Tumour acidosis: from the passenger to the driver's seat

C Corbet, O Feron - Nature Reviews Cancer, 2017 - nature.com
The high metabolic demand of cancer cells leads to an accumulation of H+ ions in the
tumour microenvironment. The disorganized tumour vasculature prevents an efficient wash …

How many carbonic anhydrase inhibition mechanisms exist?

CT Supuran - Journal of enzyme inhibition and medicinal chemistry, 2016 - Taylor & Francis
Six genetic families of the enzyme carbonic anhydrase (CA, EC 4.2. 1.1) were described to
date. Inhibition of CAs has pharmacologic applications in the field of antiglaucoma …

The RCSB Protein Data Bank: views of structural biology for basic and applied research and education

PW Rose, A Prlić, C Bi, WF Bluhm… - Nucleic acids …, 2015 - academic.oup.com
Abstract The RCSB Protein Data Bank (RCSB PDB, http://www. rcsb. org) provides access to
3D structures of biological macromolecules and is one of the leading resources in biology …

Targeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies

M Kciuk, A Gielecińska, S Mujwar… - Journal of Enzyme …, 2022 - Taylor & Francis
Carbonic anhydrases IX and CAXII (CAIX/CAXII) are transmembrane zinc metalloproteins
that catalyze a very basic but crucial physiological reaction: the conversion of carbon dioxide …

NSAIDs and cancer resolution: new paradigms beyond cyclooxygenase

OR Kolawole, K Kashfi - International journal of molecular sciences, 2022 - mdpi.com
Acute inflammation or resolved inflammation is an adaptive host defense mechanism and is
self-limiting, which returns the body to a state of homeostasis. However, unresolved …

How many drug targets are there?

JP Overington, B Al-Lazikani, AL Hopkins - Nature reviews Drug …, 2006 - nature.com
For the past decade, the number of molecular targets for approved drugs has been debated.
Here, we reconcile apparently contradictory previous reports into a comprehensive survey …

Structure-based drug discovery of carbonic anhydrase inhibitors

CT Supuran - Journal of enzyme inhibition and medicinal chemistry, 2012 - Taylor & Francis
Inhibition of the metalloenzyme carbonic anhydrase (CA; EC 4.2. 1.1) has pharmacologic
applications in the field of anti-glaucoma, anti-convulsant and anti-cancer agents. But …

Designed multiple ligands. An emerging drug discovery paradigm

R Morphy, Z Rankovic - Journal of medicinal chemistry, 2005 - ACS Publications
For much of the past century, drug discovery relied largely on the use of animal models of
disease as the first-line screens for testing the compounds produced by medicinal chemists …

Hypoxia-induced carbonic anhydrase IX as a target for cancer therapy: from biology to clinical use

J Pastorek, S Pastorekova - Seminars in cancer biology, 2015 - Elsevier
The tumor microenvironment includes a complicated network of physiological gradients
contributing to plasticity of tumor cells and heterogeneity of tumor tissue. Hypoxia is a key …

Endoplasmic reticulum stress: its role in disease and novel prospects for therapy

AH Schönthal - Scientifica, 2012 - Wiley Online Library
The endoplasmic reticulum (ER) is a multifunctional organelle required for lipid biosynthesis,
calcium storage, and protein folding and processing. A number of physiological and …