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 …
Multiple binding modes of inhibitors to carbonic anhydrases: how to design specific drugs targeting 15 different isoforms?
V Alterio, A Di Fiore, K D'Ambrosio, CT Supuran… - Chemical …, 2012 - ACS Publications
Carbonic anhydrases (CAs, EC 4.2. 1.1) are ubiquitous metallo-enzymes, present
throughout most living organisms and encoded by five evolutionarily unrelated gene …
throughout most living organisms and encoded by five evolutionarily unrelated gene …
Progress in the development of human carbonic anhydrase inhibitors and their pharmacological applications: Where are we today?
Abstract Carbonic anhydrases (CAs, EC 4.2. 1.1) are widely distributed metalloenzymes in
both prokaryotes and eukaryotes. They efficiently catalyze the reversible hydration of carbon …
both prokaryotes and eukaryotes. They efficiently catalyze the reversible hydration of carbon …
Discovery of novel benzenesulfonamides incorporating 1, 2, 3-triazole scaffold as carbonic anhydrase I, II, IX, and XII inhibitors
Sulfonamides are among the most promising potential inhibitors for carbonic anhydrases
(CAs), which are pharmaceutically relevant targets for treating several disease conditions …
(CAs), which are pharmaceutically relevant targets for treating several disease conditions …
A simple yet multifaceted 90 years old, evergreen enzyme: Carbonic anhydrase, its inhibition and activation
CT Supuran - Bioorganic & Medicinal Chemistry Letters, 2023 - Elsevier
Advances in the carbonic anhydrase (CA, EC 4.2. 1.1) research over the last three decades
are presented, with an emphasis on the deciphering of the activation mechanism, the …
are presented, with an emphasis on the deciphering of the activation mechanism, the …
Targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors
Y Lou, PC McDonald, A Oloumi, S Chia, C Ostlund… - Cancer research, 2011 - AACR
Carbonic anhydrase IX (CAIX) is a hypoxia and HIF-1–inducible protein that regulates intra-
and extracellular pH under hypoxic conditions and promotes tumor cell survival and …
and extracellular pH under hypoxic conditions and promotes tumor cell survival and …
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 …
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 …
Overcoming the limits of hypoxia in photodynamic therapy: a carbonic anhydrase IX-targeted approach
A major challenge in photodynamic cancer therapy (PDT) is avoiding PDT-induced hypoxia,
which can lead to cancer recurrence and progression through activation of various …
which can lead to cancer recurrence and progression through activation of various …
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 …