑C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C‑X‑C Chemokine Receptor Type 4 (CXCR4) Antagonists

We previously reported the discovery of a CXCL12-mimetic cyclic peptide (2) as a selective CXCR4 antagonist showing promising in vitro and in vivo anticancer activity. However, further development of this peptide was hampered by its degradation in biological fluids as well as by its low micromolar a...

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Published in:	Journal of medicinal chemistry 2016-09, Vol.59 (18), p.8369-8380
Main Authors:	Di Maro, Salvatore, Trotta, Anna Maria, Brancaccio, Diego, Di Leva, Francesco Saverio, La Pietra, Valeria, Ieranò, Caterina, Napolitano, Maria, Portella, Luigi, D’Alterio, Crescenzo, Siciliano, Rosa Anna, Sementa, Deborah, Tomassi, Stefano, Carotenuto, Alfonso, Novellino, Ettore, Scala, Stefania, Marinelli, Luciana
Format:	Article
Language:	English
Subjects:	Amino Acid Sequence Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Cell Line, Tumor Cell Movement - drug effects Chemokine CXCL12 - chemistry Chemokine CXCL12 - pharmacology Colonic Neoplasms - drug therapy Humans Leukemia - drug therapy Models, Molecular Peptides, Cyclic - chemistry Peptides, Cyclic - pharmacology Phosphorylation - drug effects Receptors, CXCR4 - antagonists & inhibitors
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