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Since the rates of biochemical reactions are controlled by activation energy, and enzymes lower and determine activation energies for chemical reactions, the relative amounts and functioning of the variety of enzymes within a cell ultimately determine which reactions will proceed and at what rates. This determination is tightly controlled in cells. In certain cellular environments, enzyme activity is partly controlled by environmental factors like pH, temperature, salt concentration, and, in some cases, cofactors or coenzymes.

Enzymes can also be regulated in ways that either promote or reduce enzyme activity. There are many kinds of molecules that inhibit or promote enzyme function, and various mechanisms by which they do so. In some cases of enzyme inhibition, an inhibitor molecule is similar enough to a substrate that it can bind to the active site and simply block the substrate from binding. When this happens, the enzyme is inhibited through competitive inhibition    , because an inhibitor molecule competes with the substrate for binding to the active site.

On the other hand, in noncompetitive inhibition    , an inhibitor molecule binds to the enzyme in a location other than the active site, called an allosteric site, but still manages to block substrate binding to the active site. Some inhibitor molecules bind to enzymes in a location where their binding induces a conformational change that reduces the affinity of the enzyme for its substrate. This type of inhibition is called allosteric inhibition    ( [link] ). Most allosterically regulated enzymes are made up of more than one polypeptide, meaning that they have more than one protein subunit. When an allosteric inhibitor binds to a region on an enzyme, all active sites on the protein subunits are changed slightly such that they bind their substrates with less efficiency. There are allosteric activators as well as inhibitors. Allosteric activators bind to locations on an enzyme away from the active site, inducing a conformational change that increases the affinity of the enzyme’s active site(s) for its substrate(s) ( [link] ).

The left part of this diagram shows allosteric inhibition. The allosteric inhibitor binds to the enzyme at a site other than the active site. The shape of the active site is altered so that the enzyme can no longer bind to the substrate. The right part of this diagram shows allosteric activation. The allosteric activator binds to the enzyme at a site other than the active site. The shape of the active site is changed, allowing substrate to bind.
Allosteric inhibition works by indirectly inducing a conformational change to the active site such that the substrate no longer fits. In contrast, in allosteric activation, the activator molecule modifies the shape of the active site to allow a better fit of the substrate.

Careers in action

Pharmaceutical drug developer

This photo shows several red capsule pills.
Have you ever wondered how pharmaceutical drugs are developed? (credit: Deborah Austin)

Enzymes are key components of metabolic pathways. Understanding how enzymes work and how they can be regulated are key principles behind the development of many of the pharmaceutical drugs on the market today. Biologists working in this field collaborate with other scientists to design drugs ( [link] ).

Consider statins for example—statins is the name given to one class of drugs that can reduce cholesterol levels. These compounds are inhibitors of the enzyme HMG-CoA reductase, which is the enzyme that synthesizes cholesterol from lipids in the body. By inhibiting this enzyme, the level of cholesterol synthesized in the body can be reduced. Similarly, acetaminophen, popularly marketed under the brand name Tylenol, is an inhibitor of the enzyme cyclooxygenase. While it is used to provide relief from fever and inflammation (pain), its mechanism of action is still not completely understood.

How are drugs discovered? One of the biggest challenges in drug discovery is identifying a drug target. A drug target is a molecule that is literally the target of the drug. In the case of statins, HMG-CoA reductase is the drug target. Drug targets are identified through painstaking research in the laboratory. Identifying the target alone is not enough; scientists also need to know how the target acts inside the cell and which reactions go awry in the case of disease. Once the target and the pathway are identified, then the actual process of drug design begins. In this stage, chemists and biologists work together to design and synthesize molecules that can block or activate a particular reaction. However, this is only the beginning: If and when a drug prototype is successful in performing its function, then it is subjected to many tests from in vitro experiments to clinical trials before it can get approval from the U.S. Food and Drug Administration to be on the market.

Questions & Answers

Species A has 12 pairs of chromosomes and Species B has 11 pairs of chromosomes. Explain what occurs during mitosis and during meiosis in the hybrid that allows normal development and growth from zygote to adult, but causes the adults to be sterile.
Christina Reply
Why does water move through a membrane?
Christina Reply
How many bones are in the human skeleton
Treasure Reply
203
Oyeleke
procce of digestion of proteins a long human alimentarycanal
Carson Reply
what are the properties of lipids?
Isiah Reply
They are: Fatty acids, fats, oils, waxes, phospholipid, glycolipids, steroids and some vitamins
Rachel
explain why a fresh water fish excrete ammonia
Leonard Reply
plz answer my question
Leonard
sorry i meant it has a nucleous unlike plant cells lol
Lailah
Ammonia is the end product of protein catabolism and is stored in the body of the fish in high concentrations relative to basal excretion rates. Ammonia, if allowed to accumulate, is toxic and is converted to less toxic compounds or excreted
Rachel
What are eukaryotic cells?
Nwosueke Reply
cell with no nucleous so not a plant cell
Lailah
eukaryotic cells are membrane bound organelles that have a membrane bound nucleus
ojeen
where does the cell get energy for active transport processes?
A'Kaysion Reply
IDK maybe glucose
Lailah
what is synapsis
Adepoju Reply
how many turns are required to make a molecule of sucrose in Calvin cycle
Amina Reply
why Calvin cycle occurs in stroma
Amina
why do humans enhale oxygen and exhale carbondioxide?
Maryam Reply
why do humans enhale oxygen and exhale carbondioxide? For the purpose of breaking down the food
dil
what is allele
uzoka Reply
process of protein synthesis
SANTOSH Reply
what is cell
Zulf Reply
a cell is a smallest basic, structural and functional unit of life that is capable of self replication
Lucas
why does a fresh water fish excrete ammonia
Leonard
plz answer my question
Leonard
Ammonia is a toxic colorless gas and when its inside the fish biological system is converted to a less toxic compound then excreted in the form of urea. However too much ammonia will kill the fish " Ammonia Poisoning " which is a very common disease among fish.
This
what is cytoplasm
uzoka Reply
cytoplasm is fluid of cell.
Deepak

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Source:  OpenStax, Concepts of biology. OpenStax CNX. Feb 29, 2016 Download for free at http://cnx.org/content/col11487/1.9
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