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PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti‐tumour activity
TLDR
The interactions of PM01183 with selected DNA molecules of defined sequence and its in vitro and in vivo cytotoxicity are characterized. Expand
Lurbinectedin (PM01183), a New DNA Minor Groove Binder, Inhibits Growth of Orthotopic Primary Graft of Cisplatin-Resistant Epithelial Ovarian Cancer
TLDR
Preclinical orthotopically perpetuated ovarian tumor grafts are useful tools for drug development, providing hard evidence that lurbinectedin might be a useful therapy in the treatment of EOC by overcoming cisplatin resistance. Expand
Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A
TLDR
The results indicate that plitidepsin is a promising therapeutic candidate for COVID-19, and in cells, the drug is substantially more potent than remdesivir against SARS-CoV-2, with limited cellular toxicity. Expand
Aplidin, a marine organism-derived compound with potent antimyeloma activity in vitro and in vivo.
TLDR
The marine-derived cyclodepsipeptide Aplidin exhibits, at clinically achievable concentrations, potent in vitro activity against primary MM tumor cells and a broad spectrum of human MM cell lines, including cells resistant to conventional or novel anti-MM agents. Expand
Host-directed therapies against early-lineage SARS-CoV-2 retain efficacy against B.1.1.7 variant
TLDR
It is found that plitidepsin is over an order of magnitude more potent than remdesivir against both viruses, highlighting the importance of continued development of host-directed therapeutics to combat current and future coronavirus variant outbreaks. Expand
Zalypsis: a novel marine-derived compound with potent antimyeloma activity that reveals high sensitivity of malignant plasma cells to DNA double-strand breaks.
TLDR
The potent in vitro and in vivo antimyeloma activity of Zalypsis uncovers the high sensitivity of tumor plasma cells to DSBs and strongly supports the use of this compound in MM patients. Expand
Activities of Sordarins in Experimental Models of Candidiasis, Aspergillosis, and Pneumocystosis
TLDR
GM193663 and GM237354 are new sordarin derivatives that may potentially play a major role in the treatment of candidiasis and PCP and are studied in mouse models of disseminated candidiasisand in a rat model of pneumocystosis. Expand
Molecular pharmacology and antitumor activity of Zalypsis in several human cancer cell lines.
TLDR
Zalypsis administration in four murine xenograft models of human cancer demonstrates significant tumor growth inhibition that is highest in the Hs746t gastric cancer cell line with no weight loss of treated animals. Expand
PM060184, a new tubulin binding agent with potent antitumor activity including P-glycoprotein over-expressing tumors.
TLDR
It is shown that PM060184 has a potent antitumor activity in a panel of different tumor xenograft models and is able to overcome P-gp mediated resistance in vivo, an effect that could be related to its high binding affinity for tubulin. Expand
Lurbinectedin Inactivates the Ewing Sarcoma Oncoprotein EWS-FLI1 by Redistributing It within the Nucleus.
TLDR
Important mechanistic advances and a second-generation inhibitor are reported to provide insight into the therapeutic targeting of EWS-FLI1 and illustrate the preclinical safety and efficacy of a disease-specific therapy targeting the central oncogenic driver in Ewing sarcoma. Expand
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