Poster Presenter

Opioid Analogs As Prospective Selective Carriers Of Platinum Ion In Anticancer Therapy
Misicka-Kesik A, Glowinska A, Jaworska K, Lazarczyk M, Matyja E., Kosson P, Lipkowski
Poland

The Most Powerful And Useful Anticancer Drugs Belong To Cisplatin Derivatives.Cis-Diaminedichloplatinum Analogs Are Responsible For The Inhibition Of DNA Transcription What Leads To Cell Death. Cisplatin Binds Strongly To DNA In Regions Containing Several Guanine Units, Forming Pt-DNA Links Within Strands. Through Disrupting Base-Pairing Guanine To Cytosine Cross-Links Lead To Unwinding Of The DNA. As A Result Cisplatin Work Against Both Types Of Cells, Destroying Cancer And Normal Type Ones. Therefore More Selective Delivery System Of Platinum Ion To Cancer Cells Is Still Needed.

Based On The Evidence That Various Neuropeptide Receptors Are Present On Different Human Cancer Cell Membranes In Higher Concentration, Comparing To Normal Tissue, We Proposed To Use Peptide Ligands Of Such Receptors As Prospective Selective Carriers Of Platinum Ions To Cancer Cells. We Started With The Opioid Receptor System Which Is One Of Possible Target Of Such Directed Chemotherapy. We Designed Hybride Molecules Which Combine Two Fragments: One Part Of The Molecule Contains The Opioid Pharmacophore And The Other Fragment Is Designed To Form A Complex With Platinum Ion. The Binding Affinity At The Opioid Receptors And Effect On The Proliferation Of The Human Glioblastoma Cells Of The Synthesized Compounds Will Be Presented And Discussed.