Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 15, Issue 7, 2015

Hepatocellular carcinoma (HCC) is one of the most malignant cancers, with the second highest cancer death rate world-wide, next to lung cancer. The signaling mechanisms in HCC are currently not clear. Notch signaling, which is highly conserved and plays a critical role in many cancers, was found to be aberrantly upregulated in HCC tissues compared to normal liver tissues. Accumulating evidence supports that Notch signalin Read More

Squamous cell carcinoma (SCC) has a high worldwide incidence that is commonly seen as head and neck cancers, esophageal cancers, and non-small cell lung cancers. There is a poor prognosis for SCC due to potential recurrence and its metastatic tendency so the 5-year survival rate is very low. Target therapy is a novel and promising treatment strategy exhibiting great anti-tumor effects and survival benefits in SCC. This revi Read More

Antibody-drug conjugates (ADCs) showed strong anticancer efficacy in the clinic. However, the current conventional technologies generate conjugates with undefined attachment sites and heterogeneous profiles containing different sub-populations, leading to potential off-target toxicity. In order to reduce the variability and heterogeneity associated with the ADCs generated using conventional technologies, several site-sp Read More

In solid tumors, neoplastic cells are surrounded by a specific microenvironment that integrates the extracellular matrix, lymphatic and blood vessels, and mesenchymal and immune cells, which together are known as the tumor microenvironment (TME). The TME governs many of the aggressive features of tumors, such as local invasion and metastasis. Additionally, new evidence indicates that the TME can trigger stem Read More

Surgery, radiation therapy, and chemotherapy are the traditional options to control tumor progression. However, these strategies are fraught with harmful side effects and are ineffective in metastatic and advanced cancers. Biomarkers that are overexpressed in cancers and are involved in cell growth, proliferation, migration, and survival have recently become the focus of new molecular targeting therapies. Novel therapies tar Read More

Anti-cancer targeting drugs appear to be a new and powerful "weapon" for cancer therapies. These targeting drugs are directed against specific molecules that are over-expressed or where certain unique factors are aberrantly expressed either in cancer cells or in diseased cell sites. Compared with traditional chemotherapeutic drugs, these targeting drugs have the advantages of high specificity, efficacy and less side Read More

Osteosarcoma (OS) is the most common pediatric bone cancer in children and young adults. Previous studies have suggested the importance of osteoblast activity in OS tumorigenesis and metastasis, as OS is characterized by abnormal bone formation, while osteoblast is the predominant cell type both in OS and in metastatic tumor tissues. RUNX2 is a known essential transcription factor for osteoblast differentiation. RUNX2 ha Read More

Nowadays, dietary guidelines acknowledge the therapeutic role of omega-3 polyunsaturated fatty acids, as the most important class of fatty acids, against different human diseases. During the last two decades, the average level of consumption of omega-3 polyunsaturated fatty acids has increased from 0.1 to 0.2 g per day. Omega-3 polyunsaturated fatty acids are a group of long-chain polyunsaturated fatty acids which a Read More

Natural products such as aromatase inhibitors have been the object of growing attention in recent years because of their potential to inhibit aromatase with fewer side effects and the possible translation of their current use as chemotherapeutic agents to future clinical applications in breast cancer chemoprevention. We have previously investigated CTet, a novel anticancer agent obtained from the broccoli-derived co Read More

Flavokawain A is a chalcone that can be found in the kava-kava plant (Piper methsyticum) extract. The kava-kava plant has been reported to possess anti-cancer, anti-inflammatory and antinociceptive activities. The state of the immune system, and the inflammatory process play vital roles in the progression of cancer. The immunomodulatary effects and the anti-inflammatory effects of flavokawain A in a breast cancer Read More

Inhibition of the Hsp90 function is an essential therapeutic approach and several inhibitors were designed as anti-cancer agents. These inhibitors are ATPases and they aim to deregulate Hsp90 folding function. ATPase proteins are common in human metabolism but they form nonspecific targets. Hsp90 functions as dimer with coordinating chaperones. Heat Shock Organizing Protein (Hop) forms a bridge between Hsp90 an Read More