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Inhibition of proteasome deubiquitinating activity as a new cancer therapy
TLDR
Treatment with b-AP15 inhibited tumor progression in four different in vivo solid tumor models and inhibited organ infiltration in an acute myeloid leukemia model, showing that the deubiquitinating activity of the 19S regulatory particle is a new anticancer drug target.
Genome-wide signatures of differential DNA methylation in pediatric acute lymphoblastic leukemia
TLDR
Analysis of relapse-free survival identified CpG sites with subtype-specific differential methylation that divided the patients into different risk groups, depending on their methylation status, suggesting an important biological role for DNA methylation in the differences between ALL subtypes and in their clinical outcome after treatment.
Aminopeptidase N (CD13) as a target for cancer chemotherapy
TLDR
The prevalence and possible function of APN in malignant diseases, mainly solid tumors, as well as its “drugability” evaluated in preclinical in vivo models are discussed, and a brief overview of current clinical trials focused on APN is provided.
Induction of mitochondrial dysfunction as a strategy for targeting tumour cells in metabolically compromised microenvironments
TLDR
The small molecule VLX600 is identified as a drug that is preferentially active against quiescent cells in colon cancer 3-D microtissues and displays tumour growth inhibition in vivo, suggesting that tumours in metabolically compromised microenvironments have a limited ability to respond to decreased mitochondrial function.
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
TLDR
High lipophilicity and a positive net charge were found to be the key physicochemical properties for OCT1 inhibition, whereas a high molecular dipole moment and many hydrogen bonds were negatively correlated to Oct1 inhibition.
A Phase I study of CHS 828 in patients with solid tumor malignancy.
TLDR
No objective tumor responses were observed, and 7 patients showed stable disease after two courses of therapy, and there was an apparent inverse relationship between systemic exposure of CHS 828, and thrombocyte and lymphocyte nadir levels.
The fluorometric microculture cytotoxicity assay
The fluorometric microculture cytotoxicity assay (FMCA) is a nonclonogenic microplate-based cell viability assay used for measurement of the cytotoxic and/or cytostatic effect of different compounds
Anticancer agent CHS 828 suppresses nuclear factor‐κB activity in cancer cells through downregulation of IKK activity
TLDR
It is hypothesized that the anticancer activity of CHS 828 is due to inhibition of the IKK activity by which the antiapoptotic protection of NF‐κB is removed, leading to the promotion of apoptosis.
Cyclotides: a novel type of cytotoxic agents.
TLDR
Activity profiles of the cyclotides differed significantly from those of antitumor drugs in clinical use, which may indicate a new mode of action in cytotoxic activities of naturally occurring macrocyclic peptides isolated from the two violets.
CHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo.
TLDR
CHS 828 is an effective new antitumor agent, with a potentially new mechanism of action, found to compare favorably with established chemotherapeutic agents such as cyclophosphamide, etoposide, methotrexate, and paclitaxel and long-term survival was observed in mice with NYH tumors.
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