What is surprising is that before the computers electronic weights and many of the other modern advancements medical advancement were taking place. What is even more surprising is the way that the drugs were stumbled upon. Many of the scientists during the fifties knew that they were going in the right direction but few were able to be achieved because of the lack of technology. It is basically equivalent to having a specific thought “in the tip of your tongue.” You know what you are going to say but you just cant say it because it is not able to be said. Not much could be done in regards to the medicines because of the lack of technology, but they knew exactly what was needed. One such example was the drug known as Captapril.
Captapril became a pharmaceutical drug in 1975. The drug Captapril was a defense against the protein PNP. PNP is an enzyme which takes out the sugar and nitrogenous substances out of the cells. It then divides the purine form of the sugar, making it independent and creating or destroying in order to build more molecules such as DNA. But PNP separates anti-cancer and other helpful agents, and destroys the therapy provided by those agents. The goal was to create a drug which could inactivate PNP until therapy for these agents were complete. A computer was used to create a model of the protein in order to understand each aspect of this model.
The computers assessed the chemicals which could possibly fulfill the code of this protein, and begin fitting it into the simulated molecule. When it came to the real thing everything was accomplished the only problem was that the lack of technology in the 70’s led them only to tale pictures and study them with x-ray technology. This data revealed to them that that PNP was penetrable. The pictures also showed the shape of the active site region and the amino acids which constitute into the activity of the region of the protein. The three scientists grouped up and decided to fill up the purine binding region of the active site and then they could approach the sugar binding region and than the phosphate binding region. This would then cause a greater attraction between the drug and enzyme.
In order to fill the purine binding form, they had to make amino acids which would have carbon atoms rather than nitrogen atoms which would increase the attraction between itself and PNP. The substitution counteracted with one of their other solutions, but their method made it easier for them to correct themselves. The next step was to fill the sugar binding g region. The three amino acids layout in this were like water and oil, two were like water the other was like an oil. Neither had an affinity for one another. they saw the sugar pocket which was made up of benzene could be best fit with chlorine and carbon. The final job was to fill the phosphate binding site. The structural methods failed, but the crystallographic methods enabled them to arrive at their goal. It was now time to see their molecule in action, and it worked 100 times better than the controlled group. Now it had to be tested on humans.
Their goal was to develop PNP inhibitors that could extend the lifetime of synthetic nucleoside in animals had been accomplished within three years. This was done because there were only about 60 compounds involved in this experiment. Structured based drug design, created another door into the future of drug producing. This is probably how agouron pharmaceuticals came out with three drug which could help stop 46 different types of cold virus. But the obstacles ahead of it are many for many proteins are not in pure form., and solving the structure of protein is as difficult task as well. Still there is the friendly machine which could decode the difficult tasks.