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Olaparib Conjugates with Selenopheno[3,2-c]quinolinone Inhibit PARP1 and Reverse ABCB1-Related Multidrug Resistance.

Marina Makrecka-Kuka1, Jelena Vasiljeva1, Pavels Dimitrijevs1

  • 1Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.

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|December 23, 2022
PubMed
Summary

Novel drug conjugates targeting multidrug resistant (MDR) cancers show promise. These compounds inhibit ABCB1 transporter and PARP1 activity, restoring doxorubicin efficacy in uterine sarcoma cells for improved cancer therapy.

Keywords:
MDRPARP1cancerolaparibquinolinoneselenium

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Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Multidrug resistant (MDR) cancers pose a significant challenge in cancer therapy.
  • Overexpression of the ABCB1 transporter reduces the effectiveness of conventional drugs like doxorubicin.
  • Combined inhibition of ABCB1 and PARP1 offers a potential strategy to overcome drug resistance and enhance DNA repair inhibition in cancer cells.

Purpose of the Study:

  • To design and synthesize novel olaparib conjugates with selenophenoquinolinones.
  • To evaluate the ability of these conjugates to reverse doxorubicin resistance in uterine sarcoma cells.
  • To elucidate the mechanism of action of the most potent conjugate.

Main Methods:

  • Synthesis of three novel olaparib conjugates incorporating selenophenoquinolinones.
  • In vitro assessment of doxorubicin resistance reversal in uterine sarcoma cell lines.
  • Evaluation of PARP1 inhibitory activity and ABCB1 transporter inhibition.

Main Results:

  • One synthesized conjugate demonstrated significant efficacy in reversing doxorubicin resistance.
  • The most potent compound retained PARP1 inhibitory activity.
  • This conjugate attenuated doxorubicin resistance by effectively inhibiting the ABCB1 transporter.

Conclusions:

  • Conjugating PARP inhibitors with selenophenoquinolinones is a promising approach for developing new agents against MDR cancers.
  • The lead compound acts as a chemosensitizer by targeting both PARP1 and ABCB1 pathways.
  • This strategy holds potential for improving treatment outcomes in patients with multidrug resistant cancers.