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Enzyme induction and inhibition

Enzyme induction is a process in which a molecule (e.g. a drug) induces (i.e. initiates or enhances) the expression of an enzyme.

Enzyme inhibition can refer to

If the molecule induces enzymes that are responsible for its own metabolism, this is called auto-induction (or auto-inhibition if there is inhibition). These processes are particular forms of gene expression regulation.

These terms are of particular interest to pharmacology, and more specifically to drug metabolism and drug interactions. They also apply to molecular biology.

History edit

In the late 1950s and early 1960s, the French molecular biologists François Jacob and Jacques Monod became the first to explain enzyme induction, in the context of the lac operon of Escherichia coli. In the absence of lactose, the constitutively expressed lac repressor protein binds to the operator region of the DNA and prevents the transcription of the operon genes. When present, lactose binds to the lac repressor, causing it to separate from the DNA and thereby enabling transcription to occur. Monod and Jacob generated this theory following 15 years of work by them and others (including Joshua Lederberg), partially as an explanation for Monod's observation of diauxie. Previously, Monod had hypothesized that enzymes could physically adapt themselves to new substrates; a series of experiments by him, Jacob, and Arthur Pardee eventually demonstrated this to be incorrect and led them to the modern theory, for which he and Jacob shared the 1965 Nobel Prize in Physiology or Medicine (together with André Lwoff).[1]

Potency edit

Index inducer or just inducer predictably induce metabolism via a given pathway and are commonly used in prospective clinical drug-drug interaction studies.[2]

Strong, moderate, and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by ≥80%, ≥50% to <80%, and ≥20% to <50%, respectively.[2]

References edit

  1. ^ Mulligan, Martin. . Archived from the original on 2007-11-16. Retrieved 2007-01-01.
  2. ^ a b "Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers". U S Food and Drug Administration Home Page. 2009-06-25. Retrieved 2019-01-31.

External links edit

enzyme, induction, inhibition, this, article, needs, additional, citations, verification, please, help, improve, this, article, adding, citations, reliable, sources, unsourced, material, challenged, removed, find, sources, news, newspapers, books, scholar, jst. This article needs additional citations for verification Please help improve this article by adding citations to reliable sources Unsourced material may be challenged and removed Find sources Enzyme induction and inhibition news newspapers books scholar JSTOR February 2021 Learn how and when to remove this message This article is about enzyme regulation at the gene expression level For the inhibition of enzymes at the enzyme level see Enzyme inhibitor Enzyme induction is a process in which a molecule e g a drug induces i e initiates or enhances the expression of an enzyme Enzyme inhibition can refer to the inhibition of the expression of the enzyme by another molecule interference at the enzyme level basically with how the enzyme works This can be competitive inhibition uncompetitive inhibition non competitive inhibition or partially competitive inhibition If the molecule induces enzymes that are responsible for its own metabolism this is called auto induction or auto inhibition if there is inhibition These processes are particular forms of gene expression regulation These terms are of particular interest to pharmacology and more specifically to drug metabolism and drug interactions They also apply to molecular biology Contents 1 History 2 Potency 3 References 4 External linksHistory editIn the late 1950s and early 1960s the French molecular biologists Francois Jacob and Jacques Monod became the first to explain enzyme induction in the context of the lac operon of Escherichia coli In the absence of lactose the constitutively expressed lac repressor protein binds to the operator region of the DNA and prevents the transcription of the operon genes When present lactose binds to the lac repressor causing it to separate from the DNA and thereby enabling transcription to occur Monod and Jacob generated this theory following 15 years of work by them and others including Joshua Lederberg partially as an explanation for Monod s observation of diauxie Previously Monod had hypothesized that enzymes could physically adapt themselves to new substrates a series of experiments by him Jacob and Arthur Pardee eventually demonstrated this to be incorrect and led them to the modern theory for which he and Jacob shared the 1965 Nobel Prize in Physiology or Medicine together with Andre Lwoff 1 Aryl hydrocarbon receptorPotency editIndex inducer or just inducer predictably induce metabolism via a given pathway and are commonly used in prospective clinical drug drug interaction studies 2 Strong moderate and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by 80 50 to lt 80 and 20 to lt 50 respectively 2 References edit Mulligan Martin Induction Archived from the original on 2007 11 16 Retrieved 2007 01 01 a b Drug Development and Drug Interactions Table of Substrates Inhibitors and Inducers U S Food and Drug Administration Home Page 2009 06 25 Retrieved 2019 01 31 External links editEnzymologic Gene Expression Regulation at the U S National Library of Medicine Medical Subject Headings MeSH Retrieved from https en wikipedia org w index php title Enzyme induction and inhibition amp oldid 1129883895, wikipedia, wiki, book, books, library,

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