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PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti‐tumour activity
BACKGROUND AND PURPOSE PM01183 is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumours. In this study we haveExpand
Irvalec Inserts into the Plasma Membrane Causing Rapid Loss of Integrity and Necrotic Cell Death in Tumor Cells
Irvalec is a marine-derived antitumor agent currently undergoing phase II clinical trials. In vitro, Irvalec induces a rapid loss of membrane integrity in tumor cells, accompanied of a significantExpand
Cellular senescence induced by p53‐ras cooperation is independent of p21waf1 in murine embryo fibroblasts
Oncogenic activation in primary murine fibroblasts initiates a senescence‐like cell cycle arrest that depends on the p53 tumor suppressor pathway. Conditional p53 activation efficiently induced aExpand
Extreme sensitivity to Yondelis® (Trabectedin, ET‐743) in low passaged sarcoma cell lines correlates with mutated p53
Yondelis® (Trabectedin, ET‐743) is a marine anticancer agent currently in Phase II/III development in patients with advanced pretreated soft tissue sarcoma. In the present study, we generated a panelExpand
Transcriptional signature of Ecteinascidin 743 (Yondelis, Trabectedin) in human sarcoma cells explanted from chemo-naïve patients
Ecteinascidin 743 (ET-743; Yondelis, Trabectedin) is a marine anticancer agent that induces long-lasting objective remissions and tumor control in a subset of patients with pretreated/resistantExpand
Levels of p27kip1 determine Aplidin sensitivity
Aplidin (plitidepsin) is a novel anticancer drug isolated from the marine tunicate Aplidium albicans. Aplidin shows potent antitumor activity in preclinical models against a wide variety of humanExpand
Molecular pharmacology and antitumor activity of Zalypsis in several human cancer cell lines.
Zalypsis is a new synthetic alkaloid tetrahydroisoquinoline antibiotic that has a reactive carbinolamine group. This functionality can lead to the formation of a covalent bond with the amino group ofExpand
Large scale genetic screen identifies MAP17 as protein bypassing TNF‐induced growth arrest
Although activated macrophages destroy cancer cells more effectively than normal cells, the ability to escape activated macrophages is a characteristic of tumor cells. One of the mechanismsExpand
Using cells devoid of RAS proteins as tools for drug discovery
Mutational activation of RAS proteins occurs in nearly 30% of all human tumors. To date direct pharmacological inhibition of RAS oncoproteins has not been possible. As a consequence, currentExpand
Inhibition of phosphatidylinositol-3-kinase synergizes with gemcitabine in low-passage tumor cell lines correlating with Bax translocation to the mitochondria
Apoptotic pathways, including the phosphatidylinositol-3-kinase (PI3K)/AKT survival pathway, are altered in most cancer cells in relation to their normal counterparts and these differences mayExpand