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How does a drug stick to a protein and alter its function? Protein molecules are large, whereas drugs are much smaller than proteins. If a protein were the head of a life-size statue, a drug would be like an earplug sitting in the ear canal of the statue.



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Here is the surprising fact: All of the 20,000 or so drug products that ever have been approved by the U.S. Food and Drug Administration interact with just 2% of the proteins found in human cells.3



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This number of possible small molecules has been estimated to be on the order of 1060; that is “1” followed by 60 zeros. Thus, even testing a million compounds is not that many in terms of sampling a significant fraction of all possible small molecules. To get a sense of how big the number 1060 is, if all the possible drug molecules filled up the space of 10,000 different planets, then 1 million chemicals would be represented by just a single molecule on a single one of these planets. All of the remaining molecules on all of the planets would still remain to be tested.



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At this point, Dennis remarked, “You are confusing two different questions. First, there is the question of what you want. Only then should you consider the second question, which is how do you find a path to get there.” He went on to say that if I loved one apartment, then I should focus on finding a way to realize that goal rather than settling for something less desirable that would leave me unhappy. First, the goal. Then, the means. This straightforward view of the world is applicable to the problems facing academia and the pharmaceutical industry in discovering new drugs.



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There are more than 600 different kinases in humans.



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heralded as a defining moment for drug discovery. Imatinib was the first kinase-inhibiting drug approved, and the first time that a specific protein product of a genetic lesion in a tumor was directly targeted by a small molecule drug.