Related Experiment Video

Updated: Jul 8, 2026

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
10:20

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b

Published on: November 11, 2016

Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

Claudiu T Supuran1

  • 1Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Rm 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino, Firenze, Italy. claudiu.supuran@unifi.it

Nature Reviews. Drug Discovery
|January 3, 2008
PubMed

Insights

Carbonic anhydrases (CAs) are enzymes with roles in many diseases. Inhibitors and activators of CAs show promise for treating obesity, cancer, infections, and Alzheimer's disease.

Area of Science:

  • Biochemistry
  • Enzymology
  • Pharmacology

Background:

  • Carbonic anhydrases (CAs) are essential metalloenzymes involved in critical physiological and pathological processes.
  • Established roles of CA inhibitors (CAIs) include diuretics and antiglaucoma treatments.
  • Emerging research indicates CAIs have potential as anti-obesity, anticancer, and anti-infective agents.

Purpose of the Study:

  • To discuss the biological basis for novel therapeutic applications of CA modulators.
  • To highlight advancements in developing specific modulators for CA isoforms.
  • To review the potential of CA-targeted therapies for various diseases.

Main Methods:

  • Literature review of CAIs and activators in disease treatment.
  • Analysis of biological rationale for CA modulation in pathology.
  • Overview of clinical trial progress for CA-targeting drugs.

Main Results:

  • CAIs demonstrate potential in anti-obesity, anticancer, and anti-infective therapies.
  • CA activation is being explored as a novel therapeutic strategy for Alzheimer's disease.
  • Specific CA isoform modulators are progressing, with some in clinical trials.

Conclusions:

  • Carbonic anhydrase modulation offers promising therapeutic avenues for diverse diseases.
  • Targeting specific CA isoforms represents a significant advancement in drug development.
  • Further research and clinical evaluation are crucial for realizing the full potential of CA-based therapies.

More Related Videos

A Fluorescence-Based Assay of Membrane Potential for High-Throughput Functional Study of Two Endogenous Ion Channels in Two Epithelial Cell Lines06:59

A Fluorescence-Based Assay of Membrane Potential for High-Throughput Functional Study of Two Endogenous Ion Channels in Two Epithelial Cell Lines

Published on: June 22, 2022

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels10:07

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels

Published on: January 27, 2013

Related Concept Videos

Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors01:30

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
Open Angle Glaucoma: Treatment01:27

Open Angle Glaucoma: Treatment

In open-angle glaucoma, the iridocorneal angle remains open, but the trabecular meshwork becomes stiff, slowing down the outflow of aqueous humor. This causes a buildup of aqueous humor in the anterior chamber, leading to a sudden increase in intraocular pressure. The treatment for open-angle glaucoma focuses on reducing the elevated intraocular pressure by either decreasing the secretion of aqueous humor or increasing its outflow.
Drugs such as carbonic anhydrase inhibitors, α2- and...
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren syndrome.
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include: