Siderophore conjugates

Page, Malcolm G. P.

doi:10.1111/nyas.12024

Cited by 103 publications

(71 citation statements)

References 74 publications

(158 reference statements)

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“…Siderophore conjugates in the past have experienced a high rate of resistance development due to selection of mutations in TonB or other proteins associated with iron transport systems (130,131). At this time, it appears that BAL30072 has much lower rates of resistance selection than those described for previous siderophore conjugates, with most mutations observed in ␤-lactamase-related activities rather than in iron transport genes (126). Because of the lability of this molecule to occasional ␤-lactamases (128), it is possible that optimal therapeutic use of this monosulfactam will be in combination therapy.…”

Section: Novel ␤-Lactams and ␤-Lactamase Inhibitor Combinationsmentioning

confidence: 96%

“…The siderophore-substituted monosulfactam BAL30072 (Fig. 4, compound 1) from Basilea Pharmaceutica International is a monocyclic ␤-lactam that is in phase 1 clinical trials (126). BAL30072 exhibits in vitro activity against Enterobacteriaceae similar to that of other monocyclic ␤-lactams, including against strains that produce MBLs (127).…”

Section: Novel ␤-Lactams and ␤-Lactamase Inhibitor Combinationsmentioning

confidence: 99%

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Investigational Antimicrobial Agents of 2013

Pucci

Bush

2013

Clin Microbiol Rev

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SUMMARY New antimicrobial agents are always needed to counteract the resistant pathogens that continue to be selected by current therapeutic regimens. This review provides a survey of known antimicrobial agents that were currently in clinical development in the fall of 2012 and spring of 2013. Data were collected from published literature primarily from 2010 to 2012, meeting abstracts (2011 to 2012), government websites, and company websites when appropriate. Compared to what was reported in previous surveys, a surprising number of new agents are currently in company pipelines, particularly in phase 3 clinical development. Familiar antibacterial classes of the quinolones, tetracyclines, oxazolidinones, glycopeptides, and cephalosporins are represented by entities with enhanced antimicrobial or pharmacological properties. More importantly, compounds of novel chemical structures targeting bacterial pathways not previously exploited are under development. Some of the most promising compounds include novel β-lactamase inhibitor combinations that target many multidrug-resistant Gram-negative bacteria, a critical medical need. Although new antimicrobial agents will continue to be needed to address increasing antibiotic resistance, there are novel agents in development to tackle at least some of the more worrisome pathogens in the current nosocomial setting.

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Section: Novel ␤-Lactams and ␤-Lactamase Inhibitor Combinationsmentioning

confidence: 96%

Section: Novel ␤-Lactams and ␤-Lactamase Inhibitor Combinationsmentioning

confidence: 99%

Investigational Antimicrobial Agents of 2013

Pucci

Bush

2013

Clin Microbiol Rev

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“…infections showed promising results; nevertheless, it warrants further investigation. Moreover, a number of studies on complex siderophore-drug conjugates have been made to test their potential as effective antimicrobial agents [23,34,[61][62][63]. It could be speculated that these siderophore conjugates could be radiolabelled or derivatized and used for molecular imaging of infections.…”

Section: Siderophores For Molecular Imaging Of Infectionmentioning

confidence: 99%

Siderophores for molecular imaging applications

Petřík

Zhai

Haas

et al. 2016

Clin Transl Imaging

106

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This review covers publications on siderophores applied for molecular imaging applications, mainly for radionuclide-based imaging. Siderophores are low molecular weight chelators produced by bacteria and fungi to scavenge essential iron. Research on these molecules has a continuing history over the past 50 years. Many biomedical applications have been developed, most prominently the use of the siderophore desferrioxamine (DFO) to tackle iron overload related diseases. Recent research described the upregulation of siderophore production and transport systems during infection. Replacing iron in siderophores by radionuclides, the most prominent Ga-68 for PET, opens approaches for targeted imaging of infection; the proof of principle has been reported for fungal infections using 68 Ga-triacetylfusarinine C (TAFC). Additionally, fluorescent siderophores and therapeutic conjugates have been described and may be translated to optical imaging and theranostic applications. Siderophores have also been applied as bifunctional chelators, initially DFO as chelator for Ga-67 and more recently for Zr-89 where it has become the standard chelator in Immuno-PET. Improved DFO constructs and bifunctional chelators based on cyclic siderophores have recently been developed for Ga-68 and Zr-89 and show promising properties for radiopharmaceutical development in PET. A huge potential from basic biomedical research on siderophores still awaits to be utilized for clinical and translational imaging.

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“…Early studies on non-b-lactam siderophore conjugates for the most part resulted in compounds with lower activities than the parent antibiotic, often due to problems with solubility, receptor uptake, or possibly, lack of release of the antibiotic from its siderophore partner upon entry (as needed for proper function) (reviewed in Ref. 98). …”

mentioning

confidence: 99%

One ring to rule them all: Current trends in combating bacterial resistance to the β‐lactams

2016

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From humble beginnings of a contaminated petri dish, b-lactam antibiotics have distinguished themselves among some of the most powerful drugs in human history. The devastating effects of antibiotic resistance have nevertheless led to an "arms race" with disquieting prospects. The emergence of multidrug resistant bacteria threatens an ever-dwindling antibiotic arsenal, calling for new discovery, rediscovery, and innovation in b-lactam research. Here the current state of b-lactam antibiotics from a structural perspective was reviewed.

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Siderophore conjugates

Cited by 103 publications

References 74 publications

Investigational Antimicrobial Agents of 2013

Investigational Antimicrobial Agents of 2013

Siderophores for molecular imaging applications

One ring to rule them all: Current trends in combating bacterial resistance to the β‐lactams

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