Emerging role of carbonic anhydrase inhibitors
CT Supuran - Clinical Science, 2021 - portlandpress.com
Inhibition of carbonic anhydrase (CA, EC 4.2. 1.1) was clinically exploited for decades, as
most modern diuretics were obtained considering as lead molecule acetazolamide, the …
most modern diuretics were obtained considering as lead molecule acetazolamide, the …
DNA-encoded chemistry: enabling the deeper sampling of chemical space
RA Goodnow Jr, CE Dumelin, AD Keefe - Nature Reviews Drug …, 2017 - nature.com
DNA-encoded chemical library technologies are increasingly being adopted in drug
discovery for hit and lead generation. DNA-encoded chemistry enables the exploration of …
discovery for hit and lead generation. DNA-encoded chemistry enables the exploration of …
Carbonic anhydrase inhibitors targeting metabolism and tumor microenvironment
The tumor microenvironment is crucial for the growth of cancer cells, triggering particular
biochemical and physiological changes, which frequently influence the outcome of …
biochemical and physiological changes, which frequently influence the outcome of …
Interfering with pH regulation in tumours as a therapeutic strategy
D Neri, CT Supuran - Nature reviews Drug discovery, 2011 - nature.com
The high metabolic rate of tumours often leads to acidosis and hypoxia in poorly perfused
regions. Tumour cells have thus evolved the ability to function in a more acidic environment …
regions. Tumour cells have thus evolved the ability to function in a more acidic environment …
Carbonic anhydrase inhibitors as emerging agents for the treatment and imaging of hypoxic tumors
CT Supuran - Expert opinion on investigational drugs, 2018 - Taylor & Francis
Introduction: Hypoxic tumors overexpress two carbonic anhydrases (CA, EC 4.2. 1.1), CA IX
and XII, involved in complex processes connected to tumorigenesis (pH regulation …
and XII, involved in complex processes connected to tumorigenesis (pH regulation …
Targeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies
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 …
that catalyze a very basic but crucial physiological reaction: the conversion of carbon dioxide …
Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: three for the price of one
CT Supuran, V Alterio, A Di Fiore… - Medicinal Research …, 2018 - Wiley Online Library
Human carbonic anhydrase (CA) IX is a tumor‐associated protein, since it is scarcely
present in normal tissues, but highly overexpressed in a large number of solid tumors, where …
present in normal tissues, but highly overexpressed in a large number of solid tumors, where …
Selection of DNA-encoded chemical libraries against endogenous membrane proteins on live cells
Membrane proteins on the cell surface perform a myriad of biological functions; however,
ligand discovery for membrane proteins is highly challenging, because a natural cellular …
ligand discovery for membrane proteins is highly challenging, because a natural cellular …
Advances in the structural annotation of human carbonic anhydrases and impact on future drug discovery
A Nocentini, CT Supuran - Expert Opinion on Drug Discovery, 2019 - Taylor & Francis
Introduction: Of the 15 human carbonic anhydrase (CA, EC 4.2. 1.1) isoforms known to date,
for 11 the crystal structure is known. Many different classes of CA inhibitors (CAIs) were …
for 11 the crystal structure is known. Many different classes of CA inhibitors (CAIs) were …
Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase
Inorganic anions inhibit the metalloenzyme carbonic anhydrase (CA, EC 4.2. 1.1) generally
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …