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Makale Tam Makale Uluslararası 2016

The human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibition effects of trimethoxyindane derivatives

Parham TASLIMI, İlhami Gülçin, Bunyamin ÖZGERIŞ, Süleyman Göksu, Ferhan Tumer, Saleh H. ALWASEL, Claudiu T. SUPURAN

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 31 · Sayı 1 · ss. 152–157 · 02.01.2016
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Özet

Carbonic anhydrases (CAs, EC 4.2.1.1) had six genetically distinct families described to date in various organisms. There are 16 known CA isoforms in humans. Human CA isoenzymes I and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. Acetylcholine esterase (AChE. EC 3.1.1.7) is a hydrolase that hydrolyzes the neurotransmitter acetylcholine relaying the signal from the nerve. In this study, some trimethoxyindane derivatives were investigated as inhibitors against the cytosolic hCA I and II isoenzymes, and AChE enzyme. Both hCA isozymes were inhibited by trimethoxyindane derivatives in the low nanomolar range. These compounds were good hCA I inhibitors (Kis in the range of 1.66-4.14nM) and hCA II inhibitors (Kis of 1.37-3.12nM) and perfect AChE inhibitors (Kis in the range of 1.87-7.53nM) compared to acetazolamide as CA inhibitor (Ki: 6.76nM for hCA I and Ki: 5.85nM for hCA II) and Tacrine as AChE inhibitor (Ki: 7.64nM).

Anahtar kelimeler

enzyme inhibition TROUT ONCORHYNCHUS-MYKISS SULFONAMIDE DERIVATIVES ENZYME-ACTIVITY ISOZYMES I ISOFORMS I PURIFICATION VITRO ACETYLCHOLINE ESTERASE enzyme purification Lactoperoxidase bovine milk affinity chromatography carbonic anhydrase trimethoxyindane derivatives

Atıf için künye

TASLIMI, P., Gülçin, İ., ÖZGERIŞ, B., Göksu, S., Tumer, F., ALWASEL, S. H., & SUPURAN, C. T. (2016). The human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibition effects of trimethoxyindane derivatives. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31(1), 152–157. https://doi.org/10.3109/14756366.2015.1014476

BibTeX 
@article{taslimi2016-67580,
  author = {TASLIMI, Parham and Gülçin, İlhami and ÖZGERIŞ, Bunyamin and Göksu, Süleyman and Tumer, Ferhan and ALWASEL, Saleh H. and SUPURAN, Claudiu T.},
  title = {The human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibition effects of trimethoxyindane derivatives},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2016},
  volume = {31},
  number = {1},
  pages = {152--157},
  issn = {1475-6366},
  doi = {10.3109/14756366.2015.1014476},
  url = {https://akademik.atauni.edu.tr/yayinlar/67580-the-human-carbonic-anhydrase-isoenzymes-i-and-ii-hca-i-and-ii-inhibition-effects}
}