Delving into the Latest Updates on CA inhibitor (Sakarya University) with Synapse

Overview

Basic Info

Drug Type

Chemical drugs

Synonyms-

Target

CA1 x CA2

Action

inhibitors

Mechanism

CA1 inhibitors(Carbonic anhydrase I inhibitors), CA2 inhibitors(Carbonic anhydrase II inhibitors)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Sakarya University

Active Organization

Sakarya University

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

HCO₃^- is involved in pH homoeostasis and plays a multifaceted role in human health. HCO₃^- has been recognized for its antimicrobial properties and is pivotal in bacterial antibiotic susceptibility. Notably, the interconversion between CO₂ and HCO₃^-, facilitated by the enzyme carbonic anhydrase (CA), is crucial in tissues infected by pathogens. Studies have highlighted the antimicrobial potency of CA inhibitors, emphasizing the importance of this enzyme in this area. The potential of HCO₃^- as an antibiotic adjuvant is evident; its ability to increase virulence in pathogens such as Enterococcus faecalis and Mycobacterium tuberculosis requires meticulous scrutiny. HCO₃^- modulates bacterial behaviours in diverse manners: it promotes Escherichia coli O157:H7 colonization in the human gut by altering specific gene expression and, with Pseudomonas aeruginosa, amplifies the effect of tobramycin on planktonic cells while promoting biofilm formation. These multifaceted effects necessitate profound mechanistic exploration before HCO₃^- can be considered a promising clinical adjuvant.

31 Dec 2025·JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Hidden targets in dermatology: In vitro and In silico inhibitory effects of common 23 dermatologic drugs on human carbonic anhydrase isoenzymes I and II

Article

Author: Uslu, Harun ; Çıkrıkcı, Kübra ; Can, İlkay ; Gençer, Nahit

In this study, we have aimed to determine the in vitro and in silico effects of 23 frequently used dermatologic drugs on human carbonic anhydrase I (hCA I) and II (hCA II). The inhibitory effects of the drugs on hCA I and hCA II were determined by esterase methods. The most potent inhibitors were isotretinoin for hCA I (Ki= 5.75 µM) and valaciclovir for hCA II (Ki= 5.74 µM). Ketotifen (Ki= 6.98 µM), pantoprazole (Ki= 7.16 µM) and acyclovir (Ki= 7.31 µM) were also potent inhibitors for hCA I. Isotretinoin (Ki= 6.54 µM), brivudine (Ki= 7.44 µM) and fluconazole (Ki= 7.91 µM) were also potent inhibitors for hCA II. Terbinafine hydrochloride was a weak CA inhibitor for both of these isoenzymes (Ki= 20.58 µM for hCA I and 20.32 µM for hCA I). Therefore, the drug, having a weak CA inhibitory activity, may be preferred primarily in patients with a skin disease compared to the other drugs due to important physiological functions of CAs. Molecular docking studies have shown that acitretin and isotretinoin, in particular, will inhibit hCA I at lower concentrations and have higher docking scores. For hCA II, it was shown that Isotretinoin and Ketotifen would inhibit at lower concentrations and have higher placement scores.

01 Oct 2025·Sleep and Breathing

Reduction of carbonic anhydrase activity is associated with amelioration of obstructive sleep apnea

Article

Author: Grote, Ludger ; Hedner, Jan ; Zou, Ding ; Musovic, Saliha ; Komai, Ali M ; Stenlöf, Kaj

Abstract:

Background:

The carbonic anhydrase (CA) enzyme plays an important role in the equilibration of carbon dioxide and bicarbonate (HCO3) under the production of H+ ions. Emerging evidence suggest that CA activity may play a fundamental regulatory role on respiratory control mechanisms in obstructive sleep apnea (OSA). Clinical trials suggest that CA inhibitors significantly reduce OSA.

Methods:

Data from three separate cohorts of healthy volunteers and patients with OSA were used to quantify CA activity in whole blood and cerebrospinal fluid (CSF). The influence of the CA inhibitory drugs acetazolamide and sulthiame, on CA activity in-vitro/in-vivo, was assessed. The association between CA-inhibitor plasma concentration and HCO3, as well as the influence of HCO3 on the apnea-hypopnea severity was determined.

Results:

Stability of CA activity in stored blood was high. CA activity in whole blood contained five times higher activity compared with CSF. The CA-inhibitory drugs dose-dependently reduced CA activity in-vitro/in-vivo. The CA inhibitor sulthiame reduced venous HCO3 concentration (P = 0.022). The reduction of HCO3 was linked to improvement of OSA (P = 0.040).

Conclusions:

CA-inhibitory drugs reduced CA activity in whole blood suggesting a therapeutic role of CA inhibition in OSA. The findings also suggest that an activated CA system may constitute a pathophysiological mechanism in some forms of OSA.

Clinical trial registration:

N/A.

100 Deals associated with CA inhibitor (Sakarya University)

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