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PM00104 (Zalypsis®): A Marine Derived Alkylating Agent

by Bradley J. Petek 1,† and Robin L. Jones 2,*,†
1
University of Washington School of Medicine, 1959 NE Pacific St, Seattle, WA 98195, USA
2
Fred Hutchinson Cancer Research Center, University of Washington, 825 Eastlake Avenue East, G-3630, Seattle, WA 98109-1023, USA
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2014, 19(8), 12328-12335; https://doi.org/10.3390/molecules190812328
Received: 25 July 2014 / Revised: 11 August 2014 / Accepted: 11 August 2014 / Published: 15 August 2014
(This article belongs to the Special Issue Alkaloids: Novel Therapeutic Perspectives)
PM00104 (Zalypsis®) is a synthethic tetrahydroisoquinolone alkaloid, which is structurally similar to many marine organisms. The compound has been proposed as a potential chemotherapeutic agent in the treatment of solid human tumors and hematological malignancies. PM00104 is a DNA binding agent, causing inhibition of the cell cycle and transcription, which can lead to double stranded DNA breaks. After rigorous pre-clinical testing, the drug has been evaluated in a number of phase II clinical trials. This manuscript provides a review of current trials and appraises the efficacy of PM00104 as a future cancer treatment. View Full-Text
Keywords: PM00104; Zalypsis; alkaloid; chemotherapy; cancer therapy PM00104; Zalypsis; alkaloid; chemotherapy; cancer therapy
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Petek, B.J.; Jones, R.L. PM00104 (Zalypsis®): A Marine Derived Alkylating Agent. Molecules 2014, 19, 12328-12335.

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