Category: Second Column

Makriyannis Lab Determines Structure of the CB1 Receptor

Crystal Structure of the Human Cannabinoid Receptor CB1  was published in Cell October 20, 2016. Thanks to Dale Deutsch for sending the link. Seems like big news. Don’t know how we missed it. Highlights: •AM6538 is presented as a stabilizing, tight binding antagonist of CB1 •Crystal structure of human CB1 in complex with AM6538 is determined •Molecular docking predicts CB1 binding modes of THC and synthetic cannabinoids •Resolution of the binding pocket provides path for rational CB1 drug design Summary: Cannabinoid receptor 1 (CB1) is the principal target of Δ9-tetrahydrocannabinol (THC), a psychoactive chemical from Cannabis sativa with a wide range of therapeutic applications and a long history of recreational use. CB1 is activated by endocannabinoids and is a promising therapeutic target for pain management, inflammation, obesity, and substance abuse disorders. Here, we present the 2.8 Å crystal structure of human CB1 in complex with AM6538, a stabilizing antagonist, synthesized and characterized for this structural study. The structure of the CB1-AM6538 complex reveals key features of the receptor and critical interactions for antagonist binding. In combination with functional studies and molecular modeling, the structure provides insight into the binding mode of naturally occurring CB1 ligands, such as THC, and synthetic cannabinoids. This enhances our understanding of the molecular basis for the physiological functions of CB1 and provides new opportunities for the design of next-generation CB1-targeting pharmaceuticals.  ...

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It’s News in New York: Cannabis for the Elderly

The New York Times has broken the news that medicinal cannabis can be a boon for nursing home residents. The front-page  piece by Winnie Hu February 20 notes that California is far ahead of New York in making the herb available to the elderly. Hu reports that the Hebrew Home at Riverdale is “taking the unusual step of helping its residents use medical marijuana under a new program to treat various illnesses with an alternative to prescription drugs.” Whereas, “A medical marijuana education and support club started by residents of Rossmoor Walnut Creek, a retirement community east of San...

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Note to the MBC’s Marijuana Task Force

 The Medical Board of California’s Marijuana Task Force is weighing changes to the board’s guidelines governing MDs who issue approvals to patients, and they have solicited input from “interested parties.”  I’m putting together relevant material from O’Shaughnessy’s back issues to submit (interesting word). I strongly urge SCC members to read the two articles I’m sending the Task Force. (More will follow.) Understanding the history of the medical marijuana movement is as important —if you want that movement to advance— as understanding the role of the endocannabinoid system.  What follows is the start of my submission to the Task Force (working title: “I Thought You’d Never...

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Link to IOM 2.0 Release

The new Institute of Medicine Report on cannabis is going to be released today (January 12, 2017) at 1 p.m. East Coast Time. Here’s how to watch the presentation: Register for the WebEx. And here’s the IOM’s modest press release: In one of the most comprehensive studies of recent research on the health effects of recreational and therapeutic cannabis use, a new report from the National Academies of Sciences, Engineering, and Medicine offers a rigorous review of relevant scientific research published since 1999. This report summarizes the current state of evidence regarding what is known about the health impacts of...

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Fake Science Finds Funding

Syngenta, the Swiss-based agrochemical giant (just acquired by ChemChina), wants the bee die-off blamed on the varroa mite instead of on the pesticides they manufacture. In 2012 an English bee expert named James Cresswell  accepted funding from Syngenta (under heavy pressure from his employer, the University of Exeter). When his findings tended to exonerate the varroa mite, Syngenta leaned on him to revise his study. This low-key example is NY Times reporter Danny Hakim’s hook into a January 2 feature about the influence of corporate funding on scientific research. Major excerpts follow: Scientists who cross agrochemical companies can find themselves at...

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