Current Medicinal Chemistry - Volume 20, Issue 38, 2013

Treatment of murine EL4 T cell lymphoma with N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer conjugates of doxorubicin (Dox) leads to complete tumor regression and to the development of therapy-dependent longlasting cancer resistance. This phenomenon occurs with two types of Dox conjugates tested, despite differences in the covalent linkage of Dox to the polymer carrier. Such a cancer resistance cannot fully Read More

Purpose: In pancreatic cancer median survival times range around 6, 6 to 6,9 months. Here we retrospectively analyzed the outcome of immunotherapy in the additional palliative treatment of pancreatic cancer with long antigen exposition dendritic cell therapy (LANEX-DC®) in 138 patients who were treated at our institution. Patients: Data were available of 134 patients (97.1%). The median interval between first dia Read More

G-quadruplex based DNA aptamers for human thrombin are promising pharmaceuticals as anticoagulants. Initially discovered 15-mer DNA aptamer (15-TBA) has a minimal G-quadruplex structure which is able to inhibit thrombin. 15-TBA was modified and extended to improve aptamer activity and in vivo stability providing 31-TBA, NU172, RA-36, and some others as successful examples. In this paper an interplay betwee Read More

Osteoporosis is classified as a public health problem due to its increased risk for fragility fractures. Osteoporotic fractures, in particular spine and hip fractures, are associated with a high morbidity and mortality, and generate immense financial cost. The World Health Organisation (WHO) based the diagnosis of osteoporosis on the measurement of bone mineral density (BMD) using dual-energy X-ray absorptiometry (DXA). Read More

We summarize the alterations of classical neurotransmitters and neuropeptides and the corresponding subreceptors involved in major depression. Neuronal circuits in the brainstem, hippocampus and hypothalamus are developed, since they can be used to derive a multimodal pharmacotherapy. In this sense, serotonin hypoactivity could occur through a strong presynaptic inhibition of glutaminergic neurons via Read More

Systemic fungal infections of humans and economically important animals are increasingly common throughout the world. These infections are severe and often hard to treat with existing safe, oral medications. Thus there has been increasing research on alternatives resulting in study of natural and synthetic inhibitors of 1,3-β-Glucan synthase (GS) and chitin synthase (CS)-enzymes important in the biosynthesis of fungal c Read More

Farnesyltransferase inhibitors (FTIs) have mainly been used in cancer therapy. However, more recently, investigations on these inhibitors revealed that FTIs can be used for the treatment of other diseases such as Progeria, P. falciparum resistant malaria, Trypnosomatid, etc. Hence the development of novel FTIs is an important task for the drug discovery program. Initially, numerous peptidomimetic FTIs were developed Read More

The issue of chiral drug is now a major theme in the design, discovery and development of new drugs. It has been shown for many pharmaceuticals that only one enantiomer contains the desired activity, and the synthesis of such drug molecules in their optically pure form is becoming increasingly important. Mitsunobu reaction was carried out between (R)- and (S)-3,4-dihydro-2H-1,5-benzoxathiepin-3-ol and purines un Read More

Essential hypertension is one of the major contributors to premature morbidity and mortality due to the incresased risk for coronary heart disease, stroke, renal disease, peripheral vascular disease and vascular dementia for both men and women. However, its basic causes remain unknown. In the present work we studied the activity of several proteolytic regulatory enzymes related to renin-angiotensin-system (RAS) (aminopept Read More