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Related Concept Videos

Enzymes02:34

Enzymes

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Inside living organisms, enzymes act as catalysts for many biochemical reactions involved in cellular metabolism. The role of enzymes is to reduce the activation energies of biochemical reactions by forming complexes with its substrates. The lowering of activation energies favor an increase in the rates of biochemical reactions.
Enzyme deficiencies can often translate into life-threatening diseases. For example, a genetic abnormality resulting in the deficiency of the enzyme G6PD...
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Induced-fit Model01:13

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Most chemical reactions in cells require enzymes—biological catalysts that speed up the reaction without being consumed or permanently changed. They reduce the activation energy needed to convert the reactants into products. Enzymes are proteins, that usually work by binding to a substrate—a reactant molecule that they act upon.
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Introduction to Mechanisms of Enzyme Catalysis01:13

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For many years, scientists thought that enzyme-substrate binding took place in a simple "lock-and-key" fashion. This model stated that the enzyme and substrate fit together perfectly in one instantaneous step. However, current research supports a more refined view scientists call induced fit. The induced-fit model expands upon the lock-and-key model by describing a more dynamic interaction between enzyme and substrate. As the enzyme and substrate come together, their interaction causes...
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Allosteric Regulation01:08

Allosteric Regulation

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Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
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Introduction to Enzymes01:22

Introduction to Enzymes

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The use of enzymes by humans dates to 7000 BCE. Humans first used enzymes to ferment sugars and produce alcohol without knowing that this was an enzyme-catalyzed reaction. Wilhelm Kuhne coined the term 'enzyme' in 1877 from the Greek words ‘en’ meaning ‘in’ or ‘within’ and ‘zyme’ meaning ‘yeast.’
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Catalytically Perfect Enzymes01:07

Catalytically Perfect Enzymes

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The theory of catalytically perfect enzymes was first proposed by W.J. Albery and J. R. Knowles in 1976. These enzymes catalyze biochemical reactions at high-speed. Their catalytic efficiency values range from 108-109 M-1s-1. These enzymes are also called 'diffusion-controlled' as the only rate-limiting step in the catalysis is that of the substrate diffusion into the active site. Examples include triose phosphate isomerase, fumarase, and superoxide dismutase.
 
Most enzymes...
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The evolution of small molecule enzyme activators.

Louise F Dow1, Alfie M Case1, Megan P Paustian1

  • 1Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center Omaha NE 68106 USA paul.trippier@unmc.edu.

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Researchers are exploring small molecules that activate enzymes, offering a new therapeutic approach for diseases linked to enzyme downregulation. This strategy complements traditional enzyme inhibition methods.

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Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Enzymes are crucial for physiological homeostasis, regulated by complex signaling pathways.
  • Traditional drug discovery targets enzyme inhibitors due to disease-related upregulation.
  • Enzyme downregulation in diseases necessitates novel therapeutic strategies.

Purpose of the Study:

  • To review advancements in identifying and developing non-kinase enzyme activators.
  • To explore the therapeutic potential of enzyme activators in various disease states.

Main Methods:

  • Literature review of scientific publications on enzyme activators.
  • Analysis of medicinal chemistry approaches for small molecule enzyme activator discovery.
  • Evaluation of therapeutic applications and disease intervention strategies.

Main Results:

  • Significant progress has been made in identifying non-kinase enzyme activators.
  • Small molecules capable of activating enzymes represent a promising therapeutic avenue.
  • Enzyme activation offers an alternative to inhibition for treating specific diseases.

Conclusions:

  • Non-kinase enzyme activators are emerging as valuable tools in drug discovery.
  • Targeting enzyme activation provides a complementary approach to enzyme inhibition.
  • Further research into enzyme activators holds potential for novel therapeutics.