CHAPTER 20 - Enzymes and Drug Design (MOL S11)

CHAPTER 20 - Enzymes and Drug Design (MOL S11) - Chapter...

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Chapter 20: Enzymes and Drug Design 1 CHAPTER 20: ENZYMES AND DRUG DESIGN 20.1 INTRODUCTION: What Has Been the Impact of Anti-HIV Drugs? Anti-HIV drugs have significantly reduced the number of AIDS-related deaths in the United State. 20.2 PRINCIPLES OF ENZYME INHIBITION 20.2.1 What is Enzyme Inhibition? Enzyme inhibitors bind to the active site and prevent enzymatic conversion of substrate to product. 20.2.2 Enzyme Inhibition and Drug Design Effective enzyme inhibitor drugs can function as “transition state analogs” or “suicide inhibitors.” 20.3 HIV PROTEASE INHIBITORS 20.2.1 HIV Protease Revisited HIV protease enzymes cut polypeptide chains into smaller components that allow HIV to assemble. 20.3.2 Designing an Effective HIV Protease Inhibitor Protease inhibitor drugs contain a region that mimics the reaction’s tetrahedral transition state. 20.3.3 Has Protease Inhibitor Therapy Defeated HIV? HIV evolves rapidly in response to protease drug therapy. 20.4 ASPIRIN AND “SUPER-ASPIRINS” 20.4.1 Aspirin is a “Suicide Inhibitor” Aspirin is “suicide inhibitor” that transfers a functional group to the active site of cyclo-oxygenase. 20.4.2 “Super Aspirins”: The COX-2 Inhibitors COX-2 inhibitors selective inhibit the variant of cyclo-oxygenase that is responsible for inflammation. 20.5 HOW ARE NEW DRUGS TESTED AND APPROVED? New drugs must pass a series of laboratory and clinical trials to show they are safe and effective. 20.6 CHAPTER SUMMARY
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Chapter 20: Enzymes and Drug Design 2 20.1 INTRODUCTION: What Has Been the Impact of Anti-HIV Drugs? In 1981, when AIDS first emerged in the United States as a major health threat, there was little that physicians could do to help their patients. A diagnosis of AIDS was almost invariably a death sentence; the only question was how long the patient would survive. Today the diagnosis is much more hopeful. Figure 20.1 shows the number of AIDS- related deaths during a 20-year span from 1981 to 2001. The number of fatalities from this disease increased sharply from 1981 through the early 1990s, but there was a rapid decrease in AIDS deaths that begins in 1995. Part of this change can be attributed to public health efforts to reduce the spread of HIV infections. But an important contribution to reduced AIDS mortality was the introduction in 1995 of a new class of drugs called HIV protease inhibitors . As you learned in the previous chapter, HIV protease is an essential enzyme for HIV replication; it cuts long polypeptide chains and allows new viruses to assemble. A protease inhibitor drug binds to the active site of the enzyme and inhibits its function, thereby slowing the ability of HIV to replicate. 0 10 20 30 40 50 60 1980 1985 1990 1995 2000 Year AIDS deaths (thousands) Figure 20.1 The number of AIDS-related death in the United States from 1981 to 2001.
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CHAPTER 20 - Enzymes and Drug Design (MOL S11) - Chapter...

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