Related Experiment Videos

Carbonic anhydrase inhibitors and the management of cancer

Silvia Pastorekova1, Juraj Kopacek, Jaromir Pastorek

  • 1Center of Molecular Medicine, Institute of Virology, Slovak Academy of Sciences, Dubravska cesta 9, Bratislava, Slovakia. virusipa@savba.sk

Current Topics in Medicinal Chemistry
|May 17, 2007
PubMed

Insights

Carbonic anhydrase inhibitors targeting cancer-associated CA IX and CA XII offer new diagnostic and therapeutic strategies. These inhibitors show promise for cancer imaging, pH modulation, and directly impeding tumor cell survival.

Area of Science:

  • Biochemistry
  • Oncology
  • Pharmacology

Background:

  • Cancer-related carbonic anhydrases (CAs), specifically CA IX and CA XII, play crucial roles in tumor progression.
  • Understanding their catalytic activity in tumors opens avenues for targeted cancer therapies.
  • Selective inhibition of these isoforms presents a promising strategy for cancer treatment.

Purpose of the Study:

  • To review recent advancements in the understanding of cancer-related carbonic anhydrases (CA IX and CA XII).
  • To discuss the development and preclinical evaluation of novel carbonic anhydrase inhibitors.
  • To explore the diagnostic and therapeutic potential of these inhibitors in oncology.

Main Methods:

  • Literature review of expression, regulation, and functional aspects of CA IX and CA XII in cancer.
  • Summary of synthesis strategies for isozyme-selective carbonic anhydrase inhibitors.
  • Analysis of preclinical data for carbonic anhydrase inhibitors as diagnostic and therapeutic agents.

Main Results:

  • Cancer-associated carbonic anhydrases CA IX and CA XII are key targets for cancer therapy.
  • Various classes of inhibitors have been developed and investigated for in vivo imaging, intratumoral pH modulation, and direct anti-tumor effects.
  • Advances in synthesis have yielded highly efficient and isozyme-selective inhibitors.

Conclusions:

  • Selective inhibition of carbonic anhydrases CA IX and CA XII holds significant potential for cancer diagnostics and therapeutics.
  • Carbonic anhydrase inhibitors can be utilized as imaging agents, to enhance chemotherapy efficacy by modulating tumor pH, or as standalone anti-cancer drugs.
  • Further preclinical studies support the development of these inhibitors for clinical application.

Related Concept Videos

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
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...
Urinary Tract Calculi III: Medical Management01:30

Urinary Tract Calculi III: Medical Management

The diagnosis of renal calculi involves several imaging techniques, including non-contrast CT scans and ultrasound. These methods help visualize kidney stones, assess their size and location, and detect possible obstructions. Additionally, Measuring urine pH is useful for diagnosing specific stone types, such as struvite (alkaline pH) and uric acid stones (acidic pH). Cystine stones are primarily linked to cystinuria, a genetic condition. A urinalysis helps detect blood in the urine (hematuria)...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...