Abstract:
:A chemokine receptor, CXCR4, and its endogenous ligand, stromal cell-derived factor-1 (SDF-1), have been recognized to be involved in the metastasis of several types of cancers. T140 analogs are peptidic CXCR4 antagonists composed of 14 amino acid residues that were previously developed as anti-HIV agents having inhibitory activity against HIV-entry through its co-receptor, CXCR4. Herein, we report that these compounds effectively inhibited SDF-1-induced migration of human breast cancer cells (MDA-MB-231), human leukemia T cells (Sup-T1) and human umbilical vein endothelial cells at concentrations of 10-100 nM in vitro. Furthermore, slow release administration by subcutaneous injection using an Alzet osmotic pump of a potent and bio-stable T140 analog, 4F-benzoyl-TN14003, gave a partial, but statistically significant (P=0.05 (t-test)) reduction in pulmonary metastasis of MDA-MB-231 in SCID mice, even though no attempt was made to inhibit other important targets such as CCR7. These results suggest that T140 analogs have potential use for cancer therapy, and that small molecular CXCR4 antagonists could potentially replace neutralizing antibodies as anti-metastatic agents for breast cancer.
journal_name
FEBS Lettjournal_title
FEBS lettersauthors
Tamamura H,Hori A,Kanzaki N,Hiramatsu K,Mizumoto M,Nakashima H,Yamamoto N,Otaka A,Fujii Ndoi
10.1016/s0014-5793(03)00824-xkeywords:
subject
Has Abstractpub_date
2003-08-28 00:00:00pages
79-83issue
1-3eissn
0014-5793issn
1873-3468pii
S001457930300824Xjournal_volume
550pub_type
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