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 …

Causes, consequences, and therapy of tumors acidosis

SR Pillai, M Damaghi, Y Marunaka… - Cancer and Metastasis …, 2019 - Springer
While cancer is commonly described as “a disease of the genes,” it is also associated with
massive metabolic reprogramming that is now accepted as a disease “Hallmark.” This …

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 …

1, 3, 4-Thiadiazole: synthesis, reactions, and applications in medicinal, agricultural, and materials chemistry

Y Hu, CY Li, XM Wang, YH Yang, HL Zhu - Chemical reviews, 2014 - ACS Publications
Over the past decades, the bulk of chemists' interests have been on heterocyclic compounds
and their various derivatives as well as their applications in the pharmaceutical and …

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 anhydrases: novel therapeutic applications for inhibitors and activators

CT Supuran - Nature reviews Drug discovery, 2008 - nature.com
Carbonic anhydrases (CAs), a group of ubiquitously expressed metalloenzymes, are
involved in numerous physiological and pathological processes, including …

1, 3, 4‐Thiadiazole and its derivatives: A review on recent progress in biological activities

AK Jain, S Sharma, A Vaidya… - Chemical biology & …, 2013 - Wiley Online Library
The 1, 3, 4‐thiadiazole nucleus is one of the most important and well‐known heterocyclic
nuclei, which is a common and integral feature of a variety of natural products and medicinal …

Thiadiazole—A promising structure in medicinal chemistry

Y Li, J Geng, Y Liu, S Yu, G Zhao - ChemMedChem, 2013 - Wiley Online Library
Many compounds containing a five‐membered heterocyclic ring display exceptional
chemical properties and versatile biological activities. In this Minireview, thiadiazoles are …

Carbonic anhydrases as potential targets against neurovascular unit dysfunction in Alzheimer's disease and stroke

N Lemon, E Canepa, MA Ilies, S Fossati - Frontiers in aging …, 2021 - frontiersin.org
The Neurovascular Unit (NVU) is an important multicellular structure of the central nervous
system (CNS), which participates in the regulation of cerebral blood flow (CBF), delivery of …

Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX

F Abbate, A Casini, T Owa, A Scozzafava… - Bioorganic & medicinal …, 2004 - Elsevier
E7070 [N-(3-chloro-7-indolyl)-1, 4-benzenedisulfonamide] is an anticancer drug candidate
under clinical development for the treatment of several types of cancers. We prove here that …