Enhancing intracellular levels of a cyclic nucleotide, useful to treat e.g. chemotherapy resistance, comprises administering inhibitors of multidrug resistance protein 5 and phosphodiesterase
Опубликовано: 07-03-2002
Автор(ы): Dietrich Keppler, Gabriele Jedlitschky
Принадлежит: Deutsches Krebsforschungszentrum DKFZ
Реферат: A method for enhancing intracellular levels of a cyclic nucleotide comprises administering an inhibitor of both multidrug resistance protein isoform 5 (MRP5) and phophodiesterase or by administering an inhibitor to MRP5 in combination with an inhibitor to phophodiesterases. Independent claims are included for: (1) compositions comprising an inhibitor to MRP5 and/or an inhibitor to phosphodiesterases in a carrier, diluent or vehicle; (2) identification of inhibitors, that increase cellular levels of cyclic nucleotides by use of MRP5 expressing cells or membranes from these cells (screening methods); (3) method to test drugs or compounds to improve tissue specificity comprising comparing the tissue specific expression of MRP5 and phophodiesterases and the relative potency of inhibition of MRP5 and phosphodiesterases by the drug; and (4) reversing or preventing chemotherapy resistance mediated by MRP5 or triggering apoptosis in tumor cells which express MRP5 comprising administering an inhibitor to MRP5.
Use of inhibitors to multidrug resistance protein 5 (mrp5) to enhance intracellular levels of cyclic nucleotides
Номер патента: WO2002003993A3. Автор: Gabriele Jedlitschky,Dietrich Keppler. Владелец: Dietrich Keppler. Дата публикации: 2002-08-08.