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from the how-to-make-a-heavy-methyl-band dept.
Newly discovered 'magic methyl' reaction could turbocharge the potency of some drugs:
For years, drug discovery chemists have struggled to streamline a process that can boost a drug's potency up to 2000-fold: "magic methylation." The reaction sweeps out single hydrogen atoms and replaces them with methyl groups—reshaping the drug molecule to more easily interact with its biological targets. But carrying out this sleight of hand is so difficult that few researchers even try. Now, a team of chemists reports it has created a new catalyst that performs this delicate exchange with ease on a wide variety of druglike molecules, an advance that could lead to novel treatments for everything from cancer to infectious diseases.
"This paper is just stunning," says Tim Cernak, an organic chemist at the University of Michigan, Ann Arbor, who was not involved in the research. The new catalyst manages the reaction in one easy step—a huge improvement on previous multistep methods that were expensive and time-consuming. "This is the wish [of] every drug hunter," Cernak says. "It really is a dream reaction."
[...] This could help "across the board" in drug discovery, says David Rees, chief scientific officer of Astex Pharmaceuticals. Where adding a methyl group does increase a drug's potency, doctors may be able to give their patients less of a drug. That could improve safety and reduce side effects. Among the drugmakers he knows, Rees says, "Everyone will jump on this."
Posted in: Chemistry DOI: 10.1126/science.abb7567.
(Score: -1, Offtopic) by Anonymous Coward on Tuesday March 24 2020, @10:47AM
(Score: 0) by Anonymous Coward on Tuesday March 24 2020, @01:15PM (1 child)
2000 times more potent! Clears communities of junkies overnight!
(Score: 3, Funny) by DannyB on Tuesday March 24 2020, @02:32PM
It may be 2000 times more potent, but can the researchers find a way to compensate for this by making it 2000 times the price per dose?
That may take wizardry that mere scientists cannot achieve. Enter the MBAs!
The lower I set my standards the more accomplishments I have.
(Score: 0) by Anonymous Coward on Tuesday March 24 2020, @02:05PM (2 children)
I prefer peanut butter.
(Score: 0) by Anonymous Coward on Tuesday March 24 2020, @02:24PM (1 child)
It will make you brave enough to get more peanut butter.
(Score: 2) by DannyB on Tuesday March 24 2020, @02:35PM
I can personally recommend against using peanut butter as a substitute. Stick to regular CPU thermal grease on the heat sink.
Always beware of a software developer carrying tools into a server room to "fix something minor".
The lower I set my standards the more accomplishments I have.
(Score: 2) by Megahard on Tuesday March 24 2020, @03:31PM
Also a name for Methyl fluorosulfonate [wikipedia.org]. Back in my lab days, it was the methylating reagent of last resort due to its volatility combined with extreme toxicity by inhalation.
(Score: 5, Interesting) by Hartree on Tuesday March 24 2020, @03:43PM
The group that did this at the University of Illinois is one of my main customers for lab equipment repair.
Unfortunately, my shop is shut down at the moment due to COVID-19, so I haven't had a chance to talk to Raundi or Kaibo (the grad students who are the lead authors on this) about what they've been up to with this.
(Score: 0) by Anonymous Coward on Tuesday March 24 2020, @03:52PM (3 children)
I've been juicing up plain water with a couple of methyl groups for years now. I can assure you it is 2000+ times more potent.
(Score: 1) by pTamok on Tuesday March 24 2020, @07:53PM (1 child)
Drinking dimethyl ether [wikipedia.org] isn't my kind of fun.
(Score: 0) by Anonymous Coward on Wednesday March 25 2020, @10:26AM
Or maybe he meant to say that he replaced one of the hydrogen atoms with two methyl groups back to back.
(Score: 0) by Anonymous Coward on Wednesday March 25 2020, @02:20AM
Off topic? Likely unrelated process--
Grapefruit tends to make certain drugs more potent, like coumadin for blood clotting (thinner). I've known several heart patients that took this for years...had constant problems with bruising and eventually had internal bleeding. If I get to the point where I need coumadin, I'm going to talk with the doc about a standard amount of grapefruit juice every day, so the coumadin dose will be less.
(Score: 2) by sonamchauhan on Wednesday March 25 2020, @01:41AM
Methylation of DNA (epigenetic changes)
Methylation of proteins (homocysteine metabolism).