Name:
De Carvahlo and Abraham_final.pdf
Size:
351.5Kb
Format:
PDF
Description:
original manuscript
Average rating
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Star rating
Your vote was cast
Thank you for your feedback
Thank you for your feedback
Issue Date
2012-07-01
Metadata
Show full item recordAbstract
Diketopiperazines are the smallest cyclic peptides known. 90% of Gram-negative bacteria produce diketopiperazines and they have also been isolated from Gram-positive bacteria, fungi and higher organisms. Biosynthesis of cyclodipeptides can be achieved by dedicated nonribosomal peptide synthetases or by a novel type of synthetases named cyclopeptide synthases. Since the first report in 1924 a large number of bioactive diketopiperazines was discovered spanning activities as antitumor, antiviral, antifungal, antibacterial, antiprion, antihyperglycemic or glycosidase inhibitor agents. As infections are of increasing concern for human health and resistances against existing antibiotics are growing this review focuses on the antimicrobial activities of diketopiperazines. The antibiotic bicyclomycin is a diketopiperazine and structure activity studies revealed the unique nature of this compound which was finally developed for clinical applications. The antimicrobial activities of a number of other diketopiperazines along with structure activity relationships are discussed. Here a special focus is on the activity-toxicity problem of many compounds setting tight limitations to their application as drugs. Not only these classical antimicrobial activities but also proposed action in modulating bacterial communication as a new target to control biofilms will be evaluated. Pathogens organized in biofilms are difficult to eradicate because of the increase of their tolerance for antibiotics for several orders. Diketopiperazines were reported to modulate LuxR-mediated quorum-sensing systems of bacteria, and they are considered to influence cell-cell signaling offering alternative ways of biofilm control by interfering with microbial communication. Concluding the review we will finally discuss the potential of diketopiperazines in the clinic to erase biofilm infections.Citation
Antimicrobial and biofilm inhibiting diketopiperazines. 2012, 19 (21):3564-77 Curr. Med. Chem.Affiliation
Helmholtz Center for Infection Research, Chemical Microbiology, Inhoffenstrasse 7, 38124 Braunschweig, Germany. wolf-rainer.abraham@helmholtz-hzi.de.Journal
Current medicinal chemistryPubMed ID
22709011Type
ArticleLanguage
enISSN
1875-533XThe following license files are associated with this item:
Related articles
- Identification of antimicrobial compound, diketopiperazines, from a Bacillus sp. N strain associated with a rhabditid entomopathogenic nematode against major plant pathogenic fungi.
- Authors: Nishanth Kumar S, Mohandas C, Siji JV, Rajasekharan KN, Nambisan B
- Issue date: 2012 Oct
- Development and evaluation of cationic amphiphilic antimicrobial 2,5-diketopiperazines.
- Authors: Labrière C, Kondori N, Caous JS, Boomgaren M, Sandholm K, Ekdahl KN, Hansen JH, Svenson J
- Issue date: 2018 Jul
- Hybrid combinations containing natural products and antimicrobial drugs that interfere with bacterial and fungal biofilms.
- Authors: Zacchino SA, Butassi E, Cordisco E, Svetaz LA
- Issue date: 2017 Dec 15
- Targeting pathogenic fungi, bacteria and fungal-bacterial biofilms by newly synthesized quaternary ammonium derivative of pyridoxine and terbinafine with dual action profile.
- Authors: Garipov MR, Sabirova AE, Pavelyev RS, Shtyrlin NV, Lisovskaya SA, Bondar OV, Laikov AV, Romanova JG, Bogachev MI, Kayumov AR, Shtyrlin YG
- Issue date: 2020 Nov
- Antimicrobial peptide-inspired NH125 analogues: bacterial and fungal biofilm-eradicating agents and rapid killers of MRSA persisters.
- Authors: Basak A, Abouelhassan Y, Zuo R, Yousaf H, Ding Y, Huigens RW
- Issue date: 2017 Jul 5