The metabolic enzyme fatty acid synthase (FASN) is responsible for the endogenous synthesis of palmitate, a saturated long-chain fatty acid. In contrast to most normal tissues, a variety of human cancers overexpress FASN. One such cancer is cutaneous melanoma, in which the level of FASN expression is associated with tumor invasion and poor prognosis. We previously reported that two FASN inhibit...

One of the fundamental principles of pharmacology is that most drugs have side effects. Although considerable attention is paid to detrimental side effects, drugs can also have beneficial side effects. Given the time and expense of drug development, it would be particularly exciting if a systematic method could be applied to reveal all of the activities, including the unappreciated actions, of ...

The aim of this review article is to discuss the Emax pharmacodynamic model. An essential component of drug development is to understand the dose-response relationship of a pharmaceutical compound under identical condition and find out an optimal dose to achieve targeted drug level for maximal desired pharmacological response. The current article represents the mathematical considerations of Em...

Fatty acid synthase (FASN) is the metabolic enzyme responsible for the endogenous synthesis of the saturated long-chain fatty acid palmitate. In contrast to most normal cells, FASN is overexpressed in a variety of human cancers including cutaneous melanoma, in which its levels of expression are associated with a poor prognosis and depth of invasion. Recently, we have demonstrated the mitochondr...

O rlistat is a drug frequently prescribed as an adjuvant in weight control therapy (1–2). Orlistat inhibits gastric and pancreatic lipases in the lumen of the gastrointestinal tract to decrease the systemic absorption of dietary fat (1,2). In clinical trials, steatorrhoea and other gastrointestinal disorders are the most frequently reported side effects (3). Other reported adverse effects inclu...

objective(s):the current study was aimed to determine the bioactive constituents and biological effects of the crataegus monogyna ethanolic extracts from bark, leaves and berries on hypercholesterolemia. materials and methods: oleanolic acid, ursolic acid, quercetin and lupeol concentrations were quantified by hplc. total phenol content and radical scavenging activity of extracts were also meas...

BACKGROUND The prevalence of obesity in developed societies is increasing. Obesity is associated with an increased risk of co-morbidity, including cardiovascular disease and diabetes. Following the withdrawal of fenfluramine and dexfenfluramine, interest has focused on a novel anti-obesity drug orlistat. OBJECTIVE To systematically assess the clinical effectiveness and cost-effectiveness of o...

UNLABELLED The XENDOS study showed that behavioural and pharmacological therapy can decrease the risk of metabolic disorders in obese patients. METHODS A probabilistic Bayesian Markov model simulating the outcomes of orlistat treatment on the obese Italian population has been developed with the WinBUGS software. The model integrates an algorithm to estimate cardiovascular risk based on Framin...

Introduction Among all cancers, endometrial cancer is most strongly associated with obesity, more than 65% of cancers attributable to obesity and being overweight. Fatty acid synthase (FAS), a key lipogenic enzyme, expressed in tumors worse prognosis for this disease. Orlistat, an FAS inhibitor, FDA-approved weight loss medication that has demonstrated anti-tumor activity variety preclinical mo...

The present study assessed the potential of the sodium glucose-linked transporter (SGLT)-2 inhibitor empagliflozin to decrease body weight when administered alone or in combination with the clinically effective weight-loss agents orlistat and sibutramine in obese rats fed a cafeteria diet. Female Wistar rats were exposed to a cafeteria diet to induce obesity. Empagliflozin was dosed once daily ...