PatentDOI
Carbonic anhydrase inhibitors
Peter Ebbesen,Claudlu T. Supuran,Andrea Scozzafava,Erik Olai Pettersen,Kaye Williams,L.J. Dubois,Philippe Lambin +6 more
TLDR
A carbonic anhydrase IX (CA IX) inhibitor is a compound of general formula: R-NH-CX-NH-(CH 2 ) n -Ar-Q-SO 2 -NH 2 or a pharmaceutically acceptable salt, derivative or prodrug thereof.Abstract:
A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R-NH-CX-NH-(CH 2 ) n -Ar-Q-SO 2 -NH 2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n = 0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.read more
Citations
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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.
Journal ArticleDOI
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.
Journal ArticleDOI
Antioxidant activity of food constituents: an overview
TL;DR: The most commonly methods used in vitro determination of antioxidant capacity of food constituents are reviewed and presented, and the general chemistry underlying the assays in the present paper was clarified.
Journal ArticleDOI
Targeting metabolic transformation for cancer therapy
TL;DR: This Review highlights pathways against which there are already drugs in different stages of development and also discusses additional druggable targets.
References
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Book
Remington's pharmaceutical sciences
TL;DR: The 17th edition of Remington's pharmaceutical sciences is organized as its immediate predecessors, adhering to the concept of division into 9 parts, each subdivided into several chapters as mentioned in this paper.
Journal ArticleDOI
Drug Discovery: A Historical Perspective
TL;DR: The biotech industry is establishing itself as the discovery arm of the pharmaceutical industry, and in bridging the gap between academia and large pharmaceutical companies, the biotech firms have been effective instruments of technology transfer.
Journal Article
Association between Tumor Hypoxia and Malignant Progression in Advanced Cancer of the Uterine Cervix
TL;DR: Tumor oxygenation as measured with a standardized polarographic method proved to be a powerful new pretherapeutic prognostic parameter providing important information on malignant progression in terms of extracervical tumor spread and radioresistance in advanced cervical cancers.
Journal ArticleDOI
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.