[HTML][HTML] Discovery and resupply of pharmacologically active plant-derived natural products: A review

AG Atanasov, B Waltenberger… - Biotechnology …, 2015 - Elsevier
Medicinal plants have historically proven their value as a source of molecules with
therapeutic potential, and nowadays still represent an important pool for the identification of …

Natural products for human health: an historical overview of the drug discovery approaches

S Bernardini, A Tiezzi, V Laghezza Masci… - Natural product …, 2018 - Taylor & Francis
Natural products (NPs) are secondary metabolites produced and used by organisms for
defending or adapting purposes. These molecules were naturally selected during thousands …

PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS

JL Dahlin, JWM Nissink, JM Strasser… - Journal of medicinal …, 2015 - ACS Publications
Significant resources in early drug discovery are spent unknowingly pursuing artifacts and
promiscuous bioactive compounds, while understanding the chemical basis for these …

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 …

Matching the power of high throughput screening to the chemical diversity of natural products

CJ Henrich, JA Beutler - Natural product reports, 2013 - pubs.rsc.org
Matching the power of high throughput screening to the chemical diversity of natural products -
Natural Product Reports (RSC Publishing) DOI:10.1039/C3NP70052F Royal Society of …

The advancing role of fluorogens with AIE characteristics in drug screening

J You, Y Ma, H Song, J Hou, E Zhao - TrAC Trends in Analytical Chemistry, 2024 - Elsevier
As our understanding of diseases deepens, increasing therapeutic targets are being
identified, which facilitates the development of new drug candidates. However, drug …

Identification of small-molecule frequent hitters from AlphaScreen high-throughput screens

K Schorpp, I Rothenaigner, E Salmina… - Journal of …, 2014 - journals.sagepub.com
Although small-molecule drug discovery efforts have focused largely on enzyme, receptor,
and ion-channel targets, there has been an increase in such activities to search for protein …

Optical properties of natural small molecules and their applications in imaging and nanomedicine

H Yuan, A Jiang, H Fang, Y Chen, Z Guo - Advanced Drug Delivery …, 2021 - Elsevier
Natural small molecules derived from plants have fascinated scientists for centuries due to
their practical applications in various fields, especially in nanomedicine. Some of the natural …

High-throughput screening to predict chemical-assay interference

A Borrel, R Huang, S Sakamuru, M **a, A Simeonov… - Scientific Reports, 2020 - nature.com
The US federal consortium on toxicology in the 21st century (Tox21) produces quantitative,
high-throughput screening (HTS) data on thousands of chemicals across a wide range of …

Thiazolidine-2, 4-dione-based irreversible allosteric IKK-β kinase inhibitors: Optimization into in vivo active anti-inflammatory agents

A Elkamhawy, N youn Kim, AHE Hassan, J Park… - European Journal of …, 2020 - Elsevier
Selective kinase inhibitors development is a cumbersome task because of ATP binding sites
similarities across kinases. On contrast, irreversible allosteric covalent inhibition offers …