HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells

[Image: see text] A N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer–CXCR4 antagonist (BKT140) conjugate (P-BKT140) was developed and its biological activities were tested. Both free BKT140 and monomer MA-GGPLGLAG-BKT140 (MA is methacryloyl) were prepared by solid phase synthesis. P-BKT140 was pre...

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Autores principales: Peng, Zheng-Hong, Kopeček, Jindřich
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4299399/
https://www.ncbi.nlm.nih.gov/pubmed/25621190
http://dx.doi.org/10.1021/mz5006537
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author Peng, Zheng-Hong
Kopeček, Jindřich
author_facet Peng, Zheng-Hong
Kopeček, Jindřich
author_sort Peng, Zheng-Hong
collection PubMed
description [Image: see text] A N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer–CXCR4 antagonist (BKT140) conjugate (P-BKT140) was developed and its biological activities were tested. Both free BKT140 and monomer MA-GGPLGLAG-BKT140 (MA is methacryloyl) were prepared by solid phase synthesis. P-BKT140 was prepared by reversible addition–fragmentation chain transfer (RAFT) copolymerization of monomers HPMA and MA-GGPLGLAG-BKT140. The in vitro results show that the free BKT140 and P-BKT140 have similar cytotoxicity against human prostate carcinoma PC-3 cells, indicating that conjugation of BKT140 to HPMA did not significantly impact the cytotoxicity of BKT140. Both BKT140 and P-BKT140 inhibited the CXCL12-induced migration of PC-3 prostate cancer cells, but the P-BKT140 conjugate possessed a substantially higher inhibition activity than free BKT140.
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spelling pubmed-42993992015-11-17 HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells Peng, Zheng-Hong Kopeček, Jindřich ACS Macro Lett [Image: see text] A N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer–CXCR4 antagonist (BKT140) conjugate (P-BKT140) was developed and its biological activities were tested. Both free BKT140 and monomer MA-GGPLGLAG-BKT140 (MA is methacryloyl) were prepared by solid phase synthesis. P-BKT140 was prepared by reversible addition–fragmentation chain transfer (RAFT) copolymerization of monomers HPMA and MA-GGPLGLAG-BKT140. The in vitro results show that the free BKT140 and P-BKT140 have similar cytotoxicity against human prostate carcinoma PC-3 cells, indicating that conjugation of BKT140 to HPMA did not significantly impact the cytotoxicity of BKT140. Both BKT140 and P-BKT140 inhibited the CXCL12-induced migration of PC-3 prostate cancer cells, but the P-BKT140 conjugate possessed a substantially higher inhibition activity than free BKT140. American Chemical Society 2014-11-17 2014-12-16 /pmc/articles/PMC4299399/ /pubmed/25621190 http://dx.doi.org/10.1021/mz5006537 Text en Copyright © 2014 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Peng, Zheng-Hong
Kopeček, Jindřich
HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells
title HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells
title_full HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells
title_fullStr HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells
title_full_unstemmed HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells
title_short HPMA Copolymer CXCR4 Antagonist Conjugates Substantially Inhibited the Migration of Prostate Cancer Cells
title_sort hpma copolymer cxcr4 antagonist conjugates substantially inhibited the migration of prostate cancer cells
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4299399/
https://www.ncbi.nlm.nih.gov/pubmed/25621190
http://dx.doi.org/10.1021/mz5006537
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