Kato, Eisuke Kawakami, Kazuhiro Kawabata, Jun
Published in
Journal of enzyme inhibition and medicinal chemistry
Dipeptidyl peptidase 4 (DPP-4) inhibitors are used for the treatment of type-2 diabetes mellitus. Various synthetic inhibitors have been developed to date, and plants containing natural DPP-4 inhibitors have also been identified. Here, 13 plant samples were tested for their DPP-4 inhibitory activity. Macrocarpals A-C were isolated from Eucalyptus g...
Kurup, Sonali McAllister, Bradley Liskova, Pavlina Mistry, Trusha Fanizza, Anthony Stanford, Dan Slawska, Jolanta Keller, Ulrich Hoellein, Alexander
Published in
Journal of enzyme inhibition and medicinal chemistry
Simultaneous inhibition of multiple kinases has been suggested to provide synergistic effects on inhibition of tumour growth and resistance. This study describes the design, synthesis and evaluation of 18 compounds incorporating a pyrrolo[2,3-d]pyrimidine scaffold for dual inhibition of epidermal growth factor receptor kinase (EGFR) and aurora kina...
Pessôa, Marco T C Alves, Silmara L G Taranto, Alex G Villar, José A F P Blanco, Gustavo Barbosa, Leandro A
Published in
Journal of enzyme inhibition and medicinal chemistry
Digoxin and other cardiotonic steroids (CTS) exert their effect by inhibiting Na,K-ATPase (NKA) activity. CTS bind to the various NKA isoforms that are expressed in different cell types, which gives CTS their narrow therapeutic index. We have synthesised a series of digoxin derivatives (γ-Benzylidene digoxin derivatives) with substitutions in the l...
Vermelho, Alane Beatriz da Silva Cardoso, Verônica Ricci Junior, Eduardo Dos Santos, Elisabete Pereira Supuran, Claudiu T
Published in
Journal of enzyme inhibition and medicinal chemistry
Sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors targeting the α-class enzyme from the protozoan pathogen Trypanosoma cruzi, responsible of Chagas disease, were recently reported. Although many such derivatives showed low nanomolar activity in vitro, they were inefficient anti-T. cruzi agents in vivo. Here, we show that by formulating suc...
Ma, Lingman Zhang, Zhen Xue, Xiaowen Wan, Yumeng Ye, Boping Lin, Kejiang
Published in
Journal of enzyme inhibition and medicinal chemistry
Fibrotic diseases have become a major cause of death in the developed world. AdipoR1 agonists are potent inhibitors of fibrotic responses. Here, we focused on the in silico identification of novel AdipoR1 peptide agonists. A homology model was constructed to predict the 3D structure of AdipoR1. By docking to known active peptides, the putative acti...
Lu, Xiaoyun Zhang, Zhang Ren, Xiaomei Wang, Deping Ding, Ke
Published in
Journal of enzyme inhibition and medicinal chemistry
Bcr-AblT315I induced drug resistance remains a major challenge to chronic myelogenous leukemia (CML) treatment. Herein, we reported GZD856 as a novel orally bioavailable Bcr-AblT315I inhibitor, which strongly suppressed the kinase activities of both native Bcr-Abl and the T315I mutant with IC50 values of 19.9 and 15.4 nM, and potently inhibited pro...
Aspatwar, Ashok Hammarén, Milka Koskinen, Sanni Luukinen, Bruno Barker, Harlan Carta, Fabrizio Supuran, Claudiu T Parikka, Mataleena Parkkila, Seppo
Published in
Journal of enzyme inhibition and medicinal chemistry
Inhibition of novel biological pathways in Mycobacterium tuberculosis (Mtb) creates the potential for alternative approaches for treating drug-resistant tuberculosis. In vitro studies have shown that dithiocarbamate-derived β-carbonic anhydrase (β-CA) inhibitors Fc14-594 A and Fc14-584B effectively inhibit the activity of Mtb β-CA enzymes. We scree...
Soydan, Ercan Güler, Ahmet Bıyık, Selim Şentürk, Murat Supuran, Claudiu T Ekinci, Deniz
Published in
Journal of enzyme inhibition and medicinal chemistry
Carbonic anhydrase (CA) enzymes have been shown to play an important role in ion transport and in pH regulation in several organisms. Despite this information and the wealth of knowledge regarding the significance of CA enzymes, few studies have been reported about bee CA enzymes and the hazardous effects of chemicals. Using Apis mellifera as a mod...
Pustenko, Aleksandrs Stepanovs, Dmitrijs Žalubovskis, Raivis Vullo, Daniela Kazaks, Andris Leitans, Janis Tars, Kaspars Supuran, Claudiu T
Published in
Journal of enzyme inhibition and medicinal chemistry
A new chemotype with carbonic anhydrase (CA, EC 4.2.1.1) inhibitory action has been discovered, the homo-sulfocoumarins (3H-1,2-benzoxathiepine 2,2-dioxides) which have been designed considering the (sulfo)coumarins as lead molecules. An original synthetic strategy of a panel of such derivatives led to compounds with a unique inhibitory profile and...
Rinaldi, Federica Hanieh, Patrizia Nadia Longhi, Catia Carradori, Simone Secci, Daniela Zengin, Gokhan Ammendolia, Maria Grazia Mattia, Elena Del Favero, Elena Marianecci, Carlotta
...
Published in
Journal of enzyme inhibition and medicinal chemistry
The aim of the present work is to develop nanoemulsions (NEs), nanosized emulsions, manufactured for improving the delivery of active pharmaceutical ingredients. In particular, nanoemulsions composed of Neem seed oil, contain rich bioactive components, and Tween 20 as nonionic surfactant were prepared. A mean droplet size ranging from 10 to 100 nm ...
