4.7 Editorial Material

Progress of Section Biochemistry in 2022

Related references

Note: Only part of the references are listed.
Article Biochemistry & Molecular Biology

Targeting Lysosomes in Colorectal Cancer: Exploring the Anticancer Activity of a New Benzo[a]phenoxazine Derivative

Joao C. C. Ferreira et al.

Summary: Colorectal cancer (CRC) is a highly prevalent and fatal cancer type, with limited therapy options. In recent years, phenoxazines derivatives, specifically BaP1, have shown promising anticancer activity against CRC cells. BaP1 selectively reduces cell proliferation, survival, and migration, inducing reactive oxygen species (ROS) generation, lysosomal membrane permeabilization, cytosolic acidification, and apoptotic cell death. In vivo experiments using a chicken embryo choriollantoic membrane (CAM) assay confirmed BaP1's ability to inhibit tumor growth, angiogenesis, and proliferation. BaP1 emerges as a potential lysosomal-targeted agent for CRC therapy.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

A Novel Antimicrobial Peptide Sp-LECin with Broad-Spectrum Antimicrobial Activity and Anti-Pseudomonas aeruginosa Infection in Zebrafish

Yan-Chao Chen et al.

Summary: A chemically synthesized truncated peptide, Sp-LECin, derived from a C-type lectin homolog of Scylla paramamosain, exhibits broad-spectrum antimicrobial activity by disrupting microbial membrane integrity and inducing reactive oxygen species production. It also shows potent anti-biofilm activity against Pseudomonas aeruginosa and improves the survival of infected zebrafish. Sp-LECin has the potential to be a promising antibacterial agent against devastating global pathogen infections.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

Application of Antimicrobial Photodynamic Therapy for Inactivation of Acinetobacter baumannii Biofilms

Irina Buchovec et al.

Summary: This study investigated the effect of riboflavin- and chlorophyllin-based antimicrobial photodynamic therapy on A. baumannii biofilms. The results showed that the antibacterial effect of riboflavin-based therapy depends on the generation of intracellular reactive oxygen species. Additionally, chlorophyllin-based therapy demonstrated a clear inactivation efficiency on A. baumannii biofilms. These findings suggest the potential of both therapies as antibacterial treatments or preventive measures against biofilm formation.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

Role Played by Paraoxonase-2 Enzyme in Cell Viability, Proliferation and Sensitivity to Chemotherapy of Oral Squamous Cell Carcinoma Cell Lines

Roberto Campagna et al.

Summary: Oral squamous cell carcinoma is the most aggressive and frequent form of head and neck cancer. Paraoxonase-2 enzyme has been identified as a potential molecular target for effective oral cancer treatment. Silencing paraoxonase-2 gene led to a reduction in cell proliferation and viability, enhanced sensitivity to cisplatin, and activation of the apoptosis pathway. These findings suggest that paraoxonase-2 could be a promising target for molecular treatment of oral cancer.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Review Biochemistry & Molecular Biology

Overview of Cancer Metabolism and Signaling Transduction

Hee-Suk Chae et al.

Summary: Despite progress in cancer treatment, conquering the disease remains a challenge. Cancer cells reprogram their metabolism to fuel their growth and survival, even in nutrient-poor environments. Metabolic alterations, such as increased glucose uptake and glycolysis, contribute to the unique features of cancer metabolism. High glutamine dependency and oncogenic signaling pathways also play important roles. Identifying convergent metabolic phenotypes is crucial for targeting cancer cells, and recent developments in anti-cancer therapy aim to exploit these metabolic vulnerabilities.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

Ligand-Based Drug Design of Novel Antimicrobials against Staphylococcus aureus by Targeting Bacterial Transcription

Jiqing Ye et al.

Summary: Staphylococcus aureus is a common pathogen that causes infectious diseases, including drug-resistant strains. The study developed a ligand-based workflow to identify potential antimicrobials against S. aureus by targeting bacterial transcription. Four compounds were identified as potential antimicrobials, with strong binding affinity to NusB.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

Synthesis, Biological and In Silico Studies of Griseofulvin and Usnic Acid Sulfonamide Derivatives as Fungal, Bacterial and Human Carbonic Anhydrase Inhibitors

Andrea Angeli et al.

Summary: Carbonic anhydrases play a crucial role in the CO2 hydration reaction in all living organisms and have potential as antiinfective targets. Griseofulvin and usnic acid sulfonamides were synthesized and evaluated as potential CA inhibitors. These compounds showed interesting inhibitory activity against various isoforms of CA, as well as a fungal enzyme. Computational studies were performed to understand the binding mode of these compounds in the active site of human CAs.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

High-Affinity Antibodies Designing of SARS-CoV-2 Based on Molecular Dynamics Simulations

Zihui Tian et al.

Summary: SARS-CoV-2 has caused a global pandemic of new crown pneumonia, significantly impacting human society. Antibody drug therapy, using the antibody S309 from SARS-CoV patients as a target, has proven effective against SARS-CoV-2. Through molecular dynamics simulations, the influence of glycosylation on the RBD's surface steric effects was studied, revealing that glycans play a role in bringing the RBD and antibody closer. By mutating key residues at the interaction interface, including G103A, P28W, and Y100W, the binding affinity of the antibody mutants was found to be stronger than that of the wild-type, particularly the G103A mutant.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

Ribosomal Stress Couples with the Hypoxia Response in Dec1-Dependent Orthodontic Tooth Movement

Shigeru Nakamura et al.

Summary: This study investigated the impact of a deficiency of the Dec1 gene on orthodontic tooth movement (OTM) and explored the role of ribosomal proteins in the hypoxic environment during OTM. Results showed that HIF-1 alpha transgenic mice had higher expression levels of Dec1, HSP105, and ribosomal proteins. Knockout of Dec1 resulted in slower OTM and reduced expression of ribosomal proteins. These findings suggest that the hypoxic environment in OTM plays a crucial role in the functions of Dec1 and ribosomal proteins in maintaining periodontal tissue homeostasis.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Review Biochemistry & Molecular Biology

Targeting the Isoprenoid Biosynthetic Pathway in Multiple Myeloma

Staci L. L. Haney et al.

Summary: Multiple myeloma (MM) is an incurable plasma cell malignancy. The isoprenoid biosynthetic pathway (IBP) is responsible for post-translational modification of proteins, and inhibitors targeting this pathway have shown anti-MM effects. Some IBP inhibitors have entered clinical trials, including nitrogenous bisphosphonates, statins, and farnesyltransferase inhibitors. Recent advances in the development of IBP inhibitors and their potential as anti-MM agents are discussed.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

Cell Type-Specific Anti-Viral Effects of Novel SARS-CoV-2 Main Protease Inhibitors

Nina Geiger et al.

Summary: Recently, we investigated novel pyridyl indole esters and peptidomimetics as potent inhibitors of SARS-CoV-2 main protease. We analyzed the impact of these compounds on viral replication and found that their effectiveness varied in different cell lines. In Huh-7 cells, the protease inhibitors suppressed viral replication by up to 5 orders of magnitude, while in Calu-3 cells, suppression by 2 orders of magnitude was achieved. Three pyridin-3-yl indole-carboxylates showed antiviral activity in all cell lines and also in human precision-cut lung slices.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Biochemistry & Molecular Biology

Novel 1,3,5-Triazinyl Aminobenzenesulfonamides Incorporating Aminoalcohol, Aminochalcone and Aminostilbene Structural Motifs as Potent Anti-VRE Agents, and Carbonic Anhydrases I, II, VII, IX, and XII Inhibitors

Eva Havrankova et al.

Summary: A series of potential human carbonic anhydrase inhibitors were synthesized and evaluated for their inhibition of different isoenzymes. Some compounds showed significant effects on hCA IX isoenzyme and demonstrated good activity against vancomycin-resistant Enterococcus faecalis (VRE).

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Aromatic Sulfonamides including a Sulfonic Acid Tail: New Membrane Impermeant Carbonic Anhydrase Inhibitors for Targeting Selectively the Cancer-Associated Isoforms

Simone Giovannuzzi et al.

Summary: This article presents a new drug design strategy for producing membrane-impermeant carbonic anhydrase inhibitors that selectively target tumor-associated CAs IX and XII. The study shows that this drug design strategy can achieve selective inhibition of tumor-associated CAs.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Comparison of Carbonic Anhydrases for CO2 Sequestration

Franziska Steger et al.

Summary: Strategies for depleting carbon dioxide (CO2) from flue gases are urgently needed, and carbonic anhydrases (CAs) can contribute to solving this problem. This current study examines four recombinantly produced CAs from different organisms, namely CAs from Acetobacterium woodii (AwCA or CynT), Persephonella marina (PmCA), Methanobacterium thermoautotrophicum (MtaCA or Cab), and Sulphurihydrogenibium yellowstonense (SspCA). The highest expression yields and activities were found for AwCA and PmCA. AwCA showed high stability in a mesophilic temperature range, while PmCA proved to be exceptionally thermostable. These results indicate the potential to utilize CAs from anaerobic microorganisms for CO2 sequestration applications.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Review Pharmacology & Pharmacy

Perspectives on the design and discovery of α-ketoamide inhibitors for the treatment of novel coronavirus: where do we stand and where do we go?

Alessio Nocentini et al.

Summary: Crystallography, previous drug design efforts, and many computational studies have provided a deeper understanding of the structural requirements for designing effective SARS-CoV-2 M-pro alpha-ketoamide inhibitors. However, all reported derivatives are peptidomimetics with a relatively high molecular weight. It is expected that future drug development will target effective compounds with lower molecular weights and a less peptidomimetic profile.

EXPERT OPINION ON DRUG DISCOVERY (2022)

Review Biochemistry & Molecular Biology

New Developments in Carbonic Anhydrase IX-Targeted Fluorescence and Nuclear Imaging Agents

Kuo-Ting Chen et al.

Summary: Carbonic anhydrase IX (CAIX) is a tumor-specific and hypoxia-induced biomarker that can be used for molecular imaging of solid malignancies. Nuclear imaging and optical fluorescence imaging are powerful tools for the diagnosis and treatment of tumors, and many CAIX-targeted molecular imaging probes have been developed.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Identification of Novel and Potent Indole-Based Benzenesulfonamides as Selective Human Carbonic Anhydrase II Inhibitors: Design, Synthesis, In Vitro, and In Silico Studies

Ahmed Elkamhawy et al.

Summary: In this study, a novel series of indole-based benzenesulfonamides were designed and synthesized as potential carbonic anhydrase inhibitors. The synthesized compounds were evaluated for their activity against different carbonic anhydrase isoforms, and compound 2a showed the most potent inhibition against the hCA II isoform with high selectivity.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Toward the Discovery of a Novel Class of Leads for High Altitude Disorders by Virtual Screening and Molecular Dynamics Approaches Targeting Carbonic Anhydrase

Amena Ali et al.

Summary: This study utilized co-crystallized inhibitors for pharmacophore-based virtual screening and molecular simulation, identifying several compounds that show potential as inhibitors for high-altitude disorders.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Inhibitors of Mitochondrial Human Carbonic Anhydrases VA and VB as a Therapeutic Strategy against Paclitaxel-Induced Neuropathic Pain in Mice

Laura Micheli et al.

Summary: Neuropathy development is a major side effect of anticancer treatments, but two compounds 5b and 5d have shown therapeutic and protective effects against paclitaxel-induced neuropathy.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Review Biochemistry & Molecular Biology

Newly Emerged Antiviral Strategies for SARS-CoV-2: From Deciphering Viral Protein Structural Function to the Development of Vaccines, Antibodies, and Small Molecules

Chunye Zhang et al.

Summary: The structure and function of proteins encoded by SARS-CoV-2 are crucial for targeted therapy and vaccine development. This article reviews the recent research findings on viral proteins that contribute to COVID-19 infection and disease pathogenesis, and discusses various therapeutic options and vaccines targeting these proteins.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Perfusion-Based Bioreactor Culture and Isothermal Microcalorimetry for Preclinical Drug Testing with the Carbonic Anhydrase Inhibitor SLC-0111 in Patient-Derived Neuroblastoma

Zihe Huo et al.

Summary: This study proposes a new patient-derived 3D slice-culture perfusion-based model for neuroblastoma treatment evaluation, combined with isothermal microcalorimetry. The use of the novel carbonic anhydrase IX and XII (CAIX/CAXII) inhibitor SLC-0111 showed promising results in reducing cell viability and thermogenesis in neuroblastoma cells. The perfusion-based bioreactor system allowed for the evaluation of drug response with intact tumor cells and stromal structure for up to 7 days. This approach can facilitate the development of personalized treatment strategies for neuroblastoma.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Complementary Experimental Methods to Obtain Thermodynamic Parameters of Protein Ligand Systems

Shilpa Mohanakumar et al.

Summary: In this study, we compared data obtained from the non-equilibrium process of thermal diffusion forced Rayleigh scattering (TDFRS) with data obtained from the equilibrium process of isothermal titration calorimetry (ITC). The results showed that the thermophoretic behavior quantified by the Soret coefficient S_T agreed with the Gibb's free energy Delta G determined in the ITC experiment. We also investigated the influence of fluorescent labeling on the binding behavior and found that the dye had a significant impact.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Relationship between Changes in the Protein Folding Pathway and the Process of Amyloid Formation: The Case of Bovine Carbonic Anhydrase II

Bogdan S. Melnik et al.

Summary: Proteins form amyloid fibrils more easily when transitioning from a native to an intermediate state. Mutations in the protein can affect both the unfolding pathway and the rate of amyloid formation. In this study, specific amino acid substitutions in bovine carbonic anhydrase II were found to either accelerate or slow down amyloid formation.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Benzenesulfonamides Incorporating Hydantoin Moieties Effectively Inhibit Eukaryoticand Human Carbonic Anhydrases

Morteza Abdoli et al.

Summary: A series of novel compounds were synthesized and evaluated for their inhibition of eukaryotic and human carbonic anhydrases. The results showed good inhibition against some target enzymes and weaker inhibition against others. These findings are important for the search for potential antifungal drugs.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Hyperammonemia in Russia Due to Carbonic Anhydrase VA Deficiency Caused by Homozygous Mutation p.Lys185Lys (c.555G>A) of the CA5A Gene

Natalia Semenova et al.

Summary: Hyperammonemia due to carbonic anhydrase VA deficiency is a rare hereditary disease that causes unexplained encephalopathic hyperammonemia during the neonatal period and infancy. We found a high frequency of carriers of the mutation in Russia, suggesting targeted testing in neonatal intensive care units can facilitate early detection.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Identification of Darunavir Derivatives for Inhibition of SARS-CoV-2 3CLpro

Ling Ma et al.

Summary: In this study, Darunavir derivatives that inhibit SARS-CoV-2 3CL(pro) were identified through a high-throughput screening method. These compounds showed favorable antiviral activity and similar potency against Omicron variants.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

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)

Review Biochemistry & Molecular Biology

Application of Metabolic Reprogramming to Cancer Imaging and Diagnosis

Yi-Fang Yang et al.

Summary: Cellular metabolism regulates physiological mechanisms and homeostasis in an individual. Abnormal metabolic reprogramming, caused by various factors such as gene mutations and epigenetic modifications, is associated with the development of diseases, including cancer. Metabolism-related molecules can serve as markers or prevention targets for cancer progression. Translational medicines using metabolic substrates and precursors have been developed for imaging and therapeutic purposes. Isotopically labeled compounds can be used to localize and visualize tumor cells.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Ratiometric Zinc Biosensor Based on Bioluminescence Resonance Energy Transfer: Trace Metal Ion Determination with Tunable Response

Evgenia G. Matveeva et al.

Summary: A novel zinc ion biosensing approach using a carbonic anhydrase-Oplophorus luciferase fusion protein has been described, which employs bioluminescence resonance energy transfer (BRET) to detect zinc ions in solution. This method offers high sensitivity and selectivity, allowing quantitative determination of free zinc ions and detection of their presence through color change in bioluminescence.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Review Biochemistry & Molecular Biology

Nanoparticles for Antimicrobial Agents Delivery-An Up-to-Date Review

Doina-Antonia Mercan et al.

Summary: Infectious diseases pose a growing threat to public health and medical systems globally, especially with the emergence of multidrug-resistant pathogens. This has led to the convergence of medicine and nanotechnology in order to combat severe microbial infections. Recent research has focused on utilizing various nanoparticles as drug delivery vehicles to overcome the limitations of current treatment options. This paper reviews the latest successful nanoformulations that show great potential in combating bacteria, fungi, viruses, and parasites of interest in human medicine.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Synthesis and Characterization of Ligand-Stabilized Silver Nanoparticles and Comparative Antibacterial Activity against E. coli

Nishal M. Egodawaththa et al.

Summary: Silver nanoparticles conjugated with organic ligands have been successfully synthesized and demonstrated significant antimicrobial activity and antibacterial capabilities against E. coli. The synthesis of functionalized silver nanoparticles is critical for the further development of silver-nanoconjugated antibacterial agents.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Review Biochemistry & Molecular Biology

Therapeutic Targeting of Glutaminolysis as a Novel Strategy to Combat Cancer Stem Cells

Ting-Wan Kao et al.

Summary: Rare subpopulations of cancer stem cells (CSCs) play a crucial role in cancer metastasis and treatment resistance. These CSCs have unique metabolic patterns, relying on the oxidation of glucose, glutamine, and fatty acids for survival. Glutaminolysis, a series of metabolic reactions, is involved in CSCs' biosynthesis and redox homeostasis. Researchers are exploring targeting glutaminolysis as a novel therapy for CSCs, with promising early-phase clinical trials of small molecule inhibitors. This review summarizes current findings in glutaminolysis of CSCs and potential cancer therapies targeting this process.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Chalcogen Bond as a Factor Stabilizing Ligand Conformation in the Binding Pocket of Carbonic Anhydrase IX Receptor Mimic

Kamil Wojtkowiak et al.

Summary: This study investigates the non-covalent interactions of Carbonic Anhydrase IX using quantum-chemical approaches, highlighting its significance in cancer treatment and exploring potential anticancer inhibitors. The findings suggest that chalcogen bonding plays a crucial role in conformational stability and free energy mapping of the system.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Squaramide-Tethered Sulfonamides and Coumarins: Synthesis, Inhibition of Tumor-Associated CAs IX and XII and Docking Simulations

Giulia Arrighi et al.

Summary: In this study, a series of compounds inhibiting carbonic anhydrases were successfully synthesized by appending a hydrophobic aromatic tail and using squaramides as linkers. Interesting structure-activity relationships were obtained by modifying the structural parameters of the compounds. Among them, m-substituted derivative 11 and 16c exhibited good activity and selectivity.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Novel Insights on Human Carbonic Anhydrase Inhibitors Based on Coumalic Acid: Design, Synthesis, Molecular Modeling Investigation, and Biological Studies

Virginia Pontecorvi et al.

Summary: In this study, a new series of derivatives targeting tumor-related hCA isoforms IX and XII were developed, showing effective and selective inhibitory activity in the low nanomolar range. These compounds demonstrated potential synergistic effects with doxorubicin under hypoxic conditions and showed good biocompatibility on healthy cells. Computational techniques predicted the binding mode of these compounds to the active site of tumor-associated human CA IX, providing valuable data for the design of tighter binding inhibitors.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Neutralizing Ability of a Single Domain VNAR Antibody: In Vitro Neutralization of SARS-CoV-2 Variants of Concern

Blanca J. Valdovino-Navarro et al.

Summary: This study characterized a VNAR antibody (SP240) and demonstrated its potential as a neutralizing antibody against emerging SARS-CoV-2 variants.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Review Biochemistry & Molecular Biology

α-CAs from Photosynthetic Organisms

Emma Langella et al.

Summary: This article provides an overview of recent literature on alpha-CAs from photosynthetic organisms, discussing their functions and mechanisms in higher plants, algae, and cyanobacteria. It emphasizes the need for further research to understand the structure-function relationship of alpha-CAs.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

The Spike Mutants Website: A Worldwide Used Resource against SARS-CoV-2

Isabella Romeo et al.

Summary: The large number of SARS-CoV-2 mutations has prompted scientific research on vaccines and drugs. The Spike Mutants website provides structural information and molecular dynamics trajectories of the spike protein and its variants, serving as a tool for investigating the impact of novel mutations and accelerating drug discovery.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Suppression of Tumor Growth and Cell Migration by Indole-Based Benzenesulfonamides and Their Synergistic Effects in Combination with Doxorubicin

Phuong Linh Nguyen et al.

Summary: The study evaluated the antitumor effects of a series of CA inhibitors on various cancer cell lines, identifying two compounds with potent anticancer activity against breast cancer cells MCF-7 and SK-BR-3, especially in combination with DOX, demonstrating synergistic cytotoxic effects.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Review Biochemistry & Molecular Biology

Evolution of Anti-SARS-CoV-2 Therapeutic Antibodies

Juan C. Almagro et al.

Summary: This review examines the characteristics of nine therapeutic antibodies approved for Emergency Use Authorization in response to the COVID-19 pandemic. It highlights the neutralization profile against variants of concern (VOCs), selection methods, somatic mutations, isotype, Fc modifications, and epitopes recognized on the receptor-binding domain (RBD) of SARS-CoV-2. The review concludes that effective therapeutic antibodies bind to an epitope formed by conserved residues critical for the RBD:hACE-2 interaction. The information presented here can aid in the design of more efficacious antibodies for the prevention and treatment of COVID-19 and other infectious diseases.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Hypoxia Marker Carbonic Anhydrase IX Is Present in Abdominal Aortic Aneurysm Tissue and Plasma

Katarina Grossmannova et al.

Summary: Abdominal aortic aneurysms (AAA) are a significant cause of premature deaths worldwide. In this study, the presence of hypoxia-related protein CA IX in AAA tissues was confirmed, suggesting its potential role in aneurysmal wall remodeling.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Biochemistry & Molecular Biology

Evaluating the efficiency of enzyme accelerated CO2 capture: chemical kinetics modelling for interpreting measurement results

Lorenzo Parri et al.

Summary: This paper evaluates the efficiency of the carbonic anhydrase (CA) enzyme in accelerating the hydration of CO2 by monitoring the pH value and CO2 concentration of a solution, inducing transients, and analyzing different kinetics involved in the steady-state recovery. The main contribution of this work is interpreting measurement results using dynamical system theory and chemical kinetics modeling to characterize the activity of CA enzymes.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2021)

Review Pharmacology & Pharmacy

Carbonic anhydrase inhibitors: an update on experimental agents for the treatment and imaging of hypoxic tumors

Claudiu T. Supuran

Summary: Hypoxic tumors overexpress proteins that can be targeted for antitumor drugs, with CA IX and XII being validated targets that inhibit the growth and metastasis of various cancer types. Various inhibitors, including SLC-0111, have shown significant antitumor activity either alone or in combination with other therapies.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2021)

Editorial Material Chemistry, Medicinal

Coronaviruses

Claudiu T. Supuran

EXPERT OPINION ON THERAPEUTIC PATENTS (2021)

Article Multidisciplinary Sciences

Genome-wide synthetic lethal screen unveils novel CAIX-NFS1/xCT axis as a targetable vulnerability in hypoxic solid tumors

Shawn C. Chafe et al.

Summary: The study identified a redox homeostasis network involving the iron-sulfur cluster enzyme NFS1 in the survival mechanisms governed by the tumor hypoxia-induced pH regulator CAIX. Targeting CAIX while depleting NFS1 or blocking cyst(e)ine availability enhanced ferroptosis and inhibited tumor growth significantly. Altering intracellular pH and iron homeostasis through inhibiting CAIX activity may lead to the development of innovative therapeutic strategies for solid tumors to overcome hypoxia- and acidosis-mediated tumor progression and therapeutic resistance.

SCIENCE ADVANCES (2021)

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)

Review Cell Biology

Interplay of Carbonic Anhydrase IX With Amino Acid and Acid/Base Transporters in the Hypoxic Tumor Microenvironment

Geetha Venkateswaran et al.

FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2020)

Article Chemistry, Medicinal

Coral Carbonic Anhydrases: Regulation by Ocean Acidification

Didier Zoccola et al.

MARINE DRUGS (2016)

Article Biochemistry & Molecular Biology

Biochemical characterization of the chloroplastic β-carbonic anhydrase from Flaveria bidentis (L.) Kuntze

Nina A. Dathan et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2014)

Review Biotechnology & Applied Microbiology

Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

Claudiu T. Supuran

NATURE REVIEWS DRUG DISCOVERY (2008)