Results 31 to 40 of about 665 (203)

The Development of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. Combination of Monoterpene and Adamantine Moieties via Amide or Thioamide Bridges

Applied Sciences, 2019
Eleven amide and thioamide derivatives with monoterpene and adamantine substituents were synthesised. They were tested for their activity against the tyrosyl-DNA phosphodiesterase 1 DNA (Tdp1) repair enzyme with the most potent compound 47a, having an ...
Arina A. Chepanova, Evgenii S. Mozhaitsev, Aldar A. Munkuev, Evgeniy V. Suslov, Dina V. Korchagina, Olga D. Zakharova, Alexandra L. Zakharenko, Jinal Patel, Daniel M. Ayine-Tora, Jóhannes Reynisson, Ivanhoe K. H. Leung, Konstantin P. Volcho, Nariman F. Salakhutdinov, Olga I. Lavrik   +13 more
doaj   +1 more source

Screening of benzenesulfonamide in combination with chemically diverse fragments against carbonic anhydrase by differential scanning fluorimetry

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
The differential scanning fluorimetry (DSF) screening of 5.692 fragments in combination with benzenesulfonamide (BSA) against bovine carbonic anhydrase (bCA) delivered >100 hits that either caused, on their own, a significant thermal shift (ΔTm, °C) in ...
Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasiia Gryniukova, Petro Borysko, Andrea Angeli, Claudiu T. Supuran   +6 more
doaj   +1 more source

SHIP1 therapeutic target enablement: Identification and evaluation of inhibitors for the treatment of late‐onset Alzheimer's disease

Alzheimer’s & Dementia: Translational Research & Clinical Interventions, 2023
INTRODUCTION The risk of developing Alzheimer's disease is associated with genes involved in microglial function. Inositol polyphosphate‐5‐phosphatase (INPP5D), which encodes Src homology 2 (SH2) domain–containing inositol polyphosphate 5‐phosphatase 1 ...
Cynthia D. Jesudason, Emily R. Mason, Shaoyou Chu, Adrian L. Oblak, June Javens‐Wolfe, Mustapha Moussaif, Greg Durst, Philip Hipskind, Daniel E. Beck, Jiajun Dong, Ovini Amarasinghe, Zhong‐Yin Zhang, Adam K. Hamdani, Kratika Singhal, Andrew D. Mesecar, Sarah Souza, Marlene Jacobson, Jerry Di Salvo, Disha M. Soni, Murugesh Kandasamy, Andrea R. Masters, Sara K Quinney, Suzanne Doolen, Hasi Huhe, Stacey J. Sukoff Rizzo, Bruce T. Lamb, Alan D. Palkowitz, Timothy I. Richardson   +27 more
doaj   +1 more source

Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays

Acta Pharmaceutica Sinica B, 2022
SARS-CoV-2 main protease (Mpro) is one of the most extensively exploited drug targets for COVID-19. Structurally disparate compounds have been reported as Mpro inhibitors, raising the question of their target specificity.
Chunlong Ma, Haozhou Tan, Juliana Choza, Yuyin Wang, Jun Wang   +4 more
doaj   +1 more source

Identification and development of novel indazole derivatives as potent bacterial peptidoglycan synthesis inhibitors

International Journal of Mycobacteriology, 2018
Background: Tuberculosis is well-known airborne disease caused by Mycobacterium tuberculosis. Available treatment regimen was unsuccessful in eradicating the deaths caused by the disease worldwide.
Prasanthi Malapati, Vagolu Siva Krishna, Sriram Dharmarajan   +2 more
doaj   +1 more source

Assembly and Cryo-EM structure determination of yeast mitochondrial RNA polymerase initiation complex intermediates

STAR Protocols, 2021
Summary: In yeast mitochondria, transcription initiation requires assembly of mitochondrial RNA polymerase and transcription initiation factor MTF1 at the DNA promoter initiation site.
Sergio E. Martinez, Anupam Singh, Brent De Wijngaert, Shemaila Sultana, Chhaya Dharia, Hans Vanbuel, Jiayu Shen, Daniel Vasilchuk, Smita S. Patel, Kalyan Das   +9 more
doaj   +1 more source

Determination of Ligand-Target Interaction in vitro by Cellular Thermal Shift Assay and Isothermal Dose-response Fingerprint Assay

Bio-Protocol
The cellular thermal shift assay (CETSA) and isothermal dose-response fingerprint assay (ITDRF CETSA) have been introduced as powerful tools for investigating target engagement by measuring ligand-triggered thermodynamic stabilization of cellular target ...
Danyu Du, Shengtao Yuan, Jing Xiong
doaj   +1 more source

Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system

FEBS Letters, EarlyView.
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley   +1 more source

nanoDSF: In vitro Label-Free Method to Monitor Picornavirus Uncoating and Test Compounds Affecting Particle Stability

Frontiers in Microbiology, 2020
Thermal shift assays measure the stability of macromolecules and macromolecular assemblies as a function of temperature. The Particle Stability Thermal Release Assay (PaSTRy) of picornaviruses is based on probes becoming strongly fluorescent upon binding
Antonio Real-Hohn, Martin Groznica, Nadine Löffler, Dieter Blaas, Heinrich Kowalski   +4 more
doaj   +1 more source

Modulation of Homer1 EVH1 domain internal dynamics by putative autism‐associated mutations

FEBS Letters, EarlyView.
The putative autism‐associated M65I and S97L variants of the EVH1 domain of the postsynaptic scaffold protein Homer1 do not exhibit substantial changes in their overall structure or partner binding. Both of them, but especially the M65I variant, show altered internal dynamics relative to the wild‐type domain on the μs‐ms timescale, indicated by the ...
Fanni Farkas, Brigitta Maruzs, Zsófia E. Kálmán, Tomas Klumpler, Gyula Batta, Bálint Péterfia, Zoltán Gáspári   +6 more
wiley   +1 more source