Antibiotic Classification and General Information
Protein synthesis inhibitors
Major groups: aminoglycosides, tetracyclines, macrolides
General mechanism of action: Protein synthesis inhibiting antibiotics primarily target the
bacterial ribosome (70S) which is made up of a small, 30S subunit and a large, 50S subunit. A
ribosome is an essential, complex molecule made up of proteins and RNA and is responsible for
synthesizing proteins. Aminoglycosides, macrolides, and other protein synthesis inhibitors target
and prevent specific stages of protein synthesis at specific locations on 70S ribosomes. Bacterial
death occurs because the cell cannot make proteins required for essential cellular processes.
Effects on humans – Humans, and other eukaryotic cells synthesize proteins using a 80S (not
70S) ribosome which is not targeted by these inhibitors. (other side effects are possible)
Nucleic acid synthesis inhibitors
Major groups: Antifolates, topoisomerase inhibitors (floroquinolones)
General mechanism of action: These antibiotics target different stages and pathways of nucleic
acid (DNA, RNA…) synthesis. In summary, antifolates (includes sulfonamides) inhibit enzymes
involved in folate/folic acid (vitamin B9) synthesis. Folate is an essential ingredient for the
synthesis of pyrimidine and purines, two molecules found in nucleotides, the building blocks of DNA
and other nucleic acids. Topoisomerase inhibitors prevent DNA replication by inhibiting
topoisomerase activity. Toposiomerases are enzymes that relieve DNA supercoil stress during DNA
replication. By inhibiting topoisomerase activity, DNA replication is greatly hindered and cell
division rate is diminished.
Effects on humans – Humans acquire folate from dietary sources, they do not have a synthesis
pathway for folate and are not affected by antifolates in the same way bacteria are.
Topoisomerases can be found in human cells; however the molecular makeup of human
topoisomerases differs from those found in bacteria. (other side effects are possible)
Cell wall synthesis inhibitors
Major groups: Beta-lactams (cephalosporins, penicillins)
General mechanism of action: As the name implies, this group of antibiotics
inhibits certain stages in bacterial cell wall synthesis. A major structural component
in the bacterial cell wall (more so in Gram-positive bacteria) is an essential polymer
called peptidoglycan. Beta-lactam antibiotics bind to PBPs or penicillin binding
proteins which are involved in the final stages of peptidoglycan synthesis. By
inhibiting PBP function, peptidoglycan cannot be properly synthesized and the cell
lyses.
Effects on humans – Human cells do not use nor synthesize peptidoglycan and are
therefore not susceptible to beta-lactam antibiotics. (other side effects are possible)