Abstract
Of the thirteen active carbonic anhydrase (CA) isozymes, the transmembrane isoform CA IX has been shown to be linked with carcinogenesis. CA IX presents an ectopic expression in a multitude of carcinomas derived from cervix, uteri, kidney, lung, oesophagus, breast, colon, etc., contrasting with its restricted expression in normal tissues, namely in the epithelia of the gastrointestinal tract. It has been demonstrated that this membrane-bound CA is strongly overexpressed in hypoxic tumors, participating in tumor cell environment acidosis and contributing to malignant progression and poor treatment outcome. Targeting CA IX could thus be an important means of controlling cancer disease. Modulation of extracellular tumor pH via inhibition of CA IX activity represents a promising approach to novel anticancer therapies. Much attention has recently been paid to the CA IX inhibitors drug design, and efforts have been made to obtain isozyme IX inhibitors, with putative applications as antitumor drugs/diagnostic agents. This review will focus on the different CA IX inhibitors described in the literature which could represent excellent potential as candidate therapeutic agents in cancer chemotherapy.
Keywords: Carbonic anhydrase IX, anticancer agents, enzyme inhibition, sulfonamide, sulfamide, sulfamate
Anti-Cancer Agents in Medicinal Chemistry
Title: Inhibition of Carbonic Anhydrase IX: A New Strategy Against Cancer
Volume: 9 Issue: 6
Author(s): Jean-Yves Winum, Andrea Scozzafava, Jean-Louis Montero and Claudiu T. Supuran
Affiliation:
Keywords: Carbonic anhydrase IX, anticancer agents, enzyme inhibition, sulfonamide, sulfamide, sulfamate
Abstract: Of the thirteen active carbonic anhydrase (CA) isozymes, the transmembrane isoform CA IX has been shown to be linked with carcinogenesis. CA IX presents an ectopic expression in a multitude of carcinomas derived from cervix, uteri, kidney, lung, oesophagus, breast, colon, etc., contrasting with its restricted expression in normal tissues, namely in the epithelia of the gastrointestinal tract. It has been demonstrated that this membrane-bound CA is strongly overexpressed in hypoxic tumors, participating in tumor cell environment acidosis and contributing to malignant progression and poor treatment outcome. Targeting CA IX could thus be an important means of controlling cancer disease. Modulation of extracellular tumor pH via inhibition of CA IX activity represents a promising approach to novel anticancer therapies. Much attention has recently been paid to the CA IX inhibitors drug design, and efforts have been made to obtain isozyme IX inhibitors, with putative applications as antitumor drugs/diagnostic agents. This review will focus on the different CA IX inhibitors described in the literature which could represent excellent potential as candidate therapeutic agents in cancer chemotherapy.
Export Options
About this article
Cite this article as:
Winum Jean-Yves, Scozzafava Andrea, Montero Jean-Louis and Supuran T. Claudiu, Inhibition of Carbonic Anhydrase IX: A New Strategy Against Cancer, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (6) . https://dx.doi.org/10.2174/187152009788680028
DOI https://dx.doi.org/10.2174/187152009788680028 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
An Association of Virus Infection with Type 2 Diabetes and Alzheimer’s Disease
CNS & Neurological Disorders - Drug Targets A Review on Metal Nanoparticles from Medicinal Plants: Synthesis, Characterization and Applications
Nanoscience & Nanotechnology-Asia Volatile Disease Biomarkers in Breath: A Critique
Current Pharmaceutical Biotechnology The Activity of Titanocene T Against Xenografted Caki-1 Tumors
Letters in Drug Design & Discovery Prognostic Markers in Small Cell Lung Cancer
Current Cancer Therapy Reviews Design, Synthesis and Antitumor Activities of Bis-arylureas and Bis-arylamides Based on1H-benzo[d]imidazole Moiety as Novel BRaf<sup>V600E</sup>/VEGFR2 Dual inhibitors
Letters in Drug Design & Discovery Nanotechnology and Radiopharmaceuticals: Diagnostic and Therapeutic Approaches
Current Drug Delivery Requirements and Perspectives for Integrating Metabolomics with other Omics Data
Current Metabolomics Synthesis and Antitumor Activities of 3-Substituted 1-(5-formylfurfuryl)indolin-2-one Derivatives
Letters in Organic Chemistry Oncogenic Fusion Tyrosine Kinases as Molecular Targets for Anti-Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry When Ubiquitin Meets NF-κB: A Trove for Anti-cancer Drug Development
Current Pharmaceutical Design The Changing Face of HDAC Inhibitor Depsipeptide
Current Cancer Drug Targets Aliphatic and Aromatic Oxidations, Epoxidation and S-Oxidation of Prodrugs that Yield Active Drug Metabolites
Current Medicinal Chemistry The Genetic Basis of New Treatment Modalities in Melanoma
Current Drug Targets Structural Basis of Tetherin Function
Current HIV Research Pregnancy and Viral Hepatitis: Current Concepts
Current Pharmaceutical Design Adult Neural Stem Cells: Response to Stroke Injury and Potential for Therapeutic Applications
Current Stem Cell Research & Therapy Depsipeptide (FK228) as a Novel Histone Deacetylase Inhibitor: Mechanism of Action and Anticancer Activity
Mini-Reviews in Medicinal Chemistry Inhibiting HSP90 to Treat Cancer: A Strategy in Evolution
Current Molecular Medicine Clinical Approaches Toward Tumor Angiogenesis: Past, Present and Future
Current Pharmaceutical Design