@article{3021951,
    title = "Synthesis and biological evaluation of a Platinum(II)-c(RGDyK) conjugate for integrin-targeted photodynamic therapy",
    author = "Chatzisideri, T. and Thysiadis, S. and Katsamakas, S. and Dalezis, P. and Sigala, I. and Lazarides, T. and Nikolakaki, E. and Trafalis, D. and Gederaas, O.A. and Lindgren, M. and Sarli, V.",
    journal = "European Journal of Medicinal Chemistry",
    year = "2017",
    volume = "141",
    pages = "221-231",
    publisher = "Elsevier Masson SAS",
    issn = "0223-5234",
    doi = "10.1016/j.ejmech.2017.09.058",
    keywords = "4 (2,5 dioxopyrrolidin 1 yl)carbonyl 2,6 bis(pyridin 2 yl)phenyl]platinum(II) chloride;  4 carboxy 2,6 bis(pyridin 2 yl)phenyl]platinum(II) chloride;  amino acid;  arginylglycylaspartic acid;  cytostatic agent;  dimethyl sulfoxide;  integrin;  methyl 3,5 bis(4,4,5,5 tetramethyl 1,3,2 dioxaborolan 2 yl)benzoate;  methyl 3,5 di(pyridin 2 yl)benzoate;  okadaic acid;  platinum complex;  singlet oxygen;  unclassified drug;  water;  [4 (methoxycarbonyl) 2,6 bis(pyridin 2 yl)phenyl]platinum(II) chloride;  antineoplastic agent;  arginyl-glycyl-aspartic acid;  integrin;  oligopeptide;  platinum;  platinum complex, A-549 cell line;  animal cell;  antiproliferative activity;  Article;  astrocytoma cell line;  AY-27 cell line;  blue light;  cancer inhibition;  cell survival;  cell viability;  confocal microscopy;  controlled study;  drug conjugation;  drug cytotoxicity;  drug delivery system;  drug design;  drug stability;  drug synthesis;  drug targeting;  drug uptake;  electrospray mass spectrometry;  endocytosis;  female;  fluorescence analysis;  HeLa cell line;  high performance liquid chromatography;  human;  human cell;  IC50;  in vitro study;  irradiation;  light exposure;  liquid chromatography-mass spectrometry;  luminescence;  MCF-7 cell line;  MDA-MB-231 cell line;  microwave irradiation;  MTT assay;  nonhuman;  PC-3 [Human prostate carcinoma] cell line;  photodynamic therapy;  protein expression;  proton nuclear magnetic resonance;  rat;  SK-OV-3 cell line;  U87M cell line;  ultraviolet radiation;  animal;  antagonists and inhibitors;  cell proliferation;  chemical structure;  chemistry;  dose response;  drug effects;  drug screening;  metabolism;  photochemotherapy;  structure activity relation;  synthesis;  tumor cell line, Animals;  Antineoplastic Agents;  Cell Line, Tumor;  Cell Proliferation;  Cell Survival;  Dose-Response Relationship, Drug;  Drug Screening Assays, Antitumor;  Humans;  Integrins;  Molecular Structure;  Oligopeptides;  Organoplatinum Compounds;  Photochemotherapy;  Platinum;  Rats;  Structure-Activity Relationship",
    abstract = "A cancer-targeting conjugate 4 of a cyclometalated [N,C,N-Pt(II)] complex bearing a NˆCˆN 1,3-di(2-pyridyl)-benzene with c(RGDyK) peptide as guiding molecule was designed and synthesized for real-time drug delivery monitoring in cancer cells and photodynamic therapy (PDT). This conjugate demonstrates a mild cytostatic effect to six cancer cell lines expressing integrins at different extent, while possessing promising features for PDT. Conjugate 4 demonstrated rapid cell uptake by receptor-mediated endocytosis and efficient generation of 1O2 upon irradiation. Incubation of rat bladder cancer cells AY27 with conjugate 4 (50 μΜ) prior to blue light exposure (5 min) resulted in significant reduction (50%) of cell survival compared to control cells as measured by MTT assay post 24 h after treatment. © 2017 Elsevier Masson SAS"
}