An overview of novel antimicrobial carbonic anhydrase inhibitors

Article Biochemistry & Molecular Biology

Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity

Maristela Barbosa Portela et al.

Summary: Pre-treatment of dentine with sulphonamide carbonic anhydrase inhibitors (CAIs) maintains stable resin-dentine bond strength, improves dentine wettability, and exhibits antibacterial activity.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

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Review Biochemistry & Molecular Biology

Selected strategies to fight pathogenic bacteria

Aiva Plotniece et al.

Summary: Natural products and analogues are valuable sources for the discovery of antibacterial drugs. The identification of bacterial metalloenzymes and the synthesis of selective inhibitors are interesting for the development of antibacterial agents due to increasing drug resistance. Peptide nucleic acids represent a novel strategy for targeting pathogens through antisense inhibition and development of antisense peptide nucleic acids. The review also discusses alternative therapeutic options and optimized in vitro and in vivo models for studying biofilm-related infections along with an overview of drug delivery nanosystems.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

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Article Biochemistry & Molecular Biology

Inhibition studies with simple and complex (in)organic anions of the γ-carbonic anhydrase from Mammaliicoccus (Staphylococcus) sciuri, MscCAγ

Simone Giovannuzzi et al.

Summary: The gamma-carbonic anhydrase (CA, EC 4.2.1.1) from Mammaliicoccus (Staphylococcus) sciuri (MscCA gamma) was studied for its inhibition by various (in)organic anions. Peroxydisulfate and trithiocarbonate were the most effective inhibitors, while other anions showed weaker inhibitory effects. Finding more effective MscCA gamma inhibitors could help combat antibiotic resistance.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

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Review Infectious Diseases

Incidence of infection with multidrug-resistant Gram-negative bacteria and vancomycin-resistant enterococci in carriers: a systematic review and meta-regression analysis

Roel P. J. Willems et al.

Summary: This study aims to quantify the effect of gut colonisation on the subsequent risk of infection with multidrug-resistant bacteria. The results showed a substantial risk of infection, particularly in patients colonised with carbapenem-resistant Gram-negative bacteria. These data can guide prophylactic and treatment decisions and serve as a valuable resource for planning clinical trials on targeted prevention.

LANCET INFECTIOUS DISEASES (2023)

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Article Chemistry, Medicinal

Structural Characterization of Thiadiazolesulfonamide Inhibitors Bound to Neisseria gonorrhoeae a-Carbonic Anhydrase

Anil Kumar Marapaka et al.

Summary: Drug-resistant Neisseria gonorrhoeae poses a serious threat to public health. The research team solved the structure of carbonic anhydrase inhibitors bound to the essential alpha-carbonic anhydrase isoform from N. gonorrhoeae, revealing differences compared to the human enzyme.

ACS MEDICINAL CHEMISTRY LETTERS (2023)

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Review Environmental Sciences

Evidence of Antimicrobial Resistance in Bats and Its Planetary Health Impact for Surveillance of Zoonotic Spillover Events: A Scoping Review

Popy Devnath et al.

Summary: Due to the COVID-19 pandemic and other outbreaks like SARS and Ebola, bats are recognized as vital for transmitting zoonotic infectious diseases. However, knowledge of antimicrobial resistance (AMR) between bats and humans is limited. This paper reviews the evidence of AMR in bats and discusses the planetary health aspect of AMR to understand its association with the emergence and spread of AMR at the human-animal interface. The presence of clinically significant resistant bacteria in bats has implications for disease surveillance, transmission, and treatment.

INTERNATIONAL JOURNAL OF ENVIRONMENTAL RESEARCH AND PUBLIC HEALTH (2023)

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Article

How Antimicrobial Resistance Is Linked to Climate Change: An Overview of Two Intertwined Global Challenges

Roberta Magnano San Lio et al.

International Journal of Environmental Research and Public Health (2023)

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Article Microbiology

CanB is a metabolic mediator of antibiotic resistance in Neisseria gonorrhoeae

Daniel H. F. Rubin et al.

Summary: The evolution of Neisseria gonorrhoeae as a human pathogen is influenced by diverse host environments and antibiotics. Variations in antibiotic resistance across N. gonorrhoeae lineages indicate that metabolic differences may affect the acquisition of specific resistances. A study found that the requirement for supplemental CO2 in some isolates is due to a single substitution in a beta-carbonic anhydrase, CanB. This metabolic variation also influences fluoroquinolone resistance in N. gonorrhoeae by increasing the likelihood of acquisition.

NATURE MICROBIOLOGY (2023)

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Review Infectious Diseases

Carbonic Anhydrase Inhibitors as Novel Antibacterials in the Era of Antibiotic Resistance: Where Are We Now?

Alessio Nocentini et al.

Summary: Resistance to antibiotic treatment occurs when microorganisms resist clinically approved antibiotics. Medication repurposing/repositioning is a strategy that can help find new antibiotics. Among them, Zn2+ ion binders, such as sulfonamides and their bioisosteres, are considered promising compounds for obtaining novel antibacterials.

ANTIBIOTICS-BASEL (2023)

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Article Immunology

Global Epidemiology and Mechanisms of Resistance of Acinetobacter baumannii-calcoaceticus Complex

Mariana Castanheira et al.

Summary: The Acinetobacter baumannii-calcoaceticus complex (ABC) is a significant group of organisms causing human infections worldwide, with a small number of clones responsible for increased infections and resistance to antimicrobial agents. This article discusses the current epidemiology and resistance mechanisms in ABC. A. baumannii-calcoaceticus is the most common species in the Acinetobacter genus and is responsible for a large percentage of nosocomial infections, including bacteremia, pneumonia, and skin and urinary tract infections. Key clones of A. baumannii-calcoaceticus play a major role in the global dissemination of these organisms, and multidrug resistance is a common trait among these clones due to their remarkable adaptability. A. baumannii-calcoaceticus isolates can develop resistance through various mechanisms, such as horizontal gene transfer, natural transformation, acquisition of mutations, and mobilization of genetic elements.

CLINICAL INFECTIOUS DISEASES (2023)

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Article Biochemistry & Molecular Biology

Antimicrobial and Antibiofilm Activities of Carvacrol, Amoxicillin and Salicylhydroxamic Acid Alone and in Combination vs. Helicobacter pylori: Towards a New Multi-Targeted Therapy

Valentina Puca et al.

Summary: The World Health Organization has identified Helicobacter pylori as a high-priority pathogen requiring updated antibacterial treatments. This study investigated the potential of combining a CA inhibitor, carvacrol (CAR), amoxicillin (AMX), and a urease inhibitor (SHA) to develop a multiple-targeted anti-H. pylori therapy. The combinations of these compounds showed strong inhibition of H. pylori growth and biofilm formation, with CAR-AMX and CAR-SHA combinations demonstrating additive effects and AMX-SHA combination showing indifferent effects.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

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Article Biochemistry & Molecular Biology

Photoactivatable Heptamethine-Based Carbonic Anhydrase Inhibitors Leading to New Anti-Antibacterial Agents

Simone Carradori et al.

Summary: In this study, new heptamethine-based compounds decorated with a sulfonamide moiety were synthesized for selectively inhibiting bacterial carbonic anhydrases (CAs) and being photoactivated by specific wavelengths. The compounds showed potent CA inhibition and a slight preference for bacterial isoforms. They also exhibited promising effects against S. epidermidis under irradiation, while being non-cytotoxic to human red blood cells.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

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Article Infectious Diseases

High-level in vitro resistance to gentamicin acquired in a stepwise manner in Neisseria gonorrhoeae

Daniel Golparian et al.

Summary: This study describes the first high-level gentamicin-resistant Neisseria gonorrhoeae isolate (MIC = 128 mg/L) selected in vitro through experimental evolution. The most significant increases in gentamicin MICs were caused by mutations in fusA (G1560A and G1904T encoding EF-G M520I and R635L, respectively) and ubiM (D186N). The high-level gentamicin-resistant N. gonorrhoeae mutant showed impaired biofitness.

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY (2023)

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Article Biochemistry & Molecular Biology

Benzenesulfonamide derivatives as Vibrio cholerae carbonic anhydrases inhibitors: a computational-aided insight in the structural rigidity-activity relationships

Marialuigia Fantacuzzi et al.

Summary: Vibrio cholerae, a pathogen responsible for life-threatening infections in low-income countries, has developed resistance to antibacterial drugs. Researchers have identified carbonic anhydrases (CAs) encoded by V. cholerae as potential pharmacological targets. They have developed a large library of CAs inhibitors with different flexibility degrees and found compounds with strong inhibition against Vch alpha CA. Computational studies have provided insights into the inhibitory activity and isoform selectivity of these compounds.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

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Article Multidisciplinary Sciences

Coordination of bacterial cell wall and outer membrane biosynthesis

Katherine R. Hummels et al.

Summary: Gram-negative bacteria have a complex envelope that is a major factor in their inherent antibiotic resistance and drug entry. The coordination of the biogenesis of essential surface layers, such as peptidoglycan (PG) and outer membrane (OM), is still poorly understood. In this study, a regulatory interaction between the committed enzymes for PG and lipopolysaccharide (LPS) synthesis pathways in Pseudomonas aeruginosa was discovered.

NATURE (2023)

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Article Multidisciplinary Sciences

Host-specific plasmid evolution explains the variable spread of clinical antibiotic-resistance plasmids

Fabienne Benz et al.

Summary: Antibiotic resistance on plasmids is a pressing global health problem. The stability of plasmids varies among clinical plasmids and bacteria, and this variability can rapidly change the likelihood of different bacterium-plasmid combinations spreading.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2023)

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Review Microbiology

Vancomycin-resistant Enterococcus faecium and the emergence of new sequence types associated with hospital infection

Ronan F. O'Toole et al.

Summary: Enterococcus faecium has become a dominant species in vancomycin-resistant enterococci (VRE) infections in healthcare settings. Variants such as vanB ST796 and vanA ST1421 have emerged, originally from Australia, and caused VRE outbreaks in other countries. The detection of vancomycin variable enterococci (VVE) belonging to ST1421 in Europe, which exhibit a vancomycin-susceptible phenotype but can revert to resistance, is of concern. This study also explores the use of genome sequencing to understand the evolution and spread of VRE.

RESEARCH IN MICROBIOLOGY (2023)

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Article Biochemistry & Molecular Biology

Mechanistic and structural insights into the bifunctional enzyme PaaY from Acinetobacter baumannii

Min Jiao et al.

Summary: PaaY is a bifunctional enzyme in Acinetobacter baumannii that acts as a thioesterase and a γ-carbonic anhydrase. The crystal structure of AbPaaY reveals a homotrimer with a unique domain-swapped C-termini, which affects its stability and substrate specificity. Knockout of AbPaaY impairs the growth, biofilm formation, and hydrogen peroxide resistance of Acinetobacter.

STRUCTURE (2023)

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Article Chemistry, Medicinal

Evaluation of 1,3,4-Thiadiazole Carbonic Anhydrase Inhibitors for Gut Decolonization of Enterococci

Nader S. Abutaleb et al.

Summary: Vancomycin-resistant enterococci (VRE) are drug-resistant pathogens that require new therapeutic approaches. Decolonization of VRE from carriers can reduce the risk of infections in healthcare settings. This study found that carbonic anhydrase inhibitors showed better efficacy in VRE gut decolonization compared to linezolid.

ACS MEDICINAL CHEMISTRY LETTERS (2023)

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Article Microbiology

Carbonic Anhydrase Inhibition as a Target for Antibiotic Synergy in Enterococci

Gayatri Shankar Chilambi et al.

Summary: This study identified a mutant strain of Enterococcus faecalis that is hypersusceptible to aminoglycoside antibiotics due to disruption of alpha-carbonic anhydrase (alpha-CA). Disruption of alpha-CA increased proton motive force and membrane permeability, leading to increased gentamicin uptake in E. faecalis. Additionally, an FDA-approved alpha-CA inhibitor sensitized various E. faecalis strains to gentamicin.

MICROBIOLOGY SPECTRUM (2023)

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Review Infectious Diseases

Newer, Older, and Alternative Agents for the Eradication of Helicobacter pylori Infection: A Narrative Review

Gyorgy Miklos Buzas et al.

Summary: Despite being discovered four decades ago, Helicobacter pylori infection still presents challenges in terms of diagnosis and treatment. Current management is based on guidelines, but implementing them in practice is a lengthy process. Antibiotic resistance and poor patient compliance hamper successful eradication, highlighting the need for improved strategies.

ANTIBIOTICS-BASEL (2023)

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Article Chemistry, Medicinal

A simple yet multifaceted 90 years old, evergreen enzyme: Carbonic anhydrase, its inhibition and activation

Claudiu T. Supuran

Summary: This article presents advances in carbonic anhydrase (CA, EC 4.2.1.1) research over the past three decades, focusing on the understanding of the activation mechanism, the development of isoform-selective inhibitors/activators using the tail approach, and their applications in obesity management, hypoxic tumors, neurological conditions, and as anti-infectives.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2023)

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Article Biochemistry & Molecular Biology

Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of Neisseria gonorrhoeae

Nader S. Abutaleb et al.

Summary: Ethoxzolamide exhibits potent anti-gonococcal activity and warrants further investigation as an effective agent against Neisseria gonorrhoeae.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Dithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae

Simone Giovannuzzi et al.

Summary: In this study, a class of compounds called dithiocarbamates (DTCs) was found to efficiently inhibit the carbonic anhydrase enzyme in Neisseria gonorrhoeae, with better inhibition than other inorganic anions and sulphonamides. Three of these compounds showed low minimum inhibitory concentration values in antimicrobial testing, suggesting their potential as novel antigonococcal drugs.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Coumarins effectively inhibit bacterial α-carbonic anhydrases

Simone Giovannuzzi et al.

Summary: Coumarins were shown to inhibit bacterial alpha-carbonic anhydrases from Neisseria gonorrhoeae and Vibrio cholerae, with the nature and position of substituents in the coumarin ring strongly influencing the inhibitory efficacy. In comparison, human CA isoforms hCA I and II were less prone to inhibition by these compounds, indicating potential for coumarin bacterial CA inhibitors with selectivity for bacterial over human isoforms.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Inhibition studies of bacterial α-carbonic anhydrases with phenols

Simone Giovannuzzi et al.

Summary: The inhibition of alpha-class carbonic anhydrases (CAs) from bacterial pathogens by phenols and phenolic acids was investigated. Small changes in the phenol scaffold led to drastic effects on the inhibitory activity of bacterial CA. This underinvestigated class of bacterial CA inhibitors may have potential in fighting drug resistant bacteria.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Article Immunology

In vivo efficacy of acetazolamide in a mouse model of Neisseria gonorrhoeae infection

Nader S. Abutaleb et al.

Summary: Acetazolamide shows potent anti-gonococcal activity in vitro and significant efficacy in reducing gonococcal burden in a mouse model, suggesting its potential as a novel treatment option for gonorrhea.

MICROBIAL PATHOGENESIS (2022)

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Article Biochemistry & Molecular Biology

May Sulfonamide Inhibitors of Carbonic Anhydrases from Mammaliicoccus sciuri Prevent Antimicrobial Resistance Due to Gene Transfer to Other Harmful Staphylococci?

Viviana De Luca et al.

Summary: Blocking bacterial carbonic anhydrases can reduce pathogen survival and fitness. The recombinant M. sciuri gamma-CA showed significant hydratase activity, with a sulfonamide inhibitory profile different from that of MscCA beta, suggesting the possibility of developing novel CA class-specific inhibitors.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

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Article Biochemistry & Molecular Biology

Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases

Weiwei An et al.

Summary: This paper discusses the inhibition mechanism and effects of the inhibitor acetazolamide (AZM) and its analogs against vancomycin-resistant enterococci (VRE), as well as the research methods related to binding to different enzymes and selectivity.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth

Viviana De Luca et al.

Summary: Carbonic anhydrases play a crucial role in maintaining metabolic functions in organisms, with inhibitors like acetazolamide able to impair bacterial growth and metabolism.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Review Infectious Diseases

Enterococcus Virulence and Resistant Traits Associated with Its Permanence in the Hospital Environment

Catarina Geraldes et al.

Summary: Enterococcus are opportunistic pathogens of increasing importance in clinical settings, particularly in terms of hospital-acquired infections. These bacteria exhibit intrinsic and extrinsic resistance to various classes of antibiotics, with a particular emphasis on vancomycin-resistant enterococci. In addition to resistance, enterococci possess other characteristics such as the ability to form biofilms and exchange genetic information, enhancing their survival in harsh environments. These traits, along with reports of decreased susceptibility to biocides, contribute to the persistent presence of enterococci in hospitals and their role in causing difficult-to-treat infections.

ANTIBIOTICS-BASEL (2022)

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Article Infectious Diseases

Antimicrobial-resistant gonorrhoea: the national public health response, England, 2013 to 2020

Rachel Merrick et al.

Summary: Neisseria gonorrhoeae has developed resistance to all antimicrobials used to treat gonorrhoea, and the emergence of ceftriaxone-resistant strains threatens the last-line option for empirical treatment. Measures have been taken to delay the spread of antimicrobial resistance (AMR) in N. gonorrhoeae in England, but the number of gonorrhoea diagnoses has been continuously increasing. The decreased susceptibility of N. gonorrhoeae isolates to azithromycin and the detection of ceftriaxone-resistant strains have led to changes in the treatment approach in the United Kingdom.

EUROSURVEILLANCE (2022)

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Article Biochemistry & Molecular Biology

Activation studies with amino acids and amines of a β-carbonic anhydrase from Mammaliicoccus (Staphylococcus) sciuri previously annotated as Staphylococcus aureus (SauBCA) carbonic anhydrase

Andrea Angeli et al.

Summary: A previously annotated enzyme in the genome of Staphylococcus aureus was found to actually belong to another pathogenic bacterium, Mammaliicoccus (Staphylococcus) sciuri. Through experimentation, the enzyme MscCA was shown to be activated by certain amino acids and amines. This finding is significant for understanding bacterial virulence and colonization of hosts.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Effect of Sulfonamides and Their Structurally Related Derivatives on the Activity of ι-Carbonic Anhydrase from Burkholderia territorii

Viviana De Luca et al.

Summary: Carbonic anhydrases are crucial enzymes in nature, with recent advancements showing their potential as targets for antimicrobial drugs against bacterial resistance. In this study, the inhibitor profile of a newly discovered iota-CA class in bacteria, including Burkholderia territorii, was extensively explored, revealing compounds that selectively inhibit bacterial CA isoforms, contributing to the development of novel antimicrobials.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

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Article Chemistry, Medicinal

Bacterial carbonic anhydrases: underexploited antibacterial therapeutic targets

Daniel P. Flaherty et al.

FUTURE MEDICINAL CHEMISTRY (2021)

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Article Biochemistry & Molecular Biology

Selective Inhibition of Helicobacter pylori Carbonic Anhydrases by Carvacrol and Thymol Could Impair Biofilm Production and the Release of Outer Membrane Vesicles

Rossella Grande et al.

Summary: The study assessed the anti-H. pylori activity of thymol and carvacrol in terms of CA inhibition, isoform selectivity, growth impairment, biofilm production, and release of associated outer membrane vesicles-eDNA. Carvacrol and thymol could be considered as new lead compounds as alternative H. pylori CA inhibitors or used in association with current drugs to manage H. pylori infection and limit the spread of antibiotic resistance.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

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Article Microbiology

In Vivo Antibacterial Activity of Acetazolamide

Nader S. Abutaleb et al.

Summary: Acetazolamide showed promising inhibitory effects against enterococci and outperformed linezolid in VRE mouse models, suggesting it as a potential treatment option for VRE infections.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2021)

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Article Cell Biology

Microbiota, Bacterial Carbonic Anhydrases, and Modulators of Their Activity: Links to Human Diseases?

Amedeo Amedei et al.

MEDIATORS OF INFLAMMATION (2021)

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Review Biotechnology & Applied Microbiology

Natural products in drug discovery: advances and opportunities

Atanas G. Atanasov et al.

Summary: Natural products and their analogues have historically played a significant role in pharmacotherapy, however, they also present challenges. Recent technological and scientific developments are addressing these challenges and revitalizing interest in natural products as drug leads, particularly for combating antimicrobial resistance.

NATURE REVIEWS DRUG DISCOVERY (2021)

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Article Biology

Characterization of a novel type of carbonic anhydrase that acts without metal cofactors

Yoshihisa Hirakawa et al.

Summary: COG4337 proteins are a novel metal-independent variant of iota-class carbonic anhydrases, which accelerate CO2 hydration and are localized in organelles for CO2 metabolism. They share structural features with iota-class CAs but exhibit activity without reliance on metals.

BMC BIOLOGY (2021)

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Review Microbiology

Carbonic Anhydrases: New Perspectives on Protein Functional Role and Inhibition in Helicobacter pylori

Cristina Campestre et al.

Summary: Bacterial carbonic anhydrases play crucial roles in various physiological processes, including modulation of CO2 concentration, pH homeostasis, and regulation of bacterial growth and virulence. Recent studies have highlighted the importance of carbonic anhydrases in bacterial pathogens associated with human infections, suggesting their potential as targets for novel anti-ulcer therapies in the era of antibiotic resistance.

FRONTIERS IN MICROBIOLOGY (2021)

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Article Chemistry, Medicinal

Structure-Activity Relationship Studies of Acetazolamide-Based Carbonic Anhydrase Inhibitors with Activity against Neisseria gonorrhoeae

Chad S. Hewitt et al.

Summary: Gonorrhea infection poses an urgent threat to public health. Through repurposing an FDA-approved compound, researchers have developed two new molecules with significantly improved antigonococcal activity compared to traditional drugs.

ACS INFECTIOUS DISEASES (2021)

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Review Pharmacology & Pharmacy

Epidemiology, Treatments, and Vaccine Development for Antimicrobial-Resistant Neisseria gonorrhoeae: Current Strategies and Future Directions

Eric Y. Lin et al.

Summary: Neisseria gonorrhoeae is the second most common bacterial sexually transmitted infection globally, with resistance to all currently approved antibiotics. Novel strategies are needed to improve diagnosis and treatment of antimicrobial-resistant N. gonorrhoeae to combat its spread globally.

DRUGS (2021)

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Review Public, Environmental & Occupational Health

Global status of tetracycline resistance among clinical isolates of Vibrio cholerae: a systematic review and meta-analysis

Mohammad Hossein Ahmadi

Summary: The study found a high and prevalent resistance rate to tetracyclines among V. cholerae isolates globally. It emphasized the importance of conducting standard antimicrobial susceptibility testing before treatment choice, and monitoring and managing antibiotic resistance patterns of V. cholerae strains to reduce the emergence and spread of antibiotic resistant strains as well as treatment failure.

ANTIMICROBIAL RESISTANCE AND INFECTION CONTROL (2021)

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Article Infectious Diseases

Replacement of Enterococcus faecalis by Enterococcus faecium as the predominant enterococcus in UK bacteraemias

Carolyne Horner et al.

Summary: The review of two UK bacteraemia surveillance systems revealed a rising proportion of E. faecium in enterococcal bloodstream infections and stable resistance trends, particularly E. faecium's resistance to antibiotics. This highlights the importance of monitoring and addressing the increasing prevalence of multiresistant E. faecium strains in clinical settings.

JAC-ANTIMICROBIAL RESISTANCE (2021)

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Review Biochemistry & Molecular Biology

An overview on the recently discovered iota-carbonic anhydrases

Alessio Nocentini et al.

Summary: Carbonic anhydrases (CAs) are a versatile enzyme superfamily involved in multiple physiological processes, and recent discoveries have revealed a new type of iota-CAs with unique catalytic activity without the need for metal ions.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2021)

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Review Medicine, Research & Experimental

Emerging role of carbonic anhydrase inhibitors

Claudiu T. Supuran

Summary: Inhibition of carbonic anhydrase has been used clinically for various applications including treating glaucoma, epilepsy, obesity, and cancer. Recent studies have discovered new roles of CA isoforms in areas like pain management, Alzheimer's disease, and oxidative stress, leading to potential novel clinical applications. Additionally, inhibition of CA in pathogenic microorganisms is being explored for new anti-infective drugs.

CLINICAL SCIENCE (2021)

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Article Biochemistry & Molecular Biology

Anion inhibition studies of the α-carbonic anhydrases from Neisseria gonorrhoeae

Alessio Nocentini et al.

Summary: The study investigated the inhibition of Neisseria gonorrhoeae's alpha-class carbonic anhydrase NgCA by various inorganic and organic anions. The most effective inhibitors were found to be sulfamide, sulfamate, trithiocarbonate, and N,N-diethyldithiocarbamate, showcasing the potential for developing novel antibacterial drugs.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2021)

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Review Biochemistry & Molecular Biology

Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase

Alessio Nocentini et al.

Summary: This review discusses the inhibition of carbonic anhydrase by inorganic anions, including various inhibitor classes and mechanisms. It also highlights the development of highly selective CAIs through rigorous X-ray crystallography experiments.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2021)

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Article Immunology

Antibiotic resistance in Vibrio cholerae: Understanding the ecology of resistance genes and mechanisms

Bhabatosh Das et al.

VACCINE (2020)

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Article Oncology

A Phase 1 Study of SLC-0111, a Novel Inhibitor of Carbonic Anhydrase IX, in Patients With Advanced Solid Tumors

Paul C. McDonald et al.

AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS (2020)

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Article Gastroenterology & Hepatology

Antibacterial activity of ethoxzolamide against Helicobacter pylori strains SS1 and 26695

Mohammad M. Rahman et al.

GUT PATHOGENS (2020)

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Article Biochemistry & Molecular Biology

Crystal Structure of a Tetrameric Type II β-Carbonic Anhydrase from the Pathogenic Bacterium Burkholderia pseudomallei

Andrea Angeli et al.

MOLECULES (2020)

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Article Biochemistry & Molecular Biology

The Effect of Substituted Benzene-Sulfonamides and Clinically Licensed Drugs on the Catalytic Activity of CynT2, a Carbonic Anhydrase Crucial for Escherichia coli Life Cycle

Sonia Del Prete et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

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Article Chemistry, Medicinal

Optimization of Acetazolamide-Based Scaffold as Potent Inhibitors of Vancomycin-Resistant Enterococcus

Jatinder Kaur et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Article Biochemistry & Molecular Biology

Anion Inhibition Studies of the Beta-Carbonic Anhydrase from Escherichia coli

Sonia Del Prete et al.

MOLECULES (2020)

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Letter Medicine, General & Internal

Highly Resistant Cholera Outbreak Strain in Zimbabwe

Tapfumanei Mashe et al.

NEW ENGLAND JOURNAL OF MEDICINE (2020)

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Review Chemistry, Medicinal

Antibacterial carbonic anhydrase inhibitors: an update on the recent literature

Claudiu T. Supuran et al.

EXPERT OPINION ON THERAPEUTIC PATENTS (2020)

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Article Chemistry, Medicinal

Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium Vibrio cholerae

Alessandro Bonardi et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

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Article Biochemistry & Molecular Biology

Sulphonamide inhibition profile of Staphylococcus aureus β-carbonic anhydrase

Linda J. Urbanski et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2020)

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Article Biochemistry & Molecular Biology

Escherichia coli gamma-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors

Sonia Del Prete et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2020)

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News Item Biotechnology & Applied Microbiology

The small-molecule antibiotics pipeline: 2014-2018

Cara Lepore et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

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Review Biochemistry & Molecular Biology

Mycobacterium tuberculosis β-Carbonic Anhydrases: Novel Targets for Developing Antituberculosis Drugs

Ashok Aspatwar et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2019)

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Article Biochemistry & Molecular Biology

Extending the γ-class carbonic anhydrases inhibition profiles with phenolic compounds

Alessio Nocentini et al.

BIOORGANIC CHEMISTRY (2019)

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Article Cell Biology

Pseudomonas aeruginosa β-carbonic anhydrase, psCA1, is required for calcium deposition and contributes to virulence

Shalaka R. Lotlikar et al.

CELL CALCIUM (2019)

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Article Biochemistry & Molecular Biology

Identification and characterization of the α-CA in the outer membrane vesicles produced by Helicobacter pylori

Maurizio Ronci et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2019)

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Review Biochemistry & Molecular Biology

Activation of α-, β-, γ- δ-, ζ- and η- class of carbonic anhydrases with amines and amino acids: a review

Suleyman Akocak et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2019)

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Article Biochemistry & Molecular Biology

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