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In vitro viability assays against a representative panel of human cancer cell lines revealed that polyamines L1a and L5a displayed remarkable activity with IC50 values in the micromolar range. Preliminary research indicated that both compounds promoted G1 cell cycle arrest followed by cellular senescence and apoptosis. The induction of apoptotic cell death involved loss of mitochondrial outer membrane permeability and activation of caspases 3/7. Interestingly, L1a and L5a failed to activate cellular DNA damage response. High intracellular zinc chelating capacity of both compounds, deduced from the metal specific Zinquin assay and ZnL2+ stability constant values in solution strongly support their cytotoxicity. These data along with quantum mechanical studies have enabled to establish a precise Structure-Activity Relationship. Moreover, L1a and L5a showed appropriate drug-likeness by in silico methods. Based on these promising results, L1a and L5a should be considered a new class of zinc-chelating anticancer agents that deserve further development.
This article was published in the following journal.
Name: Journal of medicinal chemistry
The special linear dioxo cation structure of the uranyl cation, which relegates ligand coordination to an equatorial plane perpendicular to the O═U═O vector, poses an unusual challenge for the rat...
Diverse platinum drug candidates have been designed to improve inhibitory potency and overcome resistance for orthotopic tumor. However, the antimetastatic properties are rarely reported. We herein re...
Heavy metal stabilization by chemical chelating agent and solidification by cement are technologies currently used to reduce the leaching of heavy metals in municipal solid waste incineration (MSWI) f...
Iron depletion is an efficient strategy for the development of anticancer agents. In an effort to develop efficient chelators, two new 3-hydroxy-4-pyridinone based polyazamacrocycles 1e and 2e were de...
A lack of accurate computational tools to guide rational mutagenesis has made affinity maturation a recurrent challenge in antibody development. We previously showed that graph-based signatures can be...
Assessment of the impact of oral Human Milk Oligosaccharides (HMO) application on acute diarrhoea and the development of prolonged and persistent diarrhoea in paediatric patients hospitali...
The overall objective of this study is to examine the effect of polyamine supplementation on cognitive performance of individuals with subjective cognitive decline.
The overall objective of this study is to examine the effect of polyamine supplementation on cognitive performance and further characterization of individuals with subjective cognitive dec...
After surgery, sensitization and hyperexcitability of central nervous system result in acute and long lasting postoperative pain. It has been shown that N-methyl-D-aspartate (NMDA) recepto...
The aim of this study is to evaluate if a polyamine deficient diet started 7 days prior to a major abdominal surgery (eventration cure and digestive continuity) and followed 7 days post-su...
Chemicals that bind to and remove ions from solutions. Many chelating agents function through the formation of COORDINATION COMPLEXES with METALS.
An approach, process, or methodology which emphasizes credible evidence and the best available scientific knowledge, judiciously integrated to achieve the best possible outcomes in structural design. For example, the design of a new OUTPATIENT CLINIC might incorporate a review of published research on outpatient clinic design, decisions on similar past projects, along with interviews with staff and consumers.
A chelating agent (CHELATING AGENTS) that sequesters a variety of polyvalent cations. It is used in pharmaceutical manufacturing and as a food additive.
The degree of 3-dimensional shape similarity between proteins. It can be an indication of distant AMINO ACID SEQUENCE HOMOLOGY and used for rational DRUG DESIGN.
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
Bladder Cancer Brain Cancer Breast Cancer Cancer Cervical Cancer Colorectal Head & Neck Cancers Hodgkin Lymphoma Leukemia Lung Cancer Melanoma Myeloma Ovarian Cancer Pancreatic Cancer ...
Immunoassay - ELISA
Immunoassays are quick and accurate tests to detect specific molecules. Immunoassays rely on an antibody to bind to the specific structure of a molecule. Antibodies are proteins generated by animals in response to the invasion of a foreign molecule (anti...
Cancer is not just one disease but many diseases. There are more than 100 different types of cancer. Most cancers are named for the organ or type of cell in which they start - for example, cancer that begins in the colon is called colon cancer; cancer th...