<< Chapter < Page Chapter >> Page >

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 which rates. This determination is tightly controlled. In certain cellular environments, enzyme activity is partly controlled by environmental factors, like pH and temperature. There are other mechanisms through which cells control the activity of enzymes and determine the rates at which various biochemical reactions will occur.

Regulation of enzymes by molecules

Enzymes can be regulated in ways that either promote or reduce their activity. There are many different kinds of molecules that inhibit or promote enzyme function, and various mechanisms exist for doing so. In some cases of enzyme inhibition, for example, 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 active site binding ( [link] ). On the other hand, in noncompetitive inhibition, an inhibitor molecule binds to the enzyme in a location other than an allosteric site and still manages to block substrate binding to the active site.

This plot shows rate of reaction versus substrate concentration for an enzyme in the absence of inhibitor, and for enzyme in the presence of competitive and noncompetitive inhibitors. Both competitive and noncompetitive inhibitors slow the rate of reaction, but competitive inhibitors can be overcome by high concentrations of substrate, whereas noncompetitive inhibitors cannot.
Competitive and noncompetitive inhibition affect the rate of reaction differently. Competitive inhibitors affect the initial rate but do not affect the maximal rate, whereas noncompetitive inhibitors affect the maximal rate.

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 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).

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 its 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 at a higher affinity.
Allosteric inhibitors modify the active site of the enzyme so that substrate binding is reduced or prevented. In contrast, allosteric activators modify the active site of the enzyme so that the affinity for the substrate increases.

Everyday connection

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

Drug discovery by looking for inhibitors of key enzymes in specific pathways

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

Consider statins for example—which is the name given to the class of drugs that reduces cholesterol levels. These compounds are essentially inhibitors of the enzyme HMG-CoA reductase. HMG-CoA reductase is the enzyme that synthesizes cholesterol from lipids in the body. By inhibiting this enzyme, the levels 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 effective in providing relief from fever and inflammation (pain), its mechanism of action is still not completely understood.

How are drugs developed? One of the first challenges in drug development is identifying the specific molecule that the drug is intended to target. 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 sufficient; 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. During this stage, chemists and biologists work together to design and synthesize molecules that can either block or activate a particular reaction. However, this is only the beginning: both if and when a drug prototype is successful in performing its function, then it must undergo many tests from in vitro experiments to clinical trials before it can get FDA approval to be on the market.

Questions & Answers

what is biology
Dada Reply
The scientific study of life.
juanita
the virus that causes mumps in humans is composed of a protein outer Shell containing a core of DNA
Daniel Reply
Basic science and applied science question about cancer
Joyce Reply
what are the importance of ATPs
Olatunji Reply
How can biology be studied from a microscopic approach to a global approach
Joyce Reply
The large central opening in the poriferan body is called
Chynna Reply
You go for a long walk on a hot day. Give an example of a way in which homeostasis keeps your body healthy.
Joyce Reply
You sweat.
juanita
sweating is your bodies way of keeping you from overheating.
juanita
Thank you
Joyce
what is biology
Neya Reply
biology is the study of life
IYANUYIMIKA
Biology is the study of Life
Brianna
is the branch of science which deals with the of living things.
Peter
what is metabolism
Sangam Reply
hi palz, what's the ?
Gbolajobi Reply
hi plz, what's the.
Atta
pls come a again
Gyamfi
Describe the steps and results of reintroducing wolves to Yellowstone National Park.
Natalia Reply
tag and release wolves into Yellowstone. wolves eventually reproduce and the pack grows. as wolves hunt they cull the sick and weak prey. the carcass that is left provides food for other species (scavengers and insect.. etc). this heals the circle of life and contributes to the biodiversity...
Will
before you know it species that are critical to the eco system return. having apex predators is crucial to an ecosystem... it helps run the deer and elk , etc around.
Will
example: there was a species of shrub/ plant that grows along river banks that moose love to eat.. the moose have no predator so they decimate that food source which also helps prevent erosion. when the wolves were reintroduced this changed. oddly enough this plant species started to repopulate in
Will
the areas where wolf feces sat and decayed
Will
which of the following statements about the parts of an egg are false?
Israel Reply
Monotremes include...?
Israel
medicinal plants including microbs
vijay Reply
,medicinal plants including microbes
vijay
what is biology
Siyanbola Reply
study of living organisms...
R0se
study of plants and animals
Divine
what is abiotic and biotic factors?
Hira Reply

Get the best Biology course in your pocket!





Source:  OpenStax, Biology. OpenStax CNX. Feb 29, 2016 Download for free at http://cnx.org/content/col11448/1.10
Google Play and the Google Play logo are trademarks of Google Inc.

Notification Switch

Would you like to follow the 'Biology' conversation and receive update notifications?

Ask