When chemists meet they talk about drugs

“You can make crystal meth in your lab?” asked my housemate who was pursuing a PhD in computer science. “Yes, it’s a fairly simple molecule. I haven’t looked but I bet that I won’t have trouble finding the chemicals needed to make it,” I said. At the time I was a lowly graduate student pursuing my PhD in organic chemistry, who was not keen on breaking any laws. So while I did not make any illegal drugs, I did spend three years in the lab making a molecule that could one day be a drug to treat colorectal cancer.

And while synthesis of illegal drugs hasn’t come up at the Lindau meeting (yet), no one should be surprised that a lot of people are talking about drugs. Chemists are bound to talk about one of their biggest contribution to humanity. Today, Aaron Ciechanover (Chemistry Nobel 2004) gave an excellent overview drug development since the time Egyptians chewed on the bark of willow trees to alleviate pain.

Credit: Louise Docker (flickr)

As Ciechanover pointed out, most drugs till the early 20th century such as salicylic acid and penicillin were found because of serendipity. Their immediate need and widespread use automatically made them “blockbusters”, drugs which made the manufacturers a lot of money.

It was only in the latter half of the 20th century that drug discovery was pursued more systematically. The process involved screening thousands of molecules to find the handful few that could attack the desired targets

Thanks to modern drugs, four times as many human beings live to be 70 as did in 1860. But the current methods are not the way forward for drug development in the 21st century, argued Ciechanover. Using the example of Angelina Jolie, he said that genetic analysis is only going to become cheaper and more accessible. This is bound to usher in the era of personalised medicine.

Ciechanover’s master class yesterday, which involved four young researchers talking about their work, was also about “new frontiers” in drug development. Mahmoud El-Sabahy from Assiut University in Egypt gave an excellent overview of the use of “nanoparticles” in diagnosing and treating diseases. The idea there is to use tiny particles (only few billionths of a meter long) that can be built to possess some special properties.

An example is their use in treating heart-related diseases. When a person suffers a heart attack, some of her heart cells are injured. Stem cells can repair this damage, but current methods limit the treatment. Stem cells have the power to transform into new heart cells and replace the injured ones, but for that to happen effectively doctors need to track the whereabouts of these cells. Nanoparticles can make that happen.

These nanoparticles have the property to be observed by shining lasers on them, or by hitting them with ultrasonic sound waves, or detect the tiny changes in their magnetic fields. When the nanoparticles are injected in stem cells, one of these three ways can be used to keep an eye on them and improve therapy many times.

There are other promising routes for new drugs that are emerging. Brian Kobilka (Chemistry Nobel 2012) spoke yesterday about the role of GPCRs, which are molecules that sit on the walls of cells as doormen. They detect chemical signals and convey those messages inside the cells. Many functions of the human body from smell and sight to heart rate modification is dependent on GPCRs. Not surprisingly, according to Kobilka about 40% of drug targets are GPCRs.

A similar picture emerges when you look at aquaporins, another class of molecules part of the cell wall. Their job is to control the flow of water. Manipulating them with the help of drugs may be the way to treat heart disease, brain edema after a stroke and even dry eye syndrome. Peter Agre (Chemistry Nobel 2003) will be speaking about his work with aquaporins tomorrow.

There are three big challenges that chemistry can solve (and most chemists would agree with them): explaining the origin of life, acquiring sufficient energy for future use and working on the constant need to improve human health. In the first two days, Nobel Laureates at the Lindau meeting have mainly addressed one of the three big challenges. I look forward to their take on the remaining two.

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