Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 12, Issue 5, 2012

Cancer is a challenging disease, characterized by a multitude of pathologically upregulated physiological processes that allow differentiating a tumor from normal tissue, providing a vast array of molecular targets. Successful cancer therapy hinges on early diagnosis and accurate staging. To this purpose, several strategies have been developed over the past two decades based on the use of small molecules or macromolec Read More

The overexpression of peptide receptors in human tumours makes peptide-ligands attractive agents for the development of specific diagnostic imaging and/or therapy of cancers. Solid-phase peptide synthesis, modern phage display technology and combinatorial peptide chemistry have profoundly affected the pool of available targeting peptides for efficient and specific delivery of imaging or therapeutic label molecules. Read More

Currently, receptor based radiopharmaceuticals have received great attention in molecular imaging and radiotherapy of cancer, and provide a unique tool for target-specific delivery of radionuclides to pathological tissues. In this context, receptor binding peptides represent an attractive class of target vectors for Nuclear Medicine purposes. The rich chemistry of the group 7 elements elaborated in past years, has allowed Read More

Radiolabeled peptides hold promise for diagnosis and therapy of cancer as well as for early monitoring of therapy outcomes, patient stratification, etc. This manuscript focuses on the development of peptides labeled with 18F, 64Cu, 68Ga and other positron-emitting radionuclides for PET imaging. The major techniques for radionuclide incorporation are briefly discussed. Then, examples of positronemitting peptides targeti Read More

Molecular imaging consists of non-invasive monitoring of spatial-temporal distribution of molecular or cellular processes, and may be used for early disease detection and real-time monitoring of therapeutic responses. Several strategies have been developed over the last two decades. Early attempts used monoclonal antibodies or antibody fragments and, although specific targeting was achieved, these probes was largely un Read More

In human pathologies, therapeutic treatments are often limited by the lack of selectivity of drugs and their elevated effective concentrations. Targeting these agents to a defined tissue could enhance their selectivity and then diminish their side effects when compared to drugs that accumulate in the entire body. Targeting could also improve treatment efficiency by allowing a localized high concentration of the agent Read More

Neuroendocrine tumors (NETs) are rare tumors with variable malignant behavior. The majority of NETs express increased levels of somatostatin (SST) receptors, particularly SST2 receptors. Radiolabeled peptides specific for the SST2 receptors may be used for diagnosis of NETs and for peptide receptor radionuclide therapy (PRRT). [111In-DTPA0]-octreotide has been the first peptide used for PRRT. This radiolabeled pepti Read More

Boron neutron capture therapy (BNCT) is based on the capture of thermal neutrons by boron 10 (10B) nuclei that have been selectively delivered to tumor cells. The amount of 10-30 μg of boron for g of tumor mass is needed to attain an acceptable therapeutic advantage. Despite that the potentialities of BNCT have been demonstrated in several preclinical studies, this technique has not yet been fully accepted in the armor Read More

Genistein, a nontoxic flavonoid compound, has potent antitumor activity in various cancer cells. In the present study, we investigated whether genistein could be employed as a novel strategy to enhance the anti-tumor activity of gemcitabine using human osteosarcoma MNNG/HOS tumor model. In vitro, by MTT, electron microscopy, immunobloting and qRT-PCR assay, we found that the combination treatment of genistein Read More