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Aim: Human carbonic anhydrases (hCAs) are involved in many physiological processes including respiration, pH control, ion transport, bone resorption, and gastric fluid secretion. Recently, CA IX and CA XII have been studied for their role in cancer diseases, motivating the design of inhibitors of these isoforms.
Material And Method: Here, we used the tail approach to design a new series of monoaryl () and bicyclic () benzensulfonamide derivatives CA IX and CA XII inhibitors.
Eur J Nucl Med Mol Imaging
December 2024
Department of PET-CT, Harbin Medical University Cancer Hospital, Harbin, 150001, China.
Purpose: This first-in-human study aimed to evaluate the radiation dosimetry and whole-body biodistribution of [F]AlF-NYM005, a novel small-molecule carbonic anhydrase IX (CAIX) targeting agent, and to investigate its ability to detect CAIX-positive tumors using PET scans in a cohort of clear cell renal cell carcinoma (ccRCC) patients.
Methods: [F]AlF-NYM005 was synthesized using a fully automatic cassette module Mortenon M1 (Nuoyu, China). Thirty-five patients with a suspicious lesion considered primary renal malignancy or a history of ccRCC were prospectively recruited and studied.
Pain Manag
September 2024
Department of Clinical Development & Medical Affairs, Hetero Labs Limited, Hyderabad, India.
Aim: Polmacoxib, a new COX-2 inhibitor with carbonic anhydrase (CA) inhibitory action, is expected to help minimize the adverse effects associated with other NSAIDs, like GI (gastrointestinal) and CV (cardiovascular) system- related issues. The comparative efficacy and safety of polmacoxib 2 mg (manufactured by Hetero Labs Limited) versus celecoxib 200 mg (manufactured by Hetero Labs Limited) were assessed in this randomized, double-anonymous, clinical study in Indian adult patients diagnosed with idiopathic osteoarthritis (OA) of the.
Patients & Methodology: 18 years and older patients of either sex, clinically and radiographically diagnosed idiopathic knee or hip OA were randomized to receive either polmacoxib or celecoxib in a 1:1 ratio.
J Nucl Med
December 2024
Department of Nuclear Medicine, Affiliated Hospital of Jiangnan University, Wuxi, China;
This study aimed to investigate the diagnostic efficacy of [Ga]Ga-NYM046 PET/CT in animal models and patients with clear cell renal cell carcinoma (ccRCC) and to compare its performance with that of F-FDG PET/CT. The in vivo biodistribution of [Ga]Ga-NYM046 was evaluated in mice bearing OS-RC-2 xenografts. Twelve patients with ccRCC were included in the study; all completed paired [Ga]Ga-NYM046 PET/CT and F-FDG PET/CT.
View Article and Find Full Text PDFBioorg Chem
December 2024
Natural and Medical Sciences Research Centre, University of Nizwa, P.O. Box 33, PC 616, Birkat Al Mauz, Nizwa, Sultanate of Oman. Electronic address:
Carbonic anhydrase II (CA II) is crucial for maintaining homeostasis in several processes, including respiration, lipogenesis, gluconeogenesis, calcification, bone resorption, and electrolyte balance. It is a pivotal druggable target which is implicated in glaucoma, renal, gastric, and pancreatic carcinomas, as well as in malignant brain tumours. Therefore, to identify new CA II (bovine) inhibitors, the current study was designed to synthesize a library of 20 new triazole-linked hydrazones (6a-t).
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