Current Medicinal Chemistry - Volume 18, Issue 11, 2011

During the last three decades, the advances in medical technology have elucidated many of the aspects of genetic and epigenetic pathways that commence the evolution of neoplasia. Standard therapeutic interventions include local control (surgery and/or radiotherapy) along with a combination of chemotherapeutic regimens for a systemic approach. Nevertheless, the appearance of genetically determined resistanc Read More

The endocannabinoid system comprises the cannabinoid receptors type 1 (CB1) and type 2 (CB2), their endogenous ligands (endocannabinoids), and the proteins responsible for their biosynthesis and degradation. This ubiquitous signalling system, that has attracted a great deal of scientist interest in the past 15 years, regulates several physiological and pathological functions. In mammals, among other functions, the endoc Read More

Bone disease is a common complication of metastatic solid tumors but also of primary hematological malignancies such as multiple myeloma. Our understanding of the molecular mechanisms underlying the development of bone disease by solid tumors and multiple myeloma has been significantly improved. A complex inter-dependence exists between bone disease and malignant cell growth, creating a vicious cycle of Read More

Treatment of metastatic colorectal cancer (mCRC) has progressed significantly over the last years, particularly with the introduction of targeted therapies. Two groups of agents targeting either the epidermal growth factor receptor (EGFR) or the vascular endothelial growth factor (VEGF) have been integrated into clinical practice. Currently available agents with established role include the anti-EGFR monoclonal antibodies (mAb Read More

Non-Small-Cell Lung Cancer (NSCLC) with somatic mutations of the epidermal growth factor receptor (EGFR) is anticipated to respond to small-molecule tyrosine kinase inhibitors (TKIs) of the EGFR tyrosine kinase. There are, however, patients with EGFR mutated tumors who do not demonstrate tumor response. The most widely accepted mechanism of ‘de novo’ (inherent) resistance to these TKIs involves mutations Read More

Despite declining incidence in developed countries, gastric cancer is still the second cause of cancer death worldwide, while proximal gastric cancer is increasing in incidence. Cytotoxic combinations of platinum salts, fluoropyrimidines with or without taxanes or anthracyclines improved response rates but failed to improve the median survival of patients with advanced gastric cancer beyond the 12-month benchmark. Novel ration Read More

As of today, advanced non-small cell lung cancer is still an incurable disease. However, recent researches on the biology of adenocarcinoma have led to considerable progress in the treatment of this subgroup of patients. The administration of bevacizumab and pemetrexed as first-line therapy, erlotinib in the maintenance phase and erlotinib again combined with vandetanib as second-line therapy, gives patients with lung adeno Read More

Surgery has been the mainstay of renal cell carcinoma (RCC) treatment for resectable tumours. In stages I-III disease, nephrectomy is the standard of care and may be curative. Historically, patients presenting with stage IV disease may achieve improved survival with debulking nephrectomy, which is commonly performed prior to systemic therapy. The response rate of immunotherapy is low, with a smaller percentage exhibiti Read More

Post translational modification of histones and non-histone proteins by acetylation play a key role in tumourigenesis. Histone deacetylases (HDACs) are enzymes involved in remodelling of chromatin by deacetylating the lysine residues and play a pivotal role in epigenetic regulation of gene expression. An aberrant activity of HDACs has been documented in several types of cancers and HDACs have emerged as an attractive Read More

Cinnamic acid and its phenolic analogues are natural substances. Chemically, in cinnamic acids the 3-phenyl acrylic acid functionality offers three main reactive sites; substitution at the phenyl ring, addition at the α,β-unsaturation and the reactions of the carboxylic acid functionality. Owing to these chemical aspects cinnamic acid derivatives received much attention in medicinal research as traditional as well as recent syntheti Read More

Matrix metalloproteinases (MMPs) are a large family of calcium-dependent zinc- containing endopeptidases, which are responsible for the tissue remodeling and degradation of the extracellular matrix (ECM), including collagens, elastins, gelatin, matrix glycoproteins, and proteoglycan. The inappropriate expression of these MMPs constitutes part of the pathogenic mechanism in several diseases, therefore they are subject to Read More

Tuberculosis is a major global health challenge and is far from being controlled. Development of resistance to currently available drugs due to the successful adaptation of the pathogen has been a major contributing factor for its control failure. Presently, there is an immense interest in identification of pathways, unique to the intracellular environment that could be utilized for the development of new and better drugs. In Read More