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Characterization of a Large Panel of Patient-Derived Tumor Xenografts Representing the Clinical Heterogeneity of Human Colorectal Cancer
An extensive in vivo analysis of patient-derived xenograft models for CRC shows the loss of human stroma cells after engraftment, observed a metastatic phenotype in some models, and compared the molecular profile with the drug sensitivity of each tumor model. Expand
Polo-like kinase 1: a potential therapeutic option in combination with conventional chemotherapy for the management of patients with triple-negative breast cancer.
Observations suggest PLK1 inhibition as an attractive therapeutic approach, in association with conventional chemotherapy, for the management of patients with TNBC. Expand
TTK/hMPS1 Is an Attractive Therapeutic Target for Triple-Negative Breast Cancer
TTK is pointed out as a protein kinase overexpressed in TNBC that may represent an attractive therapeutic target specifically for this poor prognosis associated subgroup of breast cancer. Expand
S49076 Is a Novel Kinase Inhibitor of MET, AXL, and FGFR with Strong Preclinical Activity Alone and in Association with Bevacizumab
Preclinical studies showing a favorable and novel pharmacologic profile of S49076, a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 are described and a phase I study is currently underway in patients with advanced solid tumors. Expand
An unusual DNA binding compound, S23906, induces mitotic catastrophe in cultured human cells.
The results suggest that mitotic catastrophe is one of the cellular responses to S23906 and thatMitotic catastrophe may be a common cellular response to many different types of DNA damage. Expand
Synthesis and antitumor activity of the metformin platinum (IV) complex. Crystal structure of the tetrachloro(metformin)platinum (IV) dimethylsulfoxide solvate.
- F. Bentefrit, G. Morgant, +5 authors H. Nguyen
- Chemistry, Medicine
- Journal of inorganic biochemistry
- 1 October 1997
The synthesis of (metformin) tetrachloroplatinum (IV) was investigated and was found to be as potent as cis-dichlorodiammine platinum (II), CDDP, in inhibiting the proliferation of the sensitive P388 cells, however the resistant P388/CDDP cells were threefold more sensitive to the compound than to CDDP. Expand
New triazine derivatives as potent modulators of multidrug resistance.
- A. Dhainaut, G. Régnier, +4 authors J. Prost
- Chemistry, Medicine
- Journal of medicinal chemistry
- 26 June 1992
The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the P-glycoprotein catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators. Expand
Binding characteristics of novel nonsteroidal antiestrogens to the rat uterine estrogen receptors
- C. Martel, L. Provencher, +5 authors F. Labrie
- Medicine, Biology
- The Journal of Steroid Biochemistry and Molecular…
- 1 February 1998
The present data demonstrate the high affinity and specificity of the new antiestrogen, EM-652, for the rat uterine estrogen receptor and it becomes the compound having the highest known affinity for the estrogen receptor. Expand
Marked antitumor activity of a new potent acronycine derivative in orthotopic models of human solid tumors.
- N. Guilbaud, L. Kraus-Berthier, +10 authors A. Pierré
- Clinical cancer research : an official journal of…
- 1 August 2001
In the two human lung cancer models, S 23906-1 increased the survival of the animals in a dose-dependent manner and induced treated versus control values of 162% (NCI-H460 and A549) and 193% (A549). Expand
Novel protein scaffolds as emerging therapeutic proteins: from discovery to clinical proof-of-concept.
Interestingly, several scaffolds include an immune-active component as part of their therapeutic mode of action, which yielded spectacular clinical efficacy in some hematological malignancies. Expand