Recent Patents on Anti-Cancer Drug Discovery - Volume 8, Issue 1, 2013

Both increases in the basal cytosolic calcium concentration ([Ca2+]cyt) and [Ca2+]cyt transients play a major role in cell cycle progression, cell proliferation and division. Calcium influx and release from endoplasmic reticulum are the major routes involved in the variations in [Ca2+]cyt and past studies have clearly shown that calcium influx controls cell growth and proliferation in several cell types. Furthermore, various studi Read More

Calcium channels significantly contribute to many cellular processes, including such critical ones as proliferation, differentiation, and apoptosis. In prostate cancer, the influence of calcium channels has been known for over 30 years, with the first observations that calcium channel blockers affect the progression of cancer towards more aggressive phase. Later research identified additional classes of channel proteins having Read More

Blood vessels and endothelial cells (ECs) are highly versatile in order to accomplish local tissutal needs in the physiological and pathological conditions. Tumor vasculature, in particular, exhibits special morphological and functional features, partly due to the peculiarity of tumor-derived ECs (TECs). This is of great importance for the discovery of selective molecular targets potentially suitable to interfere with tumor growt Read More

In the nervous system, the neuronal nicotinic acetylcholine receptors (nAChRs) mediate fast excitatory postsynaptic potentials as well as slower paracrine actions of ACh. They are also widely expressed in non-nervous tissue, including the neoplastic, which is intriguing as smoking is an established risk factor for cancer. Moreover, recent evidence attributes to the gene cluster coding for the α3/α5/β4 nAChR subunits a rol Read More

K+ Channels form the largest family among ion channels. Besides regulating many physiological functions, K+ channels, being aberrantly expressed in different types of tumors, affect several hallmarks of cancer. In cancer cells, K+ channel activity regulates cell proliferation, resistance to apoptotic cell death, tumor angiogenesis, invasiveness and metastatic spread. Moreover, being expressed in cells of the tumor micro Read More

A range of experimental and clinical data suggests strongly (i) that metastatic progression in carcinomas is accompanied (maybe even preceded) by upregulation of functional voltage-gated sodium channels (VGSCs) and (ii) that VGSC activity enhances cancer cell invasiveness. First, this review outlines the available in vitro and in vivo evidence for the VGSC expression and its proposed pathophysiological role. Second, we questio Read More

Cancer cells and tissues, regardless of their origin and genetic background, have an aberrant regulation of hydrogen ion dynamics leading to a reversal of the intracellular to extracellular pH gradient (ΔpHi to ΔpHe) in cancer cells and tissue as compared to normal tissue. This perturbation in pH dynamics rises very early in carcinogenesis and is one of the most common patho-physiological hallmarks of tumors. Recently, there Read More