Chalcone: a privileged structure in medicinal chemistry

C Zhuang, W Zhang, C Sheng, W Zhang, C Xing… - Chemical …, 2017 - ACS Publications
Privileged structures have been widely used as an effective template in medicinal chemistry
for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring …

Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

S Pan, A Ding, Y Li, Y Sun, Y Zhan, Z Ye… - Chemical Society …, 2023 - pubs.rsc.org
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …

[HTML][HTML] Low-dose metformin targets the lysosomal AMPK pathway through PEN2

T Ma, X Tian, B Zhang, M Li, Y Wang, C Yang, J Wu… - Nature, 2022 - nature.com
Metformin, the most prescribed antidiabetic medicine, has shown other benefits such as anti-
ageing and anticancer effects,,–. For clinical doses of metformin, AMP-activated protein …

Click chemistry in proteomic investigations

CG Parker, MR Pratt - Cell, 2020 - cell.com
Despite advances in genetic and proteomic techniques, a complete portrait of the proteome
and its complement of dynamic interactions and modifications remains a lofty, and as of yet …

Labeling preferences of diazirines with protein biomolecules

AV West, G Muncipinto, HY Wu, AC Huang… - Journal of the …, 2021 - ACS Publications
Diazirines are widely used in photoaffinity labeling (PAL) to trap noncovalent interactions
with biomolecules. However, design and interpretation of PAL experiments is challenging …

Recent advances in activity-based probes (ABPs) and affinity-based probes (A f BPs) for profiling of enzymes

H Fang, B Peng, SY Ong, Q Wu, L Li, SQ Yao - Chemical Science, 2021 - pubs.rsc.org
Activity-based protein profiling (ABPP) is a technique that uses highly selective active-site
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …

Ligand and target discovery by fragment-based screening in human cells

CG Parker, A Galmozzi, Y Wang, BE Correia, K Sasaki… - Cell, 2017 - cell.com
Advances in the synthesis and screening of small-molecule libraries have accelerated the
discovery of chemical probes for studying biological processes. Still, only a small fraction of …

Chemical proteomics approaches for identifying the cellular targets of natural products

MH Wright, SA Sieber - Natural product reports, 2016 - pubs.rsc.org
Covering: 2010 up to 2016 Deconvoluting the mode of action of natural products and drugs
remains one of the biggest challenges in chemistry and biology today. Chemical proteomics …

Activation of human STING by a molecular glue-like compound

J Li, SM Canham, H Wu, M Henault, L Chen… - Nature chemical …, 2024 - nature.com
Stimulator of interferon genes (STING) is a dimeric transmembrane adapter protein that
plays a key role in the human innate immune response to infection and has been …

Recent advances in identifying protein targets in drug discovery

J Ha, H Park, J Park, SB Park - Cell chemical biology, 2021 - cell.com
Phenotype-based screening has emerged as an alternative route for discovering new
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …