ArticleBiochemistry2016
The Structure of Carbonic Anhydrase IX Is Adapted for Low-pH Catalysis.
Article in Biochemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 62 citations in OpenAlex.
- Click Chemistry-Enabled Parallel Synthesis ofMolecules (Basel, Switzerland) · 2026Article
- Design, Synthesis, Anticancer Screening, and Mechanistic Study of Spiro-N-(4-sulfamoyl-phenyl)-1,3,4-thiadiazole-2-carboxamide Derivatives.International journal of molecular sciences · 2025Article
- Preclinical evaluation and automated synthesis of [EJNMMI radiopharmacy and chemistry · 2024Article
- Synthesis and biological evaluation of new 3-substituted coumarin derivatives as selective inhibitors of human carbonic anhydrase IX and XII.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Novel Thiopyrano[2,3-ACS omega · 2023Article
- Article
- Proton export upregulates aerobic glycolysis.BMC biology · 2022Article
- Review
- Novel humanized monoclonal antibodies for targeting hypoxic human tumors via two distinct extracellular domains of carbonic anhydrase IX.Cancer & metabolism · 2022Article
- Understanding metabolic alterations and heterogeneity in cancer progression through validated immunodetection of key molecular components: a case of carbonic anhydrase IX.Cancer metastasis reviews · 2021Review
- Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer.Journal of medicinal chemistry · 2021Article
- Novel insights on saccharin- and acesulfame-based carbonic anhydrase inhibitors: design, synthesis, modelling investigations and biological activity evaluation.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Plasmatic exosomes from prostate cancer patients show increased carbonic anhydrase IX expression and activity and low pH.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- In Silico Identification and Biological Evaluation of Antioxidant Food Components Endowed with IX and XIIAntioxidants (Basel, Switzerland) · 2020Article
- The control of acidity in tumor cells: a biophysical model.Scientific reports · 2020Article
- Biophysical Characterization of Cancer-Related Carbonic Anhydrase IX.International journal of molecular sciences · 2020Article
- How and Why Are Cancers Acidic? Carbonic Anhydrase IX and the Homeostatic Control of Tumour Extracellular pH.Cancers · 2020Review
- Extending the Inhibition Profiles of Coumarin-Based Compounds Against Human Carbonic Anhydrases: Synthesis, Biological, and In Silico Evaluation.Molecules (Basel, Switzerland) · 2019Article
- Structural comparison of protiated, H/D-exchanged and deuterated human carbonic anhydrase IX.Acta crystallographica. Section D, Structural biology · 2019Article
- Causes, consequences, and therapy of tumors acidosis.Cancer metastasis reviews · 2019Review
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
Abstract
Human carbonic anhydrase IX (hCA IX) expression in many cancers is associated with hypoxic tumors and poor patient outcome. Inhibitors of hCA IX have been used as anticancer agents with some entering Phase I clinical trials. hCA IX is transmembrane protein whose catalytic domain faces the extracellular tumor milieu, which is typically associated with an acidic microenvironment. Here, we show that the catalytic domain of hCA IX (hCA IX-c) exhibits the necessary biochemical and biophysical properties that allow for low pH stability and activity. Furthermore, the unfolding process of hCA IX-c appears to be reversible, and its catalytic efficiency is thought to be correlated directly with its stability between pH 3.0 and 8.0 but not above pH 8.0. To rationalize this, we determined the X-ray crystal structure of hCA IX-c to 1.6 Å resolution. Insights from this study suggest an understanding of hCA IX-c stability and activity in low-pH tumor microenvironments and may be applicable to determining pH-related effects on enzymes.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.