Results 21 to 30 of about 8,600 (184)

Design, synthesis and in vitro evaluation of novel inhibitors and degraders of Zn2+-dependent histone deacetylases [PDF]

, 2022
Histon-Deacetylasen (HDACs) deacetylieren Histonen und Nicht-Histon-Proteinen. Die vorgestellte Arbeit zeigt die Entwicklung neuartiger Inhibitoren und Degrader von HDAC6 und HDAC8.
Darwish, Salma Abdelaziz Ahmed Hassan
core   +1 more source

Characterization of siderophore produced by Pseudomonas sp. MT and its antagonist activity against Fusarium oxysporum f. sp. cubense and F. oxysporium f. sp. ciceris

Notulae Scientia Biologicae, 2022
Siderophores are low molecular weight iron scavengers produced by bacteria to combat iron stress and also suppress deleterious rhizobacteria. In the present study, microbes were isolated from wheat and tobacco farm in Changa village, Anand district ...
Mrugesh AMIN, Trupti K. VYAS
doaj   +1 more source

A Therapeutic Perspective of HDAC8 in Different Diseases: An Overview of Selective Inhibitors [PDF]

, 2022
Histone deacetylases (HDACs) are epigenetic enzymes which participate in transcriptional repression and chromatin condensation mechanisms by removing the acetyl moiety from acetylated ε-amino group of histone lysines and other non-histone proteins.
Butini S., Campiani G., Carullo G., Cursaro I., Fontana A., Gemma S.   +5 more
core   +1 more source

Mechanistic Insights into Binding of Ligands with Thiazolidinedione Warhead to Human Histone Deacetylase 4

Pharmaceuticals, 2021
Recently, we have reported that non-hydroxamate thiazolidinedione (TZD) analogs are capable of inhibiting human deacetylase 4 (HDAC4). This study aims at the dissection of the molecular determinants and kinetics of the molecular recognition of TZD ...
Markus Schweipert, Niklas Jänsch, Neha Upadhyay, Kalpana Tilekar, Ewelina Wozny, Sidra Basheer, Eva Wurster, Marlene Müller, Ramaa C S, Franz-Josef Meyer-Almes   +9 more
doaj   +1 more source

Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity [PDF]

Journal of Medicinal Chemistry, 2020
UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) is a zinc metalloenzyme that catalyzes the first committed step in the biosynthesis of Lipid A, an essential component of the cell envelope of Gram-negative bacteria. The most advanced, disclosed LpxC inhibitors showing antibacterial activity coordinate zinc through a hydroxamate moiety with concerns ...
Yousuke, Yamada, Hajime, Takashima, David Lee, Walmsley, Fumihito, Ushiyama, Yohei, Matsuda, Harumi, Kanazawa, Toru, Yamaguchi-Sasaki, Nozomi, Tanaka-Yamamoto, Junya, Yamagishi, Risa, Kurimoto-Tsuruta, Yuya, Ogata, Norikazu, Ohtake, Hayley, Angove, Lisa, Baker, Richard, Harris, Alba, Macias, Alan, Robertson, Allan, Surgenor, Hayato, Watanabe, Koichiro, Nakano, Masashi, Mima, Kunihiko, Iwamoto, Atsushi, Okada, Iichiro, Takata, Kosuke, Hitaka, Akihiro, Tanaka, Kiyoko, Fujita, Hiroyuki, Sugiyama, Roderick E, Hubbard   +28 more
openaire   +2 more sources

TP0586532, a non-hydroxamate LpxC inhibitor, has in vitro and in vivo antibacterial activities against Enterobacteriaceae [PDF]

The Journal of Antibiotics, 2021
The emergence of multi-drug resistant pathogenic bacteria, especially Gram-negative bacteria, is a worldwide health problem. New antibiotics directed at previously unexplored targets are urgently needed to overcome resistance to existing antibiotic classes.
Kiyoko Fujita, Iichiro Takata, Ippei Yoshida, Hirotoshi Okumura, Katsumasa Otake, Hajime Takashima, Hiroyuki Sugiyama   +6 more
openaire   +2 more sources

Design, Synthesis and Bioactivity Evaluation of Heterocycle-Containing Mono- and Bisphosphonic Acid Compounds

Molecules, 2023
Fosmidomycin (FOS) is a naturally occurring compound active against the 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) enzyme in the 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway, and using it as a template for lead structure design is an ...
Xin Wu, Zili Yang, Mengwei Bu, Jiang Duan, Aidong Zhang   +4 more
doaj   +1 more source

The Zinc-Binding Group Effect: Lessons from Non-Hydroxamic Acid Vorinostat Analogs

Journal of Medicinal Chemistry, 2023
Histone deacetylases (HDACs) are enzymes pursued as drug targets in various cancers and several non-oncological conditions, such as inflammation and neurodegenerative disorders. In the past decade, HDAC inhibitors (HDACi) have emerged as relevant pharmaceuticals, with many efforts devoted to the development of new representatives.
Silke Geurs, Dorien Clarisse, Karolien De Bosscher, Matthias D’hooghe   +3 more
openaire   +3 more sources

Elucidating the molecular programming of a nonlinear non-ribosomal peptide synthetase responsible for fungal siderophore biosynthesis

Nature Communications, 2023
Siderophores belonging to the ferrichrome family are essential for the viability of fungal species and play a key role for virulence of numerous pathogenic fungi. Despite their biological significance, our understanding of how these iron-chelating cyclic
Matthew Jenner, Yang Hai, Hong H. Nguyen, Munro Passmore, Will Skyrud, Junyong Kim, Neil K. Garg, Wenjun Zhang, Rachel R. Ogorzalek Loo, Yi Tang   +9 more
doaj   +1 more source

ADAM17 as a promising therapeutic target: from structural basis to inhibitor discovery in human diseases. [PDF]

Front Pharmacol
A disintegrin and metalloproteinase 17 (ADAM17) is a transmembrane protease that regulates diverse physiological processes by shedding membrane-bound proteins, including cytokines, their receptors, and adhesion molecules.
Liu L, Tian E, Quan S, Su C, Zhou J, Hu S, Bian N, Du S, Li J.   +8 more
europepmc   +3 more sources