Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 11, Issue 7, 2011

I would like to thank all the authors for their excellent contributions to the Focal Adhesion Kinase Signaling issue. I would also like to thank the journal for the invitation and the editorial staff for their expert help in the preparation of the second part of this issue. Focal Adhesion Kinase (FAK) is a 125 kDa protein that is localized at the focal adhesions. It plays a significant role in adhesion, motility, invasion, survival, proliferation Read More

Since its first description Focal Adhesion Kinase (FAK), a cytoplasmatic tyrosine kinase, has been implicated in the formation and progression of solid and liquid malignant tumors. Therefore orally available selective small molecule inhibitors of FAK have been developed, three of them (PF-562-271, PF-04554878 and GSK2256098) are already in clinical testing. This review discusses the recent data obtained from these Phase 1 tr Read More

Recent studies connect the FAK and Wnt/β-catenin signaling pathways, both which promote cancer when aberrantly activated in mammalian cells. Over-stimulation of either Wnt/β-catenin or FAK activities was independently shown to promote numerous types of human cancers, including colon, breast, prostate and ovary. Observations in different model systems suggest a complex and dynamic cross-talk between these two path Read More

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase which mediates integrin signaling from the sites of connection to the extracellular membrane known as focal adhesions. FAK mediates essential cellular processes including growth, proliferation, adhesion, migration, and survival through its functions as a molecular scaffold and as a kinase. FAK is frequently overexpressed and overactive in prostate cancer, which r Read More

Focal Adhesion Kinase plays a major role in cell adhesion, motility, survival, proliferation, metastasis, angiogenesis and lymphangiogenesis. In 2004, we have cloned the promoter sequence of FAK and found that p53 inhibits its activity (BBA, v. 1678, 2004). In 2005, we were the first group to show that FAK and p53 proteins directly interact in the cells (JBC, v. 280, 2005). We have shown that FAK and p53 proteins interact in the cytop Read More

Hyaluronan (HA) and hyaluronan synthases (HAS) have been implicated in cancer growth and progression. We previously have shown that HAS3 and HA mediate tumor growth in SW620 colon cancer cells, but the mechanism remains poorly understood. In addition, the effect of HAS3 inhibition on tumor growth with other cells lines has not been explored. We therefore hypothesized that inhibition of HAS3 in highly tumo Read More

Introduction: Esophageal cancer remains an aggressive disease with poor survival rates. FAK and IGF-1R are two important tyrosine kinases important for cell survival signaling and found to be upregulated in esophageal cancer. Our hypothesis is that a novel small molecule compound that disrupts FAK and IGF-1R protein-protein interactions (PPIs) would decrease the growth of human esophageal cancer. Methods: The Read More

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase implicated in cancer progression, and plays a vital role in integrating environmental signals from growth factors, extracellular matrix and mechanical forces. As a scaffolding protein, FAK interacts and regulates the activity of many signaling kinases including Src, VEGFR-3, p53, PI3k and IGF-1R. In turn, FAK activity is modulated by a complex network of regulators tha Read More

The Pax-5 gene encodes a B-cell-specific activator protein (BSAP) that plays a key role in B lymphocyte differentiation and embryogenesis. The deregulation of this transcription factor is also linked to B cell malignancies and recently to other cancers. More specifically, the downstream effects of Pax-5 promote cell-cell interactions and mediate the activation of adhesion genes which result in an epithelial phenotypic behavior of Read More

Drosophila modeling can be effectively used for comprehensive and refined analysis of tumorigenesis, including the discovery of therapeutic anti-cancer drugs and their testing [1]. The Drosophila lgl gene was the first animal tumor suppressor found and the first tumor-associated gene encoding cytoplasmic protein. We compared the gene ontology of two cancer-associated cytoplasmic proteins, Lgl and DFak56 (ortholog Read More

Extensive evidence supports involvement of electron transfer (ET), reactive oxygen species (ROS) and oxidative stress (OS) in the mechanism of many anticancer drugs. The common ET functionalities, usually present in the drug metabolites, are quinones (or precursors), metal complexes (or complexors), hydroxylamine and nitroso from ArNO2 or ArNH2, and conjugated imines (or iminium species). The ET agents function cat Read More

Cancer nanotherapeutics have shown promise in resolving some of the limitations of conventional drug delivery systems such as nonspecific biodistribution and targeting, lack of water solubility, low therapeutic indices, and poor oral bioavailability. Moreover, cancer nanotechnology has the potential of improving current approaches to cancer detection, diagnosis, and imaging. Recently, nanotechnology and molecular im Read More

At present cancer treatment is still a confusing problem. Great progress has been made in anti-tumor agents since a series of small molecules are approved by FDA as anti-tumor drugs. Nitroimidazoles is a kind of radiosensitizer with multiple bioactivities used in cancer treatment since 1950s. In this review, we focus on the development of nitroimidazoles as radiosensitizer, bio-reductive prodrug and other types of anti-tumor age Read More