Cancers, Vol. 15, Pages 4507: Reducing the Invasiveness of Low- and High-Grade Endometrial Cancers in Both Primary Human Cancer Biopsies and Cell Lines by the Inhibition of Aquaporin-1 Channels
a J. Yool
Aquaporin (AQP) channels in endometrial cancer (EC) cells are of interest as pharmacological targets to reduce tumor progression. A panel of compounds, including AQP1 ion channel inhibitors (AqB011 and 5-(phenoxymethyl) furan-2-carbaldehyde, PMFC), were used to test the hypothesis that inhibition of key AQPs can limit the invasiveness of low- and high-grade EC cells. We evaluated the effects on transwell migration in EC cell lines (Ishikawa, MFE-280) and primary EC cells established from surgical tissues (n = 8). Quantitative PCR uncovered classes of AQPs not previously reported in EC that are differentially ...
Source: Cancers - September 11, 2023 Category: Cancer & Oncology Authors: Sidra Khan Noor A. Lokman Martin K. Oehler Carmela Ricciardelli Andrea J. Yool Tags: Article Source Type: research
Design and synthesis of multivalent drug delivery system with CA IX inhibitors as ligands
In this study, we have developed a novel multivalent ligand delivery system for SN38, utilizing acetazolamide, a carbonic anhydrase IX (CA IX) inhibitor, as the target ligand. Our multivalent ligand delivery systems exhibited superior metabolic stability and enhanced targeting specificity compared to SMDC molecules. Furthermore, they demonstrated improved anti-proliferation activity, addressing the existing challenges associated with the low receptor affinity and rapid metabolism of SMDCs.PMID:37678058 | DOI:10.1016/j.bmc.2023.117456 (Source: Bioorganic and Medicinal Chemistry)
Source: Bioorganic and Medicinal Chemistry - September 7, 2023 Category: Chemistry Authors: Mengyuan Ding Qiwen Zhu Wei Lu Shulei Zhu Source Type: research
Design and synthesis of multivalent drug delivery system with CA IX inhibitors as ligands
In this study, we have developed a novel multivalent ligand delivery system for SN38, utilizing acetazolamide, a carbonic anhydrase IX (CA IX) inhibitor, as the target ligand. Our multivalent ligand delivery systems exhibited superior metabolic stability and enhanced targeting specificity compared to SMDC molecules. Furthermore, they demonstrated improved anti-proliferation activity, addressing the existing challenges associated with the low receptor affinity and rapid metabolism of SMDCs.PMID:37678058 | DOI:10.1016/j.bmc.2023.117456 (Source: Bioorganic and Medicinal Chemistry)
Source: Bioorganic and Medicinal Chemistry - September 7, 2023 Category: Chemistry Authors: Mengyuan Ding Qiwen Zhu Wei Lu Shulei Zhu Source Type: research
Acetazolamide in Acute Decompensated Heart Failure With Volume Overload
This study included 519 patients admitted for acute decompensated heart failure who were randomly assigned to receive either acetazolamide 500 mg IV daily (259 patients) or placebo (260 patients) in addition to standardized IV loop diuretics. The primary outcome was complete decongestion at 72 hours, defined as the absence of any clinical sign of fluid overload using a congestion scoring system. Successful decongestion rates were significantly higher in the treatment group (42%) versus the placebo group (31%). Of relevance to hospital medicine, patients treated with acetazolamide had shorter lengths of stay (8.8 days, vers...
Source: The Hospitalist - September 1, 2023 Category: Hospital Management Authors: Ronda Whitaker Tags: Cardiology In the Literature Source Type: research
The Vienna idiopathic intracranial hypertension database-An Austrian registry
CONCLUSION: The large representative Vienna IIH cohort characterizes IIH-related symptoms, diagnostic findings, treatment, and outcome emphasizing substantial long-term sequelae of IIH. Future analyses will aim to refine phenotyping and identify factors predicting outcome.PMID:37650963 | DOI:10.1007/s00508-023-02252-x (Source: Wiener Klinische Wochenschrift)
Source: Wiener Klinische Wochenschrift - August 31, 2023 Category: General Medicine Authors: Philip Pruckner Christoph Mitsch Stefan Macher Nik Krajnc Wolfgang Marik Klaus Novak Christian W öber Berthold Pemp Gabriel Bsteh Source Type: research
The Vienna idiopathic intracranial hypertension database-An Austrian registry
CONCLUSION: The large representative Vienna IIH cohort characterizes IIH-related symptoms, diagnostic findings, treatment, and outcome emphasizing substantial long-term sequelae of IIH. Future analyses will aim to refine phenotyping and identify factors predicting outcome.PMID:37650963 | DOI:10.1007/s00508-023-02252-x (Source: Wiener Klinische Wochenschrift)
Source: Wiener Klinische Wochenschrift - August 31, 2023 Category: General Medicine Authors: Philip Pruckner Christoph Mitsch Stefan Macher Nik Krajnc Wolfgang Marik Klaus Novak Christian W öber Berthold Pemp Gabriel Bsteh Source Type: research
The Vienna idiopathic intracranial hypertension database-An Austrian registry
CONCLUSION: The large representative Vienna IIH cohort characterizes IIH-related symptoms, diagnostic findings, treatment, and outcome emphasizing substantial long-term sequelae of IIH. Future analyses will aim to refine phenotyping and identify factors predicting outcome.PMID:37650963 | DOI:10.1007/s00508-023-02252-x (Source: Wiener Klinische Wochenschrift)
Source: Wiener Klinische Wochenschrift - August 31, 2023 Category: General Medicine Authors: Philip Pruckner Christoph Mitsch Stefan Macher Nik Krajnc Wolfgang Marik Klaus Novak Christian W öber Berthold Pemp Gabriel Bsteh Source Type: research
The Vienna idiopathic intracranial hypertension database-An Austrian registry
CONCLUSION: The large representative Vienna IIH cohort characterizes IIH-related symptoms, diagnostic findings, treatment, and outcome emphasizing substantial long-term sequelae of IIH. Future analyses will aim to refine phenotyping and identify factors predicting outcome.PMID:37650963 | DOI:10.1007/s00508-023-02252-x (Source: Wiener Klinische Wochenschrift)
Source: Wiener Klinische Wochenschrift - August 31, 2023 Category: General Medicine Authors: Philip Pruckner Christoph Mitsch Stefan Macher Nik Krajnc Wolfgang Marik Klaus Novak Christian W öber Berthold Pemp Gabriel Bsteh Source Type: research
The Vienna idiopathic intracranial hypertension database-An Austrian registry
CONCLUSION: The large representative Vienna IIH cohort characterizes IIH-related symptoms, diagnostic findings, treatment, and outcome emphasizing substantial long-term sequelae of IIH. Future analyses will aim to refine phenotyping and identify factors predicting outcome.PMID:37650963 | DOI:10.1007/s00508-023-02252-x (Source: Wiener Klinische Wochenschrift)
Source: Wiener Klinische Wochenschrift - August 31, 2023 Category: General Medicine Authors: Philip Pruckner Christoph Mitsch Stefan Macher Nik Krajnc Wolfgang Marik Klaus Novak Christian W öber Berthold Pemp Gabriel Bsteh Source Type: research
The Vienna idiopathic intracranial hypertension database-An Austrian registry
CONCLUSION: The large representative Vienna IIH cohort characterizes IIH-related symptoms, diagnostic findings, treatment, and outcome emphasizing substantial long-term sequelae of IIH. Future analyses will aim to refine phenotyping and identify factors predicting outcome.PMID:37650963 | DOI:10.1007/s00508-023-02252-x (Source: Wiener Klinische Wochenschrift)
Source: Wiener Klinische Wochenschrift - August 31, 2023 Category: General Medicine Authors: Philip Pruckner Christoph Mitsch Stefan Macher Nik Krajnc Wolfgang Marik Klaus Novak Christian W öber Berthold Pemp Gabriel Bsteh Source Type: research
P004/33 Recurrent intracranial hypertension secondary to collateral regression following successful occlusion of dural AV fistula
PresentationA 35 year-old lady presented with headache, tinnitus and papilloedema. LP showed raised CSF pressure. Acetazolamide was commenced for presumed idiopathic intracranial hypertension with atypical phenotype but papilloedema persisted despite increasing dosage.CTV showed a non-occlusive right sigmoid sinus filling defect with bilateral transverse sinus stenosis. Prominent, tortuous veins straddled the tentorium, indicating venous hypertension.Angiography identified a dural A-V fistula involving the torcula and right transverse sinus. Tributaries included bilateral MMA and occipital artery branches, bilateral poster...
Source: Journal of NeuroInterventional Surgery - August 21, 2023 Category: Neurosurgery Authors: Roberts, S., Jain, A., Islim, F., Nejadhamzeeigilani, H., Saleem, N., Lily, O., Vinjam, M. Tags: 4.2 CASE PROPOSAL - Brain AVM/AVF, spinal vascular malformations Source Type: research
Novel coumarin-chalcone derivatives: Synthesis, characterization, antioxidant, cyclic voltammetry, molecular modelling and biological evaluation studies as acetylcholinesterase, α-glycosidase, and carbonic anhydrase inhibitors
In this study, a total of 12 coumarin-chalcone derivatives, 6 of which are original were synthesized. The structures of the newly synthesized compounds were elucidated by 1H NMR, 13C NMR, IR, and elemental analysis methods (7g-7l). The antioxidant potencies measured by using CUPRAC method (Trolox equivalent total antioxidant capacity) were as follows: 7j > 7i > 7c > 7d > 7k > 7l > 7f > 7h > 7e > 7g > 7a >7b. Furthermore, the compounds were evaluated against human carbonic anhydrases I, II, acetylcholinesterase and α-glycosidase enzymes. Compounds 7c, 7e, 7g, 7i, 7j and 7l showed promising ...
Source: Chemico-Biological Interactions - August 13, 2023 Category: Molecular Biology Authors: H ülya Çelik Onar Eda Mehtap Özden Hava Dudu Taslak İlhami Gülçin Abdulilah Ece Erol Er çağ Source Type: research
Is N-methylacetazolamide a possible new therapy against ischemia-reperfusion injury?
The increase of intracellular Ca2+ concentration, produced principally by its influx through the L-type Ca2+ channels, is one of the major contributors to the ischemia-reperfusion injury. The inhibition of those channels in different experimental models was effective to ameliorate the post-ischemic damage. However, at a clinical level, the results were contradictory. Recent results of our group obtained in an ¨ex vivo¨ heart model demonstrated that a chemical derived from acetazolamide, the N-methylacetazolamide (NMA) protected the heart against ischemia-reperfusion injury, diminishing the infarct size and improving the ...
Source: Frontiers in Pharmacology - August 10, 2023 Category: Drugs & Pharmacology Source Type: research
The manifestations of metabolic acidosis during acetazolamide treatment in a cohort of pediatric idiopathic intracranial hypertension
ConclusionsAlthough laboratory finding of metabolic acidosis is common among patients with idiopathic intracranial hypertension treated with acetazolamide, it is not correlated with clinics. Therefore, we recommend sending blood tests during acetazolamide treatment based on clinical judgment.Graphical abstractA higher resolution version of the Graphical abstract is available as Supplementary information (Source: Pediatric Nephrology)
Source: Pediatric Nephrology - July 22, 2023 Category: Urology & Nephrology Source Type: research
