Targeting Metalloenzymes: The “Achilles' Heel” of Viruses and Parasites

D Moianos, GM Prifti, M Makri, G Zoidis - Pharmaceuticals, 2023 - mdpi.com
Metalloenzymes are central to the regulation of a wide range of essential viral and parasitic
functions, including protein degradation, nucleic acid modification, and many others. Given …

Expanding medicinal chemistry into 3D space: Metallofragments as 3D scaffolds for fragment-based drug discovery

CN Morrison, KE Prosser, RW Stokes, A Cordes… - Chemical …, 2020 - pubs.rsc.org
Fragment-based drug discovery (FBDD) is a powerful strategy for the identification of new
bioactive molecules. FBDD relies on fragment libraries, generally of modest size, but of high …

Catechol-mimicking transition-state analogues as non-oxidizable inhibitors of tyrosinases

M Beaumet, LM Lazinski, M Maresca… - European Journal of …, 2023 - Elsevier
Tyrosinases are copper-containing metalloenzymes involved in several processes in both
mammals, insects, bacteria, fungi and plants. Their phenol oxidation properties are …

High-throughput screening for the discovery of enzyme inhibitors

MD Lloyd - Journal of Medicinal Chemistry, 2020 - ACS Publications
Enzymes are common targets in high-throughput screening and related campaigns. An
analysis of papers published between 1990 and 2018 showed that kinases were the most …

Fragment-to-lead medicinal chemistry publications in 2019

W Jahnke, DA Erlanson, IJP De Esch… - Journal of medicinal …, 2020 - ACS Publications
Fragment-based drug discovery (FBDD) has grown and matured to a point where it is
valuable to keep track of its extent and details of application. This Perspective summarizes …

Targeting the conserved active site of splicing machines with specific and selective small molecule modulators

I Silvestri, J Manigrasso, A Andreani, N Brindani… - Nature …, 2024 - nature.com
The self-splicing group II introns are bacterial and organellar ancestors of the nuclear
spliceosome and retro-transposable elements of pharmacological and biotechnological …

SAR exploration of tight-binding inhibitors of influenza virus PA endonuclease

CV Credille, CN Morrison, RW Stokes… - Journal of medicinal …, 2019 - ACS Publications
Significant efforts have been reported on the development of influenza antivirals including
inhibitors of the RNA-dependent RNA polymerase PA N-terminal (PAN) endonuclease …

Synthesis and pyrolysis of ethyl maltol ester

A Dong, Z Yu, T Pan, L Rong, M Lai… - Flavour and …, 2023 - Wiley Online Library
Ethyl maltol is one of the most important aromatic components in food and cigarettes
because of its caramel flavour. However, the development of ethyl maltol is limited by …

A fragment-based drug discovery strategy applied to the identification of NDM-1 β-lactamase inhibitors

J Caburet, B Boucherle, S Bourdillon… - European Journal of …, 2022 - Elsevier
Hydrolysis of β-lactam drugs, a major class of antibiotics, by serine or metallo-β-lactamases
(SBL or MBL) is one of the main mechanisms for antibiotic resistance. New Delhi Metallo-β …

Fragment-based discovery of novel non-hydroxamate LpxC inhibitors with antibacterial activity

Y Yamada, H Takashima, DL Walmsley… - Journal of Medicinal …, 2020 - ACS Publications
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 …