Synthetic cannabinoids (SCs) were originally created for the scientific investigation of two cannabinoid receptors, CB1 and CB2, but have made their way to the streets as “safe” and “legal” alternatives to marijuana.
The problem is that these SCs engage the cannabinoid receptors more completely and with higher affinity than anything derived from marijuana. As a result, SCs can produce serious side effects that often require medical attention. In fact, you are 30 times more likely to seek emergency medical attention following the use of an SC than with natural cannabinoid sources like marijuana. Continue reading “Bioassay for Cannabinoid Receptor Agonists Designed with NanoBiT™ Techology”
G protein-coupled receptors (GPCRs) are the most prevalent gene family in the human genome. They are involved with everything from our sense of smell to immune system function to tumor growth. Unsurprisingly, GPCRs have been a hotbed for research and development. Of the 7,038 approved drugs analyzed for this blog post, I found that 29% of them target Class A (Rhodopsin-like) GPCRs, and 35% target any GPCR. In the spirit of Internet pop culture, I made a “quiz” to see if you can guess the top 10 receptors by their ligand’s chemical structure.
G Protein Coupled Receptors represent one of the largest classes of cell surface receptors and one of the most important classes for drug targets. Fifty of the top 200 drugs target GPCRs. GPCRs respond to various stimuli like light, odors, hormones, neurotransmitters and others. They cover virtually all therapeutic areas. When a particular GPCR is implicated in a disease, researchers screen the GPCR and its signaling pathways, the hope being that promising therapeutic targets might be identified. Major G-protein families signal via secondary messengers like cAMP, which in turn activate a range of effector systems to change cell behavior and/or gene transcription. There are various approaches and methods to study GPCRs and measure the increase or decrease of intracellular cAMP. However, the fastest and the most sensitive among all methods is a plate based cAMP-Glo™ Assay. Continue reading “Practical Tips for HEK293 Cell Culture When Using cAMP-Glo™ Assay”