Thioxolone acts as a prodrug in the presence of carbonic anhydrase II (CA II), whereby the molecule is cleaved by thioester hydrolysis to the carbonic anhydrase inhibitor, 4-mercaptobenzene-1,3-diol (TH0). Thioxolone was soaked into the proton transfer mutant H64A of CA II in an effort to capture a reaction intermediate via X-ray crystallography. Structure determination of the 1.2 Å resolution data revealed the TH0 had been modified to a 4,4'-disulfanediyldibenzene-1,3-diol, a product of crystallization conditions, and a zinc ligated 2,4-dihydroxybenzenesulfenic acid, most likely induced by radiation damage. Neither ligand was likely a result of an enzymatic mechanism.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2957018 | PMC |
| http://dx.doi.org/10.1021/jz100954h | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Association of salivary proteins with dental caries in children with mixed dentition: a systematic review.
Eur Arch Paediatr Dent
January 2025
Qatar University Health, College of Dental Medicine, Qatar University, Doha, Qatar.
Purpose: To review the current evidence on the association between salivary protein profile and dental caries in children during mixed dentition stage.
Methods: This systematic review followed the PRISMA 2020 guidelines. Searches were run in PubMed, Scopus and Embase along with gray literature.
Two-photon photosensitizer for specific targeting and induction of tumor pyroptosis to elicit systemic immunity-boosting anti-tumor therapy.
Biomaterials
January 2025
State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics & Center for Molecular Imaging and Translational Medicine, School of Public Health, Xiamen University, Xiamen, 361102, China. Electronic address:
Photodynamic therapy (PDT) has garnered increasing attention in cancer treatment due to its precise spatiotemporal selectivity and non-invasive nature. However, several challenges, including the inability of photosensitizers to discriminate between tumor and healthy tissues, as well as the limited tissue penetration depth of light sources, impede its broader application. To surmount these impediments, our research introduces a two-photon photosensitizer (TPSS) that specifically targets tumor overexpressing carbonic anhydrase IX (CA IX), thereby exhibiting exceptional specificity for tumor cells.
View Article and Find Full Text PDFSulphonyl thiourea compounds containing pyrimidine as dual inhibitors of I, II, IX, and XII carbonic anhydrases and cancer cell lines: synthesis, characterization and studies.
RSC Med Chem
December 2024
VNU University of Education, Vietnam National University, Hanoi 144 Xuan Thuy, Cau Giay Ha Noi Vietnam.
Some novel sulphonyl thiourea derivatives (7a-m) containing 4,6-diarylpyrimidine rings were designed and synthesized using a one-pot procedure. These compounds exhibited remarkable dual inhibitory activity against human carbonic anhydrase CA I, CA II, CA IX, and XII isoenzymes and some cancer cell lines. Among them, some thioureas had significantly more potent inhibitory activities in the order of 7l > 7c > 7f (against the CA I isoform), 7f > 7b > 7c (against the CA II isoform), 7c > 7g > 7a > 7b (against the CA IX isoform), and 7d > 7c > 7g > 7f (against the CA XII isoform).
View Article and Find Full Text PDFExploring Neurohormonal Modulation by Acetazolamide in Heart Failure.
Cureus
December 2024
Gastroenterolgy, Sindh Institute of Urology and Transplantation, Karachi, PAK.
Background Heart failure (HF) is commonly managed by addressing water and sodium (Na) balance, with arterial circulation playing a major role in influencing renal Na and water excretion. Recently, chloride (Cl) has been recognized as an important factor in HF, associated with volume regulation and its modulation of renin-angiotensin-aldosterone system (RAAS) activity through macula densa signaling, which impacts Na retention and neurohormonal activation. Acetazolamide, a carbonic anhydrase inhibitor, can enhance decongestion in HF by increasing urinary Na and Cl excretion when added to loop diuretics, a mechanism supported by prior studies demonstrating improved urine output and decongestion.
View Article and Find Full Text PDFNovel -(3-(1-(4-sulfamoylphenyl)triazol-4-yl)phenyl)benzamide Derivatives as Potent Carbonic Anhydrase Inhibitors with Broad-Spectrum Anticancer Activity: Leveraging Tail and Dual-Tail Approaches.
J Med Chem
January 2025
Biomedical Research Division, Korea Institute of Science and Technology (KIST), Seoul 02792, Republic of Korea.
Carbonic anhydrases (CAs) IX and XII are crucial for the survival and metastasis of solid tumors under hypoxic conditions. We designed compounds -, integrating triazole and benzenesulfonamide scaffolds known for inhibiting tumor-associated CAs IX/XII. Initial synthesis included compounds -, followed by diversification with small hydrophobic groups (-) and hydrophilic heterocyclic secondary amines (-).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!