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Related Concept Videos

Phase II Reactions: Methylation Reactions01:17

Phase II Reactions: Methylation Reactions

335
Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
The mechanism of methylation unfolds in two stages. The first stage sees a methyltransferase enzyme facilitating the transfer of a methyl group from S-adenosylmethionine (SAM) to the substrate, forming S-adenosylhomocysteine (SAH). The second stage involves further metabolism of SAH into homocysteine, which can be recycled...
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Mismatch Repair01:36

Mismatch Repair

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Overview
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Biosynthesis of Nucleic Acids01:28

Biosynthesis of Nucleic Acids

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Nucleic acid biosynthesis is a fundamental biochemical process that produces the purine and pyrimidine nucleotides essential for DNA and RNA synthesis. This pathway maintains a balanced nucleotide pool, preventing imbalances that could jeopardize genetic integrity and cellular function. Given the crucial role of nucleotides, their synthesis is tightly regulated to ensure proper cellular homeostasis.Purine BiosynthesisThe biosynthesis of purine nucleotides begins with ribose-5-phosphate, a...
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Phase II Reactions: Acetylation Reactions01:24

Phase II Reactions: Acetylation Reactions

341
Acetylation, a phase II biotransformation reaction, introduces an acetyl group to drugs or their metabolites. Acetyltransferase enzymes facilitate this reaction, which resembles α-amino acid conjugation due to the addition of a functional group to the drug molecule.
The substrates for acetylation are typically drugs or their metabolites with an amino, sulfonamide, or hydrazine functional group. Acetylation can occur at several points in the drug molecule, including primary, secondary, and...
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Master Transcription Regulators02:23

Master Transcription Regulators

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Master transcription regulators are regulatory proteins that are predominantly responsible for regulating the expression of multiple genes. Often these genes work in concert to drive a  complex process. Activation of a master transcription regulator can lead to a cascade of transcriptional activation necessary for that outcome. These regulators can directly bind to the regulatory sequences of the various genes involved, or they can indirectly regulate transcription by binding to regulatory...
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Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

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Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein....
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Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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Methyltransferases: Functions and Applications.

Eman Abdelraheem1, Benjamin Thair2, Romina Fernández Varela3

  • 1Biocatalysis, Department of Biotechnology, Delft University of Technology, Van der Maasweg 9, 2629 HZ, Delft (The, Netherlands.

Chembiochem : a European Journal of Chemical Biology
|June 12, 2022
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Summary
This summary is machine-generated.

This review explores S-adenosylmethionine (SAM)-dependent methyltransferases, detailing their structure, mechanisms, and synthetic applications. It covers drug targeting, cofactor utilization, and the potential of SAM analogues for compound diversification.

Keywords:
S-adenosyl-l-methioninebiocatalysisenzymesmethyltransferases

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Area of Science:

  • Biochemistry and Organic Chemistry
  • Enzymology and Drug Discovery

Background:

  • S-adenosylmethionine (SAM) and its dependent methyltransferases are crucial in biological methylation.
  • Understanding these enzymes is key for developing novel therapeutics and synthetic strategies.

Purpose of the Study:

  • To provide a comprehensive overview of the state-of-the-art in SAM-dependent methyltransferases.
  • To explore their structural diversity, mechanistic aspects, and applications in synthesis and drug development.

Main Methods:

  • Review of current literature on SAM-dependent methyltransferases.
  • Analysis of structural classifications and mechanistic studies.
  • Evaluation of synthetic approaches utilizing SAM and its analogues.

Main Results:

  • Detailed classification and mechanistic insights into SAM-dependent methyltransferases.
  • Assessment of catalytic SAM as a drug target and cofactor in synthesis.
  • Exploration of SAM supply, regeneration, and analogue utilization.

Conclusions:

  • SAM-dependent methyltransferases offer significant potential for synthetic applications and compound diversification.
  • Further research into SAM analogues and enzyme mechanisms can drive innovation in drug discovery and chemical synthesis.