TY - JOUR
TI - Synthesis and biological evaluation of a Platinum(II)-c(RGDyK) conjugate for integrin-targeted photodynamic therapy
AU - Chatzisideri, T.
AU - Thysiadis, S.
AU - Katsamakas, S.
AU - Dalezis, P.
AU - Sigala, I.
AU - Lazarides, T.
AU - Nikolakaki, E.
AU - Trafalis, D.
AU - Gederaas, O.A.
AU - Lindgren, M.
AU - Sarli, V.
JO - European Journal of Medicinal Chemistry
PY - 2017
VL - 141
TODO - null
SP - 221-231
PB - Elsevier Masson SAS
SN - 0223-5234
TODO - 10.1016/j.ejmech.2017.09.058
TODO - 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
TODO - 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
ER -