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 …

Targeting ribonucleases with small molecules and bifunctional molecules

L Borgelt, P Wu - ACS Chemical Biology, 2023 - ACS Publications
Ribonucleases (RNases) cleave and process RNAs, thereby regulating the biogenesis,
metabolism, and degradation of coding and noncoding RNAs. Thus, small molecules …

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 …

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 …

New anti-viral drugs for the treatment of COVID-19 instead of favipiravir

A Aktaş, B Tüzün, R Aslan, K Sayin… - Journal of Biomolecular …, 2021 - Taylor & Francis
The SARS-CoV-2 virus is a major problem in the world right now. Currently, all the attention
of research centers and governments globally are focused on the investigation of …

Development of human carbonic anhydrase II heterobifunctional degraders

CB O'Herin, YW Moriuchi, TA Bemis… - Journal of Medicinal …, 2023 - ACS Publications
Human carbonic anhydrase II (hCAII) is a metalloenzyme essential to critical physiological
processes in the body. hCA inhibitors are used clinically for the treatment of indications …

Are clarithromycin, azithromycin and their analogues effective in the treatment of COVID19?

MA Gedikli, B Tuzun, A Aktas… - Bratislava Medical …, 2021 - search.ebscohost.com
Abstract BACKGROUND: SARS-CoV-2, which started in Wuhan and later affected the whole
world, is the most important disease of the world today. Many ways to inhibit SARS-CoV-2 …

Highly efficient electrocarboxylation method to synthesize novel acid derivatives of 1, 4-dihydropyridines and to study their antimicrobial activity

DS Malhi, HS Sohal, K Singh, ZM Almarhoon… - ACS …, 2022 - ACS Publications
1, 4-Dihydropyridines (1, 4-DHPs) hold a top-notch position in the pharmaceutical world due
to a broader spectrum of applications, whereas the carboxylic moiety has been an integral …

An overview of hydroxypyranone and hydroxypyridinone as privileged scaffolds for novel drug discovery

M He, M Fan, Z Peng, G Wang - European Journal of Medicinal Chemistry, 2021 - Elsevier
Hydroxypyranone and hydroxypyridinone are important oxygen-containing or nitrogen-
containing heterocyclic nucleus and attracted increasing attention in medicinal chemistry …