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The sweeteners saccharin (SAC) and acesulfame K (ACE) recently entered the topic of anticancer human carbonic anhydrase (CA, EC 126.96.36.199) inhibitors as they showed to selectively inhibit the tumor-associated CAs IX/XII over ubiquitous CAs. A drug design strategy is here reported which took SAC and ACE as leads and produced a series of 2H-benzo[e][1,2,4]thiadiazin-3(4H)-one-1,1-dioxides (BTD). Many derivatives showed greater potency (KIs-CA IX 19.1-408.5 nM) and selectivity (II/IX SI 2-76) than the leads (KIs-CA IX 103, 2400 nM; II/IX-SI 56, >4) against CA IX/XII over off-target isoforms. A thorough X-ray crystallographic study depicted their binding mode to both CA II and IX-mimic. The most representative BTDs were characterized in vitro for their antitumor activity against A549, PC-3 and HCT-116 cancer cell lines both in normoxia and hypoxia. The two most effective compounds were assayed for their effect on several apoptosis markers, identifying promising leads for the development of new anticancer drugs.
This article was published in the following journal.
Name: Journal of medicinal chemistry
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During daily 3-h sessions, four rhesus monkeys had concurrent access to 16% alcohol (w/v) and saccharin. A response occurred when a monkey made mouth contact with the metal spout and thereby completed...
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In this study, the investigators aimed at evaluating the role of sweet taste receptors in the gastrointestinal tract (GIT). Intragastric administration of glucose, fructose or acesulfame-K...
The purpose of this study is to collect data to examine whether short-term consumption of non-caloric artificial sweeteners (NCASs), such as saccharin, can lead to changes in blood sugar l...
The purpose of this study is to collect data that will help researchers better understand the various causes of obesity and diabetes; particularly to understand how consumption of NCASs af...
This study will assess the impact of repeated sweet versus non-sweet food consumption on subsequent sweet and non-sweet food preferences and intakes
This study will assess the impact of repeated sweet breakfast consumption versus repeated non-sweet breakfast consumption on subsequent sweet and non-sweet food preferences and intakes
Chemical additives, such as aspartame, saccharin, and sucralose, that give a sweet taste to foods without contributing significant calories or promoting tooth decay. They are generally much sweeter than sucrose.
Flavoring agent and non-nutritive sweetener.
A plant species of the genus IPOMOEA, family CONVOLVULACEAE. Some cultivars are sweet and edible whereas bitter varieties are a source of SAPONINS. This sweet potato is sometimes referred to as a yam (DIOSCOREA).
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A cytoplasmic receptor and peroxin that contains a series of WD40 REPEATS and binds to PEROXISOME TARGETING SIGNAL 2. It is essential for protein import into PEROXISOMES; mutations in the human PEX7 gene are associated with PEROXISOMAL DISORDERS such as Type 1 CHONDRODYSPLASIA PUNCTATA, RHIZOMELIC.
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...
Radiology is the branch of medicine that studies imaging of the body; X-ray (basic, angiography, barium swallows), ultrasound, MRI, CT and PET. These imaging techniques can be used to diagnose, but also to treat a range of conditions, by allowing visuali...