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 …

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 …

Carbonic anhydrase inhibitors as antitumor/antimetastatic agents: a patent review (2008–2018)

A Nocentini, CT Supuran - Expert Opinion on Therapeutic Patents, 2018 - Taylor & Francis
Introduction: Human carbonic anhydrases (CA, EC 4.2. 1.1) IX and XII are tumor-associated
proteins, being part of the molecular machinery that tumor cells build as adaptive responses …

Carbonic anhydrase inhibition and the management of hypoxic tumors

CT Supuran - Metabolites, 2017 - mdpi.com
Hypoxia and acidosis are salient features of many tumors, leading to a completely different
metabolism compared to normal cells. Two of the simplest metabolic products, protons and …

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 …

Experimental carbonic anhydrase inhibitors for the treatment of hypoxic tumors

CT Supuran - Journal of Experimental Pharmacology, 2020 - Taylor & Francis
Abstract Carbonic anhydrase (CA, EC 4.2. 1.1) isoforms IX and XII are overexpressed in
many hypoxic tumors as a consequence of the hypoxia inducible factor (HIF) activation …

Recent advances in bioorthogonal click chemistry for enhanced PET and SPECT radiochemistry

X Zhong, J Yan, X Ding, C Su, Y Xu… - Bioconjugate …, 2023 - ACS Publications
Due to their high reaction rate and reliable selectivity, bioorthogonal click reactions have
been extensively investigated in numerous research fields, such as nanotechnology, drug …

Novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene) thiazolidin-2-ylidene) amino) benzenesulfonamides: Synthesis, carbonic anhydrase inhibitory activity, anticancer activity …

WM Eldehna, MF Abo-Ashour, A Nocentini… - European journal of …, 2017 - Elsevier
Herein we report the synthesis of two series of novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)
thiazolidin-2-ylidene) amino) benzenesulfonamides (4a-m and 7a-g). All the newly prepared …

Copper-mediated late-stage radiofluorination: five years of impact on preclinical and clinical PET imaging

JS Wright, T Kaur, S Preshlock, SS Tanzey… - Clinical and translational …, 2020 - Springer
Purpose Copper-mediated radiofluorination (CMRF) is emerging as the method of choice for
the formation of aromatic C–18 F bonds. This minireview examines proof-of-concept …

Advances in PET and MRI imaging of tumor hypoxia

P Gouel, P Decazes, P Vera, I Gardin, S Thureau… - Frontiers in …, 2023 - frontiersin.org
Tumor hypoxia is a complex and evolving phenomenon both in time and space. Molecular
imaging allows to approach these variations, but the tracers used have their own limitations …