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

ZhengHong Peng | Zendy; Jindřich Kopeček | Zendy

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

Author(s) -

ZhengHong Peng,

Jindřich Kopeček

Publication year - 2014

Publication title -

acs macro letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.966

H-Index - 92

ISSN - 2161-1653

DOI - 10.1021/mz5006537

Subject(s) - methacrylamide , conjugate , cytotoxicity , copolymer , monomer , raft , chain transfer , chemistry , fragmentation (computing) , in vitro , prostate cancer , antagonist , biochemistry , polymer , radical polymerization , cancer , organic chemistry , biology , medicine , receptor , acrylamide , mathematical analysis , mathematics , ecology

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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