Dual Targeting Strategies in Cancer: Carbonic Anhydrase IX Inhibitors Targeting EGFR or VEGFR-2

Tumor microenvironment influences the process of tumorigenesis, with hypoxia being a characteristic of many solid tumors and an adverse prognostic factor. Carbonic anhydrases (CAs) are highly efficient zinc-containing enzymes that are overexpressed in many cancers, particularly under acidic and hypoxic conditions. CA IX expression promotes cancer cell proliferation, migration, and invasion. Vascular endothelial growth factor receptor-2 (VEGFR-2) is a tyrosine transmembrane (ΤΜ) protein regulating embryonic development, angiogenesis, tissue homeostasis and cancer. Blocking VEGFR-2 signaling is one of the most promising approaches to hindering angiogenesis and growth of cancer cells. The epidermal growth factor receptor (EGFR) is a member of the ERBB family of receptor tyrosine kinases and plays a key role in cancer progression. EGFR is uniquely found in some brain, lung and other cancers. Development of novel strategies to regulate these factors is important for the treatment of tumors. Multifunctional drugs that act on multiple pathways offer a promising approach, improving therapeutic effectiveness while reducing side effects. The present review focuses on novel compounds that inhibit CA IX and target VEGFR-2 or EGFR.

Authors

Institutions

Publication Details

Journal
Molecules
Published
2026-07-01
DOI
https://doi.org/10.3390/molecules31132306
Primary Topic
Enzyme function and inhibition
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Dual Targeting Strategies in Cancer: Carbonic Anhydrase IX Inhibitors Targeting EGFR or VEGFR-2

Eleni Pontiki, Eleftherios Charissopoulos
Molecules
Enzyme function and inhibition
article

Dual Targeting Strategies in Cancer: Carbonic Anhydrase IX Inhibitors Targeting EGFR or VEGFR-2

Eleni Pontiki, Eleftherios Charissopoulos
article en

Abstract

Tumor microenvironment influences the process of tumorigenesis, with hypoxia being a characteristic of many solid tumors and an adverse prognostic factor. Carbonic anhydrases (CAs) are highly efficient zinc-containing enzymes that are overexpressed in many cancers, particularly under acidic and hypoxic conditions. CA IX expression promotes cancer cell proliferation, migration, and invasion. Vascular endothelial growth factor receptor-2 (VEGFR-2) is a tyrosine transmembrane (ΤΜ) protein regulating embryonic development, angiogenesis, tissue homeostasis and cancer. Blocking VEGFR-2 signaling is one of the most promising approaches to hindering angiogenesis and growth of cancer cells. The epidermal growth factor receptor (EGFR) is a member of the ERBB family of receptor tyrosine kinases and plays a key role in cancer progression. EGFR is uniquely found in some brain, lung and other cancers. Development of novel strategies to regulate these factors is important for the treatment of tumors. Multifunctional drugs that act on multiple pathways offer a promising approach, improving therapeutic effectiveness while reducing side effects. The present review focuses on novel compounds that inhibit CA IX and target VEGFR-2 or EGFR.

MoleculesVol. 31(13)
Aristotle University of Thessaloniki (GR)
Openalex Percentile: Top 12%
Enzyme function and inhibition
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.