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 …
Multiple Binding Modes of Inhibitors to Human Carbonic Anhydrases: An Update on the Design of Isoform-Specific Modulators of Activity
K D'Ambrosio, A Di Fiore, V Alterio, E Langella… - Chemical …, 2024 - ACS Publications
Human carbonic anhydrases (hCAs) are widespread zinc enzymes that catalyze the
hydration of CO2 to bicarbonate and a proton. Currently, 15 isoforms have been identified, of …
hydration of CO2 to bicarbonate and a proton. Currently, 15 isoforms have been identified, of …
Bioactivity, cytotoxicity, and molecular modeling studies of novel sulfonamides as dual inhibitors of carbonic anhydrases and acetylcholinesterase
In the present medical epoch, the prevailing approach of drug discovery, which focuses on
inhibiting a single target, has been superseded by the concept of designing drugs that target …
inhibiting a single target, has been superseded by the concept of designing drugs that target …
Identification of novel discoidin domain receptor 1 (DDR1) inhibitors using E-pharmacophore modeling, structure-based virtual screening, molecular dynamics …
Dysregulation of the discoidin domain receptor (DDR1), a collagen-activated receptor
tyrosine kinase, has been linked to several human cancer diseases including non-small cell …
tyrosine kinase, has been linked to several human cancer diseases including non-small cell …
Discovery of novel pyridazine-tethered sulfonamides as carbonic anhydrase II inhibitors for the management of glaucoma
As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left
untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective …
untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective …
Tumor-associated carbonic anhydrase isoform IX and XII inhibitory properties of certain isatin-bearing sulfonamides endowed with in vitro antitumor activity towards …
Three series of indolinone-based sulfonamides (3a–f, 6a–f and 9a–f) were in vitro evaluated
as inhibitors of the tumor-associated carbonic anhydrase (CA, EC 4.2. 1.1) isoforms hCA IX …
as inhibitors of the tumor-associated carbonic anhydrase (CA, EC 4.2. 1.1) isoforms hCA IX …
Structure-activity relationship of human carbonic anhydrase-II inhibitors: Detailed insight for future development as anti-glaucoma agents
Human carbonic anhydrase-II (hCA-II) is the most dominant physiologic isoform amongst the
sixteen reported hCA isoforms. Because of its high availability in the different anatomical …
sixteen reported hCA isoforms. Because of its high availability in the different anatomical …
SLC-0111 enaminone analogs, 3/4-(3-aryl-3-oxopropenyl) aminobenzenesulfonamides, as novel selective subnanomolar inhibitors of the tumor-associated carbonic …
SLC-0111, an ureido substituted benzenesulfonamide, is a selective carbonic anhydrase
(CA, EC 4.2. 1.1) IX inhibitor that is currently in Phase I/II clinical trials for the treatment of …
(CA, EC 4.2. 1.1) IX inhibitor that is currently in Phase I/II clinical trials for the treatment of …
Advances in the discovery of novel agents for the treatment of glaucoma
Introduction Glaucoma, a neuropathy characterized by increased intraocular pressure (IOP),
is the major cause of blindness worldwide and its treatment aims at reducing IOP. Areas …
is the major cause of blindness worldwide and its treatment aims at reducing IOP. Areas …
Identification of 1H-purine-2, 6-dione derivative as a potential SARS-CoV-2 main protease inhibitor: molecular docking, dynamic simulations, and energy calculations
The rapid spread of the coronavirus since its first appearance in 2019 has taken the world by
surprise, challenging the global economy, and putting pressure on healthcare systems …
surprise, challenging the global economy, and putting pressure on healthcare systems …