Abundant antibacterial compound libraries provide excellent chemical starting points for hit identification in antibacterial drug discovery. Creative Biolabs provides an antibacterial compound library including FDA-approved antibiotics, bacteriocins, and bacteriophage drugs.

FDA-Approved Antibiotics

FDA-approved products are more safety and effectiveness. These antibiotics have already confirmed by literature, patent reports, and clinical research, therefore saving a lot of time and expenditure for researchers. For instance, some FDA-approved drugs developed to treat non-infectious diseases have antimicrobial activities. The FDA-approved drugs mainly include barbiturates, beta-adrenergic receptor antagonists, diuretic drugs, proton pump inhibitors and antihistamines. They have different ways of inhibitions on microbial growth. Some have direct antimicrobial activity by altering cell permeability, affecting efflux pump of bacteria, cross-membrane ions transport or activity of membrane-bound enzymes. Some non-antibiotic drugs could increase the efficiency of an antibiotic as helper compounds, or change the pathogenicity of bacteria or activity on the physiology such as modulating macrophage activity.

Antimicrobial Peptides (AMPs)-Bacteriocins

Antimicrobial peptides (AMPs) are promising antibiotics for both Gram-positive and negative bacteria. AMPs have lower opportunity in inducing drug resistance comparing with conventional antibiotics. Creative Biolabs provides antimicrobial peptides database as a part of antibacterial compound libraries for antibacterial drug discovery.

Different effects of AMPs on bacterial and mammalian cell membrane Figure 1. Different effects of AMPs on bacterial and mammalian cell membrane.

Those AMPs produced by bacteria are categorized as bacteriocins. To get more nutrients and living space in the environment, bacteria produce bacteriocins to kill other competitive microbiotas to maintain their population and reduce competitors. Mechanisms of action of bacteriocins include peptide binding to the bacterial cell surface, conformational change and pore formation through the bacterial cell wall.

On the basis of their structure, bacteriocins can be classified into four classes:

  • Class I: (<5 kDa) heat-resistant peptides.
  • Class II: (<15 kDa) heat-stable, membrane active, unmodified peptides.
  • Class III: (>15 kDa) heat-labile proteins.
  • Class IV: complex bacteriocins with lipid or carbohydrate moieties bound to it.

Bacteriophage

Bacteriophage has been viewed as a potential antibacterial drug. With persistent evolutionary, bacteriophages have developed unique mechanisms that affect critical cellular processes on hosts. Different from conventional antibacterial therapy, bacteriophages, and their derived endolysins offer incomparable advantages, like high specificity and relative abundance in the environment. Using a high-throughput bacteriophage genomics strategy, Creative Biolabs can exploit inhibition of bacterial growth by identifying antimicrobial phage-encoded polypeptides.

Drug discovery basing bacteriophages genomics strategy Figure 2. Drug discovery basing bacteriophages genomics strategy.

The process of antibacterial drug discovery based on bacteriophages genomics strategy is shown below.

  • Firstly, characterization and sequencing of bacteriophage genome (e.g. Staphylococcus aureus).
  • Secondly, functional screening for antibacterial phage ORFs.
  • Thirdly, validation of the interaction between screened ORFs and bacterial targets.
  • Finally, high-throughput screen for inhibitors or mimicking the screened polypeptide by a chemical compound.

Creative Biolabs dedicates discovering innovative antibacterial drugs that using superior methodologies and technologies to address the antibacterial compound libraries. For more detailed information, please feel free to contact us or directly sent us an inquiry.

References

  1. Matsuzaki K. (2009). “Control of cell selectivity of antimicrobial peptides”. Biochimica et Biophysica Acta (BBA)-Biomembranes 1788(8):1687-1692.
  2. Nakonieczna A, Cooper C J and Gryko R. (2015). “Bacteriophages and bacteriophage-derived endolysins as potential therapeutics to combat Gram-positive spore forming bacteria”. Journal of Applied Microbiology 119: 620-631.
  3. Nigam A, Gupta D, Sharma A. (2014). “Treatment of infectious disease: Beyond antibiotics”. Microbiological Research 169 (2014): 643-651.

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