The enzyme carbonic anhydrase was detected with an indirect immunoperoxidase method in 22 kidney exploratory excisions of patients with urolithiasis, ren mobilis or stenosis of ureteral pelvic junction. The reactivity of carbonic anhydrase was related to disturbances in acid-base equilibrium. Carbonic anhydrase was detected in the convoluted parts of the distal tubules, connecting tubules and cortical collecting ducts. The distribution corresponds vastly with the localization of intercalated cells. The reaction was increased in three cases with acid rigidity and was strongly reduced in one case of renal tubular acidosis.
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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 PDFCureus
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 PDFJ 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 PDFAngew Chem Int Ed Engl
January 2025
Shanghai Jiao Tong University, Chemistry, 800 Dongchuan Road, Minhang, 200240, Shanghai, CHINA.
Hydrogen sulfide (H2S) plays crucial inflammatory modulating roles, representing a promising candidate for anti-inflammatory therapies. However, current H2S delivery approaches lack sufficient specificity against inflammatory response. Herein, regarding the overexpressed aminopeptidase N (APN) at the inflammation sites, an APN-activated self-immolative carbonyl sulfide (COS)/H2S donor (AlaCOS) was developed for inflammatory response-specific H2S delivery.
View Article and Find Full Text PDFActa Crystallogr F Struct Biol Commun
February 2025
Department of Biological Chemistry, University of Michigan, Ann Arbor, MI 48109, USA.
X-ray crystallography remains the dominant method of determining the three-dimensional structure of proteins. Nevertheless, this resource-intensive process may be hindered by the unintended crystallization of contaminant proteins from the expression source. Here, the serendipitous discovery of two novel crystal forms and one new, high-resolution structure of carbonic anhydrase 2 (CA2) from Escherichia coli that arose during a crystallization campaign for an unrelated target is reported.
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