Chapter 5: Problem 2
If you wanted to inhibit an enzyme in a microorganism that is also in humans, what approaches would you take in your research?
Chapter 5: Problem 2
If you wanted to inhibit an enzyme in a microorganism that is also in humans, what approaches would you take in your research?
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Get started for freeS-Adenosylmethionine (SAM) is biosynthesized from methionine and ATP, catalyzed by methionine adenosyl transferase. The mechanism is shown below. a. Design a competitive reversible inhibitor for this enzyme. b. Design a multi-substrate analogue inhibitor, and show the basis for your design.
Why would you want to design a drug that is an enzyme inhibitor?
a. Two isoforms of an enzyme were discovered; isoform-1 produces a hormone that causes muscle spasms and isoform-2 makes another hormone from the same substrate that lowers cholesterol levels. What would you do to prevent muscle spasms without raising cholesterol levels? b. If the active sites of isoform-1 and \(-2\) are the same except isoform-1 has a cysteine residue and isoform-2 has a phenylalanine residue at that same position, what two approaches would you take for a muscle spasm drug without a cholesterol level increase side effect?
What advantage does a slow, tight-binding inhibitor have over a simple reversible inhibitor?
GABA aminotransferase catalyzes a PLP-dependent conversion of GABA to succinic semialdehyde (see Section 5.3.3.3.1). a. Draw a mechanism for how 6 inactivates this enzyme. b. A hypothetical anticonvulsant drug that inhibits GABA aminotransferase was given to a patient in overdose quantities. Not only did the patient stop convulsing, but he went into a coma. If the problem was that the GABA concentration became too high, mention two possible solutions to the problem.
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