Biological catalysts, central to all aspects of cellular function. Largest group of targets in the body 47%. Specialised binding sites that have certain substrates.
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V max
That maximum rate at which an enzyme can carry out a reaction
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Km
Substrate concentration at which the enzyme will work at 1/2 V max.
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Competitive Inhibitor
Block the enzyme's active site.
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Non-competitive Inhibitor
Bind to the enzyme somewhere other than the active site of the enzyme (allosteric site)
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DD Transpeptidases
DD Transpeptidases is a bacterial enzyme that catalyzes the transfer of the R-L-aca-D-alanyl moiety of R-L-aca-D-alanyl-D-alanine carbonyl donors to the γ-OH of their active-site serine and from this to a final acceptor.
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DD Transpeptidases Action
• Carries out crosslinking of peptidoglycan wall subunits for bacteria • Also known as penicillin binding protein (PBP) • Beta lactam antibiotics bind to and irreversibly inhibit DD Transpeptidase.
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Protein Chemical Warfare
Bacteria counter the impact of beta lactam drugs by producing an enzymatic defence system. Some forms of antibiotic resistance.
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HIV Protease
A retroviral aspartyl protease, enzyme involved with peptide bond hydrolysis in retroviruses, used in the life-cycle of HIV. Cleaves viral virion proteins required to form the active virus.
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Atazanavir/ Reyataz
Antiretroviral medication used to treat and prevent HIV/AIDS after a needlestick injury. Acts an inhibitor to HIV enzyme, protease in the HIV genome to suppress any infection.
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Targeting Human Enzymes
Changes in protein sequences caused by mutations leads to a host of human diseases. Drugs can be used to correct these changes.
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Angiontensis Converting Enzyme (ACE)
Renin-angiotensin system which controls blood pressure by regulating the volume of fluids. Converts the hormone angiotensin I to the active vasoconstrictor angiotensin II
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Ramipril
Inhibits ACE activity, decreases the production of angiotensin II. Increases risk of stroke, as it binds as a competitive inhibitor.
Provide relief from the symptoms of inflammation and pain. Reduce the synthesis of prostaglandins.
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Prostaglandins
Active lipid compounds called eicoanoids having diverse hormone life effects in animals. Derived enzymatically from fatty acid arachidonic acid.
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Substantial concentrations of ibuprofen
Attained in synovial fluid for nonsteroidal anti-inflammatory drugs. . Ibuprofen is eliminated following biotransformation to glucuronide conjugate metabolites that are excreted in urine.
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Protein Kinases
Integral part of signalling cascades within the cell. Hydrolyse ATP through covenant modification to modify protein function.
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Imatinib
Type of biological therapy called tyrosine kinase inhibition (TKI). Acts as chemical messengers.
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Bcr/Abl
Kinase domain that is hyperactive in chronic myelogenous leukaemia (CML)
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Allosteric Modulation
Ligands able to directly active a receptor by binding to an allosteric agonist. Can alter the overall protein shape.
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Allosteric Regulation
The regulation of an enzyme by binding an effector molecule at a site other than the enzyme's active site.
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Other cards in this set
Card 2
Front
That maximum rate at which an enzyme can carry out a reaction
Back
V max
Card 3
Front
Substrate concentration at which the enzyme will work at 1/2 V max.
Back
Card 4
Front
Block the enzyme's active site.
Back
Card 5
Front
Bind to the enzyme somewhere other than the active site of the enzyme (allosteric site)
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