Polymer carriers for anticancer drugs targeted to EGF receptor.
A novel actively targeted polymer carrier for anticancer drugs based on an N-(2-hydroxypropyl)methacrylamide copolymer (PHPMA) is proposed. An oligopeptide sequence GE7, attached to the polymer, is a specific ligand for the EGF receptor overexpressed on most tumor cells. Co-attachment of selected chemotherapeutics will therefore lead to formation of tumor-specific polymer therapeutics, further enhanced by the EPR effect. FACS measurements prove elevated binding activity of the fluorescently labeled PHPMA/GE7 conjugate in EGFR-rich cells (FaDu, MCF-7), compared to conjugates of scrambled peptides. Cell lines with low EGFR level (SW620, B16F10) bind the GE7 conjugate significantly less.
Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, Heyrovsky Sq. 2, 162 06 Prague 6, Czech Republic. studenovsky@imc.cas.cz
Martin
M
Studenovsky
Robert
R
Pola
Michal
M
Pechar
Tomas
T
Etrych
Karel
K
Ulbrich
Lubomir
L
Kovar
Martina
M
Kabesova
Blanka
B
Rihova
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems / Q000379:methods*; D066246:ErbB Receptors / Q000378:metabolism*; D005434:Flow Cytometry; D006801:Humans; D009842:Oligopeptides / Q000235:genetics / Q000378:metabolism; D011109:Polymethacrylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D049268:Positron-Emission Tomography; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013056:Spectrophotometry, Ultraviolet
D000970:Antineoplastic Agents; D009842:Oligopeptides; D011109:Polymethacrylic Acids; C011533:Duxon; D066246:ErbB Receptors