Drug Design Reviews - Online (Discontinued) - Current Issue

Angiotensin-converting enzyme (ACE) inhibitors effectively interfere with the renin-angiotensin system and exert various beneficial actions on cardiovascular system beyond their blood pressure-lowering effects. Controlled clinical trials have shown that ACE inhibitors improve endothelial function and vascular remodelling, and reduce the risk of myocardial infarction, stroke, and cardiovascular death. Data from experimen Read More

Angiotensin converting enzyme (ACE) inhibitors have a myocardial protective effect, especially against the ischemia/reperfusion injury induced during coronary artery bypass grafting (CABG). Indications, dose, suitable time, and duration of administration, however, are still controversial. The heart that has undergone CABG has many pathological features, such as infarction-associated hypertrophy, myocardial stunning, vulner Read More

Soft tissue sarcomas (STSs) belong to a rare, heterogeneous family of malignancies of mesenchymal origin. Inoperable or metastatic sarcomas typically show low responsiveness to conventional chemotherapy probably due to overexpression of several genes related to cell cycle control, cell maintenance, and DNA repair. The ecteinascidins (ETs) are potent and selective antitumor agents isolated from marine tunicades from t Read More

Drug development for pediatric tumors is slow in comparison with efforts focused on adult cancers. Present risk-based therapy for neuroblastoma, the most common extra-cranial solid tumor in children, is usually effective in intermediate risk patients but treatment of the advanced disease in children over 2 years of age is not satisfactory. Novel targeted therapeutics that are at early stages of preclinical and clinical developme Read More

In the last decade, several efforts have been made to comprehend the molecular basis of hypertension through the study of Angiotensin II antagonists (AT1 antagonists or class of SARTANs since they share the same suffix in their empirical name). The structural features which determine the pharmacophoric segments of SARTANs are examined using a combination of QSAR and conformational analysis. The final Read More

Tumor cell targeting is a promising drug delivery strategy. Folate receptor (FR) is a cellular marker selectively overexpressed in a significant fraction of human neoplasms. Folate derivatized liposomes loaded with therapeutic agents have been shown to be efficiently taken up and to exhibit selective cytotoxicity in receptor positive tumor cells. FRtargeted liposomes have thus been evaluated for the targeted delivery of a vari Read More