A List I Wish Were Longer

What you’re admiring is a molecular view of a G-protein coupled receptor, or GPCR for short. These receptor proteins transmit all kinds of messages in the body, in response to things as diverse as odors and neurotransmitters, and they are one of the biggest (if not the biggest) classes of drug targets. The target of blockbuster blood thinner Plavix? A GPCR. Serotonin receptors, which come up everywhere from obesity research to schizophrenia research? They’re GPCR’s. (Read some of what we’ve written about GPCR’s at the Haystack). So far, it’s been extremely tough to determine what these proteins look like, which makes it that much harder to develop drugs that could manipulate their activities.

Researchers know that GPCR’s span cell membranes, snaking back and forth across them a total of seven times. But sometimes it’s the subtle details of structure that are important for understanding how they work. Protein structures are published quite frequently, but on the rare occasion when a GPCR structure is solved, it’s a big deal. Today Ph.D. biochemist Mary Canady (@Comprendia), founder of bioscience consulting group Comprendia, tweeted this list of the GPCR structures that have been determined so far, which she obtained via Peter Nollert at Emerald BioStructures (@reducentropy). I wish the list were longer.

Bonus pre-Friday happy hour info: Canady is tweeting from the Allosteric Modulator Drug Discovery Congress, where she is picking up tidbits galore about GPCR’s. If you want to know more about allosteric modulation (anything from what it is to what kinds of drugs are in the pipeline), read my backgrounder from last year. It mentions the Rolling Stones, valium, and alcohol. What’s not to like?

Author: Carmen Drahl

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