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
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
-
Urinary Tract Tumors, Biology and Risk for Artificial Sweeteners Use with Particular Emphasis on some South American Countries
Current Nutrition & Food Science Conditionally Replicating Adenoviruses for Cancer Treatment
Current Cancer Drug Targets Subject Index to Volume 7
Combinatorial Chemistry & High Throughput Screening Innovative Treatment Approach for Cancer-Related Cachexia
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Meta-Analysis of Anticancer Drug Structures - Significance of Their Polar Allylic Moieties
Anti-Cancer Agents in Medicinal Chemistry Targeting p53 in Cancer
Current Medicinal Chemistry - Anti-Cancer Agents The Role of Emerging Genomics and Proteomics Technologies in Cancer Drug Target Discovery
Current Cancer Drug Targets <i>In vitro</i> and <i>in vivo</i> Evaluation of 17-phenylpropylamine/phenoxyethylamine- 17-demethoxygeldanamycins as Potent Hsp90 Inhibitors
Medicinal Chemistry The Potential Role of Claudins in Regulation of Metastasis and Development of Drug Resistance in Breast Cancer
Clinical Cancer Drugs Compounds that Combine Aldose Reductase Inhibitory Activity and Ability to Prevent the Glycation (Glucation and/or Fructation) of Proteins as Putative Pharmacotherapeutic Agents
Drug Design Reviews - Online (Discontinued) Genistein: A Boon for Mitigating Ischemic Stroke
Current Topics in Medicinal Chemistry Down with the Erythropoietin. Long Live the Erythropoietin !
Current Drug Targets Tissue Protective and Anti-Fibrotic Actions of Suramin: New Uses of an Old Drug
Current Clinical Pharmacology Design of New Oxazaphosphorine Anticancer Drugs
Current Pharmaceutical Design Regulation of Tumor Immune Microenvironment by Sphingolipids and Lysophosphatidic Acid
Current Drug Targets Midkine in Inflammatory and Toxic Conditions
Current Drug Delivery Biomacromolecule-Functionalized Nanoparticle-Based Conjugates for Potentiation of Anticancer Therapy
Current Cancer Drug Targets Glycoconjugates As Vaccines for Cancer Immunotherapy: Clinical Trials and Future Directions
Anti-Cancer Agents in Medicinal Chemistry Treatment of Radiation Nephropathy with ACE Inhibitors and AII Type-1 and Type-2 Receptor Antagonists
Current Pharmaceutical Design In Vivo Biological Evaluation of Ethyl 4-(7-hydroxy-4-methyl-2-oxoquinolin-1- ylamino)-coumarin-3-carboxylate as an Antitumor Agent
Anti-Cancer Agents in Medicinal Chemistry