Journal ArticleDOI
Advances in structure-based drug discovery of carbonic anhydrase inhibitors.
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TLDR
Detailed structural characterization of all CAI classes may lead to further advances in the field with potential therapeutic implications in the management of indications including neuropathic pain, cerebral ischemia, arthritis and tumor imaging.Abstract:
Introduction: The enzyme carbonic anhydrase (CA, EC 4211) is found in numerous organisms across the tree of life, with seven distinct classes known to date CA inhibition can be exploited for thread more
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Targeting Tumor Microenvironment for Cancer Therapy.
TL;DR: In this article, a big effort has been made to develop new therapeutic strategies towards a more efficient targeting of tumor microenvironment (TME) components, extending from conventional therapeutics, to combined therapies and nanomedicines; and the development of models that accurately resemble the TME for bench investigations.
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Carbonic Anhydrase Inhibition and the Management of Hypoxic Tumors
TL;DR: The state of the art on the development of CA inhibitors (CAIs) targeting the tumor-associated CA isoforms, which may have applications for the treatment and imaging of cancers expressing them are presented.
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Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: Three for the price of one.
Claudiu T. Supuran,Vincenzo Alterio,Anna Di Fiore,Katia D’ Ambrosio,Fabrizio Carta,Simona Maria Monti,Giuseppina De Simone +6 more
TL;DR: Aim of this review is to provide a comprehensive state‐of‐the‐art of studies performed on this enzyme, regarding structural, functional, and biomedical aspects, as well as the development of molecules with diagnostic and therapeutic applications for cancer treatment.
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Carbonic anhydrase inhibitors as emerging agents for the treatment and imaging of hypoxic tumors.
TL;DR: CA IX/XII inhibitors are synergistic with other anticancer agents and are a versatile, emerging class of antitumor drugs that make them unique among anticancer drugs available.
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Targeting Metalloenzymes for Therapeutic Intervention
Allie Y. Chen,Rebecca N Adamek,Benjamin L. Dick,Cy V. Credille,Christine N. Morrison,Seth M. Cohen +5 more
TL;DR: This Review provides a broad overview of several drug discovery efforts focused on metalloenzymes and attempts to map out the current landscape of high-value metaloenzyme targets.
References
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Journal ArticleDOI
Carbonic anhydrases: novel therapeutic applications for inhibitors and activators
TL;DR: The biological rationale for the novel uses of inhibitors or activators of CA activity in multiple diseases is discussed, and progress in the development of specific modulators of the relevant CA isoforms is highlighted, some of which are now being evaluated in clinical trials.
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The Carbon Dioxide Hydration Activity of Carbonic Anhydrase I. STOP-FLOW KINETIC STUDIES ON THE NATIVE HUMAN ISOENZYMES B AND C
TL;DR: The present kinetic results are interpreted as representing a great specificity of carbonic anhydrase for the binding of its substrate CO2, and it is proposed that the enzyme-catalyzed hydration of CO2 requires, not only water activation by a basic group, but also charge neutralization in the transition state by an electron acceptor function.
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Interfering with pH regulation in tumours as a therapeutic strategy
Dario Neri,Claudiu T. Supuran +1 more
TL;DR: Key pH regulators in tumour cells include: isoforms 2, 9 and 12 of carbonic anhydrase, isoforms of anion exchangers, Na+/HCO3− co-transporters, Na+./H+ exchanger, monocarboxylate transporters and the vacuolar ATPase.
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Multiple Binding Modes of Inhibitors to Carbonic Anhydrases: How to Design Specific Drugs Targeting 15 Different Isoforms?
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Carbonic Anhydrase Inhibitors
TL;DR: The use of such enzyme inhibitors as antiglaucoma drugs will be discussed in detail, together with the recent developments that led to isozyme-specific and organ-selective inhibitors.