Current Medicinal Chemistry - Volume 17, Issue 10, 2010

Fulvestrant is a novel endocrine therapy for breast cancer, with a unique structure and mode of action. It binds competitively to the oestrogen receptor (ER), with high affinity, and downregulates ER by functional blockade and increased turnover. Fulvestrant has reached the clinic via extensive pre-clinical and clinical trials, which demonstrated fulvestrant's unique characteristics and showed that they translate to equiv Read More

2,3-dihydrobenzo[b][1,4]oxathiine represents a valuable pharmacophoric heterocyclic nucleus known since very long time. Initially, together with some patents reporting the use of these compounds as herbicides or lipogenesis inhibitors, several papers reported their ability as melatonin, histamine and serotonin receptor ligands, α-adrenoreceptor blockers as well as non-glycoside sweeteners. This wide range of biological Read More

Malaria is a major worldwide public health threat with worrying social and economic burdens due to the rapid emergence of multidrug-resistant Plasmodium falciparum strains. As a result, there is an urgent need to find novel drugs that might overcome clinical resistance to marketed antimalarials. In recent years, the mitochondrial electron transport chain (mtETC) has been explored for the development of new antim Read More

The highly conserved heat-shock proteins (HSPs) from mammals and microbial reagents are among the immunogenic proteins. Their expression is induced in response to a wide variety of physiological and environmental insults. Their functions as molecular chaperones allow cells to adapt to gradual changes in their environment and to survive in otherwise lethal conditions. Although the role of HSPs in atherosclerosis remains Read More

Acute kidney injury (AKI) is a syndrome characterized by an acute renal cell injury that leads to sudden loss of renal function. There are currently no clinically validated treatments for AKI besides substituting renal function by dialysis. However, new biomarkers will allow an earlier diagnosis, thus providing a window of opportunity for therapeutic intervention. Acute kidney injury (AKI) is a syndrome characterized by an acute r Read More

The study of neuroscience has vastly benefited from the use of brain slices. This preparation has been fundamental for the understanding of the cellular basis of nervous system function as well as for the study of the mechanisms involved in neuronal network dysfunction. This experimental model provides flexible access, and control of, specific neural circuits and maintains their basic properties, allowing them to reproduce Read More

In the last decade, there has been enormous progress in our understanding of Frontotemporal Lobar Degeneration (FTLD). Published clinicopathological series have clearly demonstrated an overlap between the clinical syndromes subsumed under the term frontotemporal dementia and the Progressive Supranuclear Palsy (PSP), and the Corticobasal Degeneration (CBD) syndrome. From a neuropathological Read More