Boron Containing Compounds as Protease Inhibitors

Smoum, Reem; Rubinstein, Abraham; Dembitsky, Valery M.; Srebnik, Morris

doi:10.1021/cr608202m

Cited by 396 publications

(296 citation statements)

References 833 publications

(728 reference statements)

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“…Boronic acids were already recognized as effective inhibitors of serine proteases in the 1970s 179. Indeed, the boron atom can act as an electrophile, mimicking a carbonyl carbon atom, which can lead to the formation of a reversible covalent bond between the serine and the boronate moiety.…”

Section: β‐Lactamase Inhibitorsmentioning

confidence: 99%

Targeting Antibiotic Resistance

2016

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Finding strategies against the development of antibiotic resistance is a major global challenge for the life sciences community and for public health. The past decades have seen a dramatic worldwide increase in human‐pathogenic bacteria that are resistant to one or multiple antibiotics. More and more infections caused by resistant microorganisms fail to respond to conventional treatment, and in some cases, even last‐resort antibiotics have lost their power. In addition, industry pipelines for the development of novel antibiotics have run dry over the past decades. A recent world health day by the World Health Organization titled “Combat drug resistance: no action today means no cure tomorrow” triggered an increase in research activity, and several promising strategies have been developed to restore treatment options against infections by resistant bacterial pathogens.

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Section: β‐Lactamase Inhibitorsmentioning

confidence: 99%

Targeting Antibiotic Resistance

2016

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“…28,29 Since their initial discovery in the late 1970s, the boronates have proven to be effective SBL inhibitors in vitro. The development of SBL inhibitory boronates has largely focused on molecular mimicry with clinically approved blactams to confer affinity and specificity.…”

Section: Boronic Acid Sbl Inhibitorsmentioning

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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“…Many studies reveal that Curcumin, [48] (−)-epigallocatechin-3-gallate, a major constituent of green tea [49], decursin [50], capsaicin [51] and the potent PSA inhibitor boron [52] fall in this category.…”

Section: Psa Lowering Substancesmentioning

confidence: 99%

Role of Prostate Specific Antigen (PSA) in Pathogenesis of Prostate Cancer

Altuwaijri¹

2012

JCT

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Prostate cancer (PCa) is most common diagnosed cancer in men and it is second most common cause of male cancer death. Many factors have been implicated in the pathogenesis of PCa. Although many papers have discussed the prostate specific antigen (PSA) as biomarker of PCa, very few have addressed its rule in the carcinogenesis, metastasis and invasion of PCa. In this article we will review the pathological role of PSA, as a potential target in the therapeutics of PCa.

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Boron Containing Compounds as Protease Inhibitors

Cited by 396 publications

References 833 publications

Targeting Antibiotic Resistance

Targeting Antibiotic Resistance

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

Role of Prostate Specific Antigen (PSA) in Pathogenesis of Prostate Cancer

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