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The cyclic pentapeptide d-Arg3FC131, a CXCR4 antagonist, induces apoptosis of somatotrope tumor and inhibits tumor growth in nude mice.

Authors
 Jeong Mo Kim  ;  Yong-ho Lee  ;  Cheol Ryong Ku  ;  Eun Jig Lee 
Citation
 ENDOCRINOLOGY, Vol.152(2) : 536-544, 2011 
Journal Title
 ENDOCRINOLOGY 
ISSN
 0013-7227 
Issue Date
2011
MeSH
Adenoviridae ; Animals ; Apoptosis/drug effects* ; Blotting, Western ; Cell Line ; Flow Cytometry ; Genetic Vectors/genetics ; Growth Hormone/metabolism ; In Situ Nick-End Labeling ; Male ; Mice ; Mice, Nude ; Oligopeptides/pharmacology* ; Peptides, Cyclic/pharmacology* ; Peptides, Cyclic/therapeutic use ; Pituitary Neoplasms/drug therapy* ; Pituitary Neoplasms/metabolism ; Rats ; Receptors, CXCR4/antagonists & inhibitors* ; Receptors, CXCR4/therapeutic use ; Reverse Transcriptase Polymerase Chain Reaction ; Somatotrophs/drug effects* ; Somatotrophs/pathology*
Abstract
The interaction between the chemokine stromal cell-derived factor 1 and its receptor CXCR4 plays an important role in GH production and cell proliferation in normal and tumorous pituitary somatotrope cells. Therefore, the chemokine receptor CXCR4 could be an attractive target for antitumor drugs in patients with acromegaly. A synthetic antagonist of CXCR4, cyclic pentapeptide d-Arg3FC131 (c[Gly1-d-Tyr2-d-Arg3-Arg4-Nal5]) significantly inhibited GH production and proliferation of GH3 somatotrope tumor cells in vitro. It also induced apoptosis of GH3 cells through activation of the caspase-3 pathway. Systemic administration of d-Arg3FC131 inhibited the growth of GH3 cell xenografts in immunodeficient nude mice by inducing apoptosis and suppressing the proliferation of tumor cells. These results indicate that d-Arg3FC131 might have potential for the treatment of pituitary tumors producing excess GH in patients with acromegaly.
Files in This Item:
T201100279.pdf Download
DOI
10.1210/en.2010-0642
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Internal Medicine (내과학교실) > 1. Journal Papers
Yonsei Authors
Ku, Cheol Ryong(구철룡) ORCID logo https://orcid.org/0000-0001-8693-9630
Lee, Yong Ho(이용호) ORCID logo https://orcid.org/0000-0002-6219-4942
Lee, Eun Jig(이은직) ORCID logo https://orcid.org/0000-0002-9876-8370
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/92625
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